Claims for Patent: 9,890,147
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Summary for Patent: 9,890,147
Title: | 2,3-benzodiazepines |
Abstract: | What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) ##STR00001## in which R.sup.1a, R.sup.1b, R.sup.1c, R.sup.2, R.sup.3, R.sup.4, R.sup.5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility. |
Inventor(s): | Siegel; Stephan (Berlin, DE), Baurle; Stefan (Berlin, DE), Cleve; Arwed (Berlin, DE), Haendler; Bernard (Berlin, DE), Fernandez-Montalvan; Amaury Ernesto (Berlin, DE), Monning; Ursula (Woltersdorf, DE), Krause; Sabine (Berlin, DE), Lejeune; Pascale (Berlin, DE), Schmees; Norbert (Berlin, DE), Busemann; Matthias (Berlin, DE), Holton; Simon (Berlin, DE), Kuhnke; Joachim (Potsdam, DE) |
Assignee: | Bayer Pharma Aktiengesellshaft (Berlin, DE) |
Application Number: | 14/421,994 |
Patent Claims: | 1. A compound of formula I ##STR00485## in which X represents an oxygen or sulphur atom, and A represents a monocyclic heteroaryl ring which has 5 or 6 ring atoms or
represents a phenyl ring, and R.sup.1a represents hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represents a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy,
C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl,
hydroxy-C.sub.1-C.sub.6-alkoxy, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylcarbonyl or C.sub.1-C.sub.6-alkoxycarbonyl radical, or represents a monocyclic heterocyclyl radical which has 3 to 8 ring atoms and may
optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl,
hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, phenyl, halophenyl,
phenyl-C.sub.1-C.sub.6-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or a
monocyclic heterocyclyl radical which has 3 to 8 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of
halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl,
halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9,
--NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 3 to 8 ring atoms, and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms, and/or by a phenyl radical which for its part may optionally be mono- or
polysubstituted by halogen, C.sub.1-C.sub.3-alkyl and/or C.sub.1-C.sub.3-alkoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy,
cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, --C(.dbd.O)NR.sup.6R.sup.7,
--C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, halo-C.sub.1-C.sub.6-alkyl,
halo-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.3-C.sub.10-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 3 to 8 ring atoms, and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms and which for its part may
optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, C.sub.1-C.sub.3-alkyl and C.sub.1-C.sub.3-alkoxy, and R.sup.1b and R.sup.1c independently of one another represent hydrogen, halogen,
hydroxy, cyano, nitro and/or represent a C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl radical and/or a monocyclic
heterocyclyl radical which has 3 to 8 ring atoms, and R.sup.2 represents a C.sub.1-C.sub.3-alkyl or trifluoromethyl or a C.sub.3- or C.sub.4-cycloalkyl radical, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, amino,
cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy,
C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino,
C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy,
carboxyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, monocyclic heterocyclyl which has 3 to 8 ring atoms and/or monocyclic heteroaryl which
has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, or represent C.sub.3-C.sub.10-cycloalkyl which may optionally be mono- or
polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino,
amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, and/or a monocyclic heterocyclyl radical which has 3 to 8 ring atoms, or represent monocyclic heteroaryl which has 5
or 6 ring atoms and which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy,
C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy,
C.sub.3-C.sub.10-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 3 to 8 ring atoms, or represent monocyclic heterocyclyl which has 3 to 8 ring atoms and which may optionally
be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl,
C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-Cycloalkyl, --C(.dbd.O)R.sup.8,
--S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 3 to 8 ring atoms, or represent phenyl which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of
halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylaminocarbonyl,
C.sub.1-C.sub.6-alkylaminosulphonyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-Cycloalkyl and/or a monocyclic heterocyclyl radical which has
3 to 8 ring atoms, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl,
halo-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl, phenyl, monocyclic heterocyclyl which has 3 to 8 ring atoms or monocyclic heteroaryl which has 5 or 6 ring atoms, where
phenyl, heteroaryl and heterocyclyl may optionally be mono- or disubstituted by halogen, C.sub.1-C.sub.3-alkoxy or C.sub.1-C.sub.3-alkyl, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer,
racemate, tautomer, or physiologically acceptable salt thereof, with the proviso that, if A represents a phenyl ring and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine,
bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylamino-carbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.6-alkyl,
C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl which may optionally be mono- or polysubstituted by identical or different substituents from
the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, monocyclic heterocyclyl which has 3
to 8 ring atoms and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, R.sup.1a does not represent hydrogen,
halogen, cyano, carboxyl, amino or aminosulphonyl, or represent a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino,
C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkoxy, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy,
C.sub.1-C.sub.6-alkylcarbonyl or C.sub.1-C.sub.6-alkoxycarbonyl radical, except that the proviso does not encompass those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen, fluorine, chlorine or bromine and R.sup.5 is
C.sub.1-C.sub.6-alkoxy which is substituted one or more times by identical or different halogens, and R.sup.1a is halogen, and also not encompass those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen and R.sup.5 is
C.sub.1-C.sub.6-alkoxy which is substituted one or more times by identical or different monocyclic heterocyclyl radicals having 3 to 8 ring atoms and/or monocyclic heteroaryl radicals having 5 or 6 ring atoms, it being possible for the stated monocyclic
heterocyclyl and heteroaryl radicals in turn to be optionally monosubstituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a is halogen.
2. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or pyridyl ring, and R.sup.1a represents hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represents a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkoxy, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylcarbonyl or C.sub.1-C.sub.6-alkoxycarbonyl radical, or represents a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, phenyl, halophenyl, phenyl-C.sub.1-C.sub.6-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms and/or by a phenyl radical which for its part may optionally be mono- or polysubstituted by halogen, C.sub.1-C.sub.3-alkyl and/or C.sub.1-C.sub.3-alkoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, --C(.dbd.O)NR.sup.6R.sup.7, C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.3-C.sub.10-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms and which for its part may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, C.sub.1-C.sub.3-alkyl and C.sub.1-C.sub.3-alkoxy, and R.sup.1b and R.sup.1c independently of one another represent hydrogen, halogen, hydroxy, cyano, nitro or represent a C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl radical, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, amino, cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, monocyclic heterocyclyl which has 4 to 7 ring atoms, and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, or represent a C.sub.3-C.sub.10-cycloalkyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heteroaryl which has 5 or 6 ring atoms and which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heterocyclyl which has 4 to 7 ring atoms and which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7 and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylaminocarbonyl, C.sub.1-C.sub.6-alkylaminosulphonyl, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.3-C.sub.10-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.5-cycloalkyl, phenyl, monocyclic heterocyclyl having 5 or 6 ring atoms, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof, with the proviso that, if A represents a phenyl ring and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkoxy-C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkylamino, amino-C.sub.1-C.sub.6-alkyl, monocyclic heterocyclyl which has 4 to 7 ring atoms and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, R.sup.1a does not represent hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represent a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylamino-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkyl, N-(heterocyclyl)-C.sub.1-C.sub.6-alkoxy, hydroxy-C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.6-alkoxy, halo-C.sub.1-C.sub.6-alkyl, halo-C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylcarbonyl or C.sub.1-C.sub.6-alkoxycarbonyl radical, and where the proviso does not embrace those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen, fluorine, chlorine or bromine and R.sup.5 is C.sub.1-C.sub.6-alkoxy which is substituted one or more times by identical or different halogens, and R.sup.1a is halogen, and also not those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen and R.sup.5 is C.sub.1-C.sub.6-alkoxy which is substituted one or more times by identical or different monocyclic heterocyclyl radicals having 4 to 7 ring atoms and/or monocyclic heteroaryl radicals having 5 or 6 ring atoms, it being possible for the stated monocyclic heterocyclyl and heteroaryl radicals in turn to be optionally monosubstituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a is halogen. 3. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or pyridyl ring, and R.sup.1a represents hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represents a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, C.sub.1-C.sub.3-alkylcarbonylamino, C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylcarbonyl or C.sub.1-C.sub.4-alkoxycarbonyl radical, or represents a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, phenyl, halophenyl, phenyl-C.sub.1-C.sub.3-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms, and/or by a phenyl radical which for its part may be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, --C(.dbd.O)NR.sup.6R.sup.7, C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.6-cycloalkyl and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms and which for its part may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, and R.sup.1b represents hydrogen, halogen, hydroxy, cyano, nitro or represents a C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, fluoro-C.sub.1-C.sub.3-alkyl or fluoro-C.sub.1-C.sub.3-alkoxy radical, and R.sup.1c represents hydrogen, fluorine, chlorine, bromine or cyano, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino which may be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, monocyclic heterocyclyl which has 4 to 7 ring atoms, and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, or represent a C.sub.3-C.sub.7-cycloalkyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heteroaryl which has 5 or 6 ring atoms and which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heterocyclyl which has 4 to 7 ring atoms and which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylaminocarbonyl, C.sub.1-C.sub.3-alkylaminosulphonyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl or monocyclic heterocyclyl which has 5 or 6 ring atoms, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof, with the proviso that, if A represents a phenyl ring and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, monocyclic heterocyclyl which has 4 to 7 ring atoms and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, R.sup.1a does not represent hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represent a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, C.sub.1-C.sub.3-alkylcarbonylamino, C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylcarbonyl or C.sub.1-C.sub.4-alkoxycarbonyl radical, and where the proviso does not embrace those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen, fluorine, chlorine or bromine and R.sup.5 is C.sub.1-C.sub.3-alkoxy which is substituted one or more times by identical or different halogens, and R.sup.1a is halogen, and also not those compounds of the formula (I) in which A is phenyl and R.sup.4 is hydrogen and R.sup.5 is C.sub.1-C.sub.3-alkoxy which is substituted one or more times by identical or different monocyclic heterocyclyl radicals having 4 to 7 ring atoms and/or monocyclic heteroaryl radicals having 5 or 6 ring atoms, it being possible for the stated monocyclic heterocyclyl and heteroaryl radicals in turn to be optionally monosubstituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a is halogen. 4. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or pyridyl ring, and R.sup.1a represents a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, phenyl, halophenyl, phenyl-C.sub.1-C.sub.3-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms, and/or by a phenyl radical which for its part may be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, --C(.dbd.O)NR.sup.6R.sup.7, C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.6-cycloalkyl and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms which for its part may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl or methoxy, and R.sup.1b represents hydrogen, halogen, hydroxy, cyano, nitro or represents a C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, fluoro-C.sub.1-C.sub.3-alkyl or fluoro-C.sub.1-C.sub.3-alkoxy radical, and R.sup.1c represents hydrogen, fluorine, chlorine, bromine or cyano, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, or represent C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino which may be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, monocyclic heterocyclyl which has 4 to 7 ring atoms, and/or monocyclic heteroaryl which has 5 or 6 ring atoms, where the monocyclic heterocyclyl and heteroaryl radicals mentioned for their part may optionally be monosubstituted by C.sub.1-C.sub.3-alkyl, or represent a C.sub.3-C.sub.7-cycloalkyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heteroaryl which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent monocyclic heterocyclyl which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represent a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylaminocarbonyl, C.sub.1-C.sub.3-alkylaminosulphonyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.5-cycloalkyl or monocyclic heterocyclyl which has 5 or 6 ring atoms, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof. 5. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or pyridyl ring, and R.sup.1a represents hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represents a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, C.sub.1-C.sub.3-alkylcarbonylamino, C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylcarbonyl or C.sub.1-C.sub.4-alkoxycarbonyl radical, or represents a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, phenyl, halophenyl, phenyl-C.sub.1-C.sub.3-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms, and/or by a phenyl radical which for its part may be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, --C(.dbd.O)NR.sup.6R.sup.7, C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.6-cycloalkyl and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms which for its part may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, and R.sup.1b represents hydrogen, halogen, hydroxy, cyano, nitro or represents a C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy radical, and R.sup.1c represents hydrogen, fluorine, chlorine, bromine or cyano, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 represents a C.sub.3-C.sub.7-cycloalkyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents monocyclic heteroaryl which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents monocyclic heterocyclyl which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)R.sup.8, --S(.dbd.O).sub.2R.sup.9, --NR.sup.6R.sup.7, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylaminocarbonyl, C.sub.1-C.sub.3-alkylaminosulphonyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, R.sup.5 represents hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkylaminosulphonyl, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl or monocyclic heterocyclyl which has 5 or 6 ring atoms, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof. 6. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or pyridyl ring, and R.sup.1a represents hydrogen, halogen, cyano, carboxyl, amino or aminosulphonyl, or represents a C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.2-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylamino, C.sub.1-C.sub.3-alkylcarbonylamino, C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.3-alkylcarbonyl or C.sub.1-C.sub.4-alkoxycarbonyl radical, or represents a monocyclic heterocyclyl radical which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, cyano, nitro, hydroxy, amino, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, phenyl, halophenyl, phenyl-C.sub.1-C.sub.3-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a monocyclic heteroaryl radical which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, hydroxy, amino, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, --NH--S(.dbd.O).sub.2--R.sup.9, and/or by a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or by a monocyclic heteroaryl radical which has 5 or 6 ring atoms, and/or by a phenyl radical which for its part may be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, --C(.dbd.O)NR.sup.6R.sup.7, --C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.6-cycloalkyl and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and/or a monocyclic heteroaryl radical which has 5 or 6 ring atoms which for its part may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, bromine, methyl and/or methoxy, and R.sup.1b represents hydrogen, halogen, hydroxy, cyano, nitro or represents a C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, fluoro-C.sub.1-C.sub.3-alkyl or fluoro-C.sub.1-C.sub.3-alkoxy radical, and R.sup.1c represents hydrogen, fluorine, chlorine, bromine or cyano, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, cyclopropylamino or C.sub.1-C.sub.3-alkylamino, and R.sup.4 represents hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C.sub.1-C.sub.6-alkyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-alkylamino, C.sub.1-C.sub.6-alkylcarbonylamino, C.sub.1-C.sub.6-alkylaminocarbonyl or C.sub.1-C.sub.6-alkyl-aminosulphonyl, and R.sup.5 represents a C.sub.3-C.sub.7-cycloalkyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents monocyclic heteroaryl which has 5 or 6 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents monocyclic heterocyclyl which has 4 to 7 ring atoms and may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, oxo, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of halogen, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, C.sub.1-C.sub.3-alkylamino, amino-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkylaminocarbonyl, C.sub.1-C.sub.3-alkylaminosulphonyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkoxy, C.sub.3-C.sub.6-cycloalkyl, and/or a monocyclic heterocyclyl radical which has 4 to 7 ring atoms, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.6-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, fluoro-C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy-C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.5-cycloalkyl or monocyclic heterocyclyl which has 5 or 6 ring atoms, and R.sup.9 represents hydrogen, C.sub.1-C.sub.6-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof. 7. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or 3-pyridyl ring, and R.sup.1a represents hydrogen or chlorine, or represents piperazinyl, pyrrolidinyl, piperidinyl, diazepanyl, oxazinanyl, oxazolidinyl, morpholinyl, thiomorpholinyl, thiazolidinyl or azetidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, cyano, nitro, hydroxy, oxo, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, dimethylamino, trifluoromethyl, difluoroethyl, trifluoroethyl, trifluoromethoxy, cyclopropyl, phenyl, fluorophenyl, phenyl-C.sub.1-C.sub.3-alkyl, pyridinyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9 and/or --NH--S(.dbd.O).sub.2--R.sup.9, or represents tetrazolyl, or represents isoxazolyl, pyrazolyl, thienyl, thiazolyl, imidazolyl, triazolyl, pyrrolyl, oxadiazolyl, pyridinyl or pyrimidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, hydroxy, amino, cyano, nitro, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, dimethylamino, trifluoromethyl, difluoroethyl, trifluoroethyl, trifluoromethoxy, cyclopropyl, pyridinyl, phenyl, fluorophenyl, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, --S(.dbd.O).sub.2--NR.sup.6R.sup.7, --S(.dbd.O)--R.sup.9, --S(.dbd.O).sub.2--R.sup.9, and/or --NH--S(.dbd.O).sub.2--R.sup.9, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, amino, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, C.sub.1-C.sub.2-alkoxy-C.sub.1-C.sub.2-alkyl, dimethylamino, --C(.dbd.O)NR.sup.6R.sup.7, --C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, trifluoromethyl, difluoroethyl, trifluoroethyl, trifluoromethoxy, hydroxy-C.sub.1-C.sub.3-alkyl, cyclopropyl, chlorothienyl, morpholino and/or pyridinyl, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen or bromine, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, methyl, ethyl, methoxy, ethoxy, cyclopropylamino, methylamino or ethylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, amino, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represent difluoromethoxy or trifluoromethoxy, or represent C.sub.1-C.sub.3-alkoxy which may be substituted by pyridinyl, morpholinyl, pyrrolidinyl or piperazinyl, in which pyridinyl and piperazinyl in turn may be optionally be substituted by C.sub.1-C.sub.3-alkyl, or represents cyclopropyl, or represents pyridinyl, pyrazolyl, triazolyl or isoxazolyl, which may be optionally mono- or polysubstituted by identical or different substituents from the group consting of hydroxy and/or methyl, or represents pyrrolidinyl, morpholinyl, piperidinyl, piperazinyl, oxazolidinyl, thiomorpholinyl, which may optionally be mono- or polysubstituted by oxo, methyl and/or --S(.dbd.O).sub.2R.sup.9, or represents phenyl optionally substituted by C.sub.1-C.sub.3-alkylaminosulphonyl or fluorine, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof, with the proviso that, if A represents a phenyl ring and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, amino, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represent difluoromethoxy or trifluoromethoxy, or represent C.sub.1-C.sub.3-alkoxy which may be substituted by pyridinyl, morpholinyl, pyrrolidinyl or piperazinyl, in which pyridinyl and piperazinyl in turn may be optionally substituted by C.sub.1-C.sub.3-alkyl, R.sup.1a does not represent hydrogen or chlorine, and where the proviso does not encompass those compounds of the formula (I) in which A represents phenyl and R.sup.4 represents hydrogen or chlorine and R.sup.5 represents trifluoromethoxy, and R.sup.1a represents chlorine, and also not those compounds of the formula (I) in which A represents phenyl and R.sup.4 represents hydrogen and R.sup.5 represents C.sub.1-C.sub.3-alkoxy which is substituted by morpholinyl, pyrrolidinyl, piperazinyl or pyridyl, in which the piperazinyl and pyridinyl itself may be substituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a represents chlorine. 8. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl or 3-pyridyl ring, and R.sup.1a represents hydrogen or chlorine, or represents piperazinyl, pyrrolidinyl, piperidinyl, diazepanyl, oxazinanyl, oxazolidinyl, morpholinyl, thiomorpholinyl, thiazolidinyl or azetidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, hydroxy, oxo, C.sub.1-C.sub.3-alkyl, methoxy, hydroxy-C.sub.1-C.sub.3-alkyl, dimethylamino, difluoroethyl, trifluoroethyl, benzyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, and/or --S(.dbd.O).sub.2--R.sup.9, or represents tetrazolyl, or represents isoxazolyl, pyrazolyl, thienyl, thiazolyl, imidazolyl, triazolyl, pyrrolyl, oxadiazolyl, pyridinyl or pyrimidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, hydroxy, cyano, C.sub.1-C.sub.2-alkyl, methoxy, methoxymethyl, trifluoromethyl, cyclopropyl, pyridinyl, phenyl, fluorophenyl and/or --C(.dbd.O)--R.sup.8, or represents a phenyl radical which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, methoxy, --C(.dbd.O)NR.sup.6R.sup.7, --C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, trifluoromethyl, trifluoromethoxy, hydroxy-C.sub.1-C.sub.3-alkyl, cyclopropyl, chlorotheinyl and/or morpholino, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen or bromine, and R.sup.2 represents methyl, ethyl or isopropyl, and R.sup.3 represents cyclopropyl, methyl, ethyl, methoxy, ethoxy, cyclopropylamino, methylamino or ethylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, amino, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represent difluoromethoxy or trifluoromethoxy, or represent C.sub.1-C.sub.3-alkoxy which may be substituted by pyridinyl, morpholinyl, pyrrolidinyl or piperazinyl, in which the pyridinyl and piperazinyl may in turn optionally be substituted by C.sub.1-C.sub.3-alkyl, or represent cyclopropyl, or represent pyridinyl, pyrazolyl, triazolyl or isoxazolyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of hydroxy and/or methyl, or represent pyrrolidinyl, morpholinyl, piperidinyl, piperazinyl, oxazolidinyl, thiomorpholinyl, which may optionally be mono- or polysubstituted by methyl, oxo, and/or --S(.dbd.O).sub.2R.sup.9, or represent phenyl optionally substituted by C.sub.1-C.sub.3-alkylaminosulphonyl or fluorine, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl, di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl or fluoropyridyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or an enantiomer, diastereomer, racemate, tautomer, or physiologically acceptable salt thereof, with the proviso that, if A represents a phenyl ring and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, amino, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represent difluoromethoxy or trifluoromethoxy, or represent C.sub.1-C.sub.3-alkoxy which may be substituted by pyridinyl, morpholinyl, pyrrolidinyl or piperazinyl, in which the pyridinyl and piperazinyl may in turn optionally be substituted by C.sub.1-C.sub.3-alkyl, R.sup.1a does not represent hydrogen or chlorine, and where the proviso does not encompass those compounds of the formula (I) in which A represents phenyl and R.sup.4 represents hydrogen or chlorine and R.sup.5 represents trifluoromethoxy, and R.sup.1a represents chlorine, and also not those compounds of the formula (I) in which A represents phenyl and R.sup.4 represents hydrogen and R.sup.5 represents C.sub.1-C.sub.3-alkoxy which is substituted by morpholinyl, pyrrolidinyl, piperazinyl or pyridyl, in which the piperazinyl and pyridinyl itself may be substituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a represents chlorine. 9. Compounds of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl ring, and R.sup.1a represents piperazinyl, pyrrolidinyl, piperidinyl, diazepanyl, oxazinanyl, oxazolidinyl, morpholinyl, thiomorpholinyl, thiazolidinyl or azetidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, hydroxy, oxo, C.sub.1-C.sub.3-alkyl, methoxy, hydroxy-C.sub.1-C.sub.3-alkyl, dimethylamino, difluoroethyl, trifluoroethyl, benzyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, and/or --S(.dbd.O).sub.2--R.sup.9, or represents tetrazolyl, or represents isoxazolyl, pyrazolyl, thienyl, thiazolyl, imidazolyl, triazolyl, pyrrolyl, oxadiazolyl, pyridinyl or pyrimidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, hydroxy, cyano, C.sub.1-C.sub.2-alkyl, methoxy, methoxymethyl, trifluoromethyl, cyclopropyl, pyridinyl, phenyl, fluorophenyl and/or --C(.dbd.O)--R.sup.8, or represents a phenyl radical, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, chlorine, hydroxy, cyano, nitro, carboxyl, C.sub.1-C.sub.3-alkyl, methoxy, --C(.dbd.O)NR.sup.6R.sup.7, C(.dbd.O)R.sup.8, C.sub.1-C.sub.3-alkylsulphinyl, C.sub.1-C.sub.3-alkylsulphonyl, --S(.dbd.O).sub.2NH.sub.2, C.sub.1-C.sub.3-alkylsulphonylamino, C.sub.1-C.sub.3-alkylaminosulphonyl, C.sub.3-C.sub.6-cycloalkylaminosulphonyl, trifluoromethyl, trifluoromethoxy, hydroxy-C.sub.1-C.sub.3-alkyl, cyclopropyl, chlorothienyl and/or morpholino, R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen, and R.sup.2 represents methyl or ethyl, and R.sup.3 represents methylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or difluoromethoxy or trifluoromethoxy, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl or di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or a tautomer or physiologically acceptable salt thereof, and where the stereocentre, which is represented by the carbon atom of the benzodiazepine skeleton which is bound to R.sup.2, is present either in racemic form or predominantly or completely in the (S) configuration. 10. A compound of formula (I) according to claim 1 in which X represents an oxygen atom, and A represents a phenyl ring, and R.sup.1a represents hydrogen or chlorine, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen, and R.sup.2 represents methyl or ethyl, and R.sup.3 represents methylamino, and R.sup.4 represents cyclopropyl, or represents pyridinyl, pyrazolyl, triazolyl or isoxazolyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of hydroxy and/or methyl, or represents pyrrolidinyl, morpholinyl, piperidinyl, piperazinyl, oxazolidinyl or thiomorpholinyl, which may optionally be mono- or polysubstituted by methyl, oxo and/or --S(.dbd.O).sub.2R.sup.9, or represents phenyl which is optionally substituted by C.sub.1-C.sub.3-alkylaminosulphonyl or fluorine, and R.sup.5 represents hydrogen, hydroxy, cyano, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represents difluoromethoxy or trifluoromethoxy, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl or di-C.sub.1-C.sub.3-alkyl-amino-C.sub.1-C.sub.3-alkyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or a tautomer or physiologically acceptable salt thereof, and where the stereocentre, which is represented by the carbon atom of the benzodiazepine skeleton which is bound to R.sup.2, is present either in racemic form or predominantly or completely in the (S) configuration. 11. A compound of formula (I), according to claim 1, in which X represents an oxygen atom, and A represents a phenyl ring, and R.sup.1a represents hydrogen or chlorine, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen, and R.sup.2 represents methyl or ethyl, and R.sup.3 represents methylamino, and R.sup.4 represents hydrogen, chlorine, methoxy or ethoxy, or represents difluoromethoxy or trifluoromethoxy, and R.sup.5 represents cyclopropyl, or represents pyridinyl or pyrazolyl, which may optionally be substituted one or more times by methyl, or represents morpholinyl, piperidinyl, piperazinyl or thiomorpholinyl, which may optionally be mono- or polysubstituted by methyl, oxo and/or --S(.dbd.O).sub.2R.sup.9, or represents phenyl which is substituted by C.sub.1-C.sub.3-alkylaminosulphonyl, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl or di-C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, and R.sup.8 represents hydroxy, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or a tautomer or physiologically acceptable salt thereof, and where the stereocentre, which is represented by the carbon atom of the benzodiazepine skeleton which is bound to R.sup.2, is present either in racemic form or predominantly or completely in the (S) configuration. 12. A compound of formula (I), according to claim 1, in which X represents an oxygen atom, and A represents a phenyl ring, and R.sup.1a represents piperazinyl, pyrrolidinyl, piperidinyl, diazepanyl, oxazinanyl, oxazolidinyl, morpholinyl, thiomorpholinyl, thiazolidinyl or azetidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of fluorine, hydroxy, oxo, C.sub.1-C.sub.3-alkyl, methoxy, hydroxy-C.sub.1-C.sub.3-alkyl, dimethylamino, difluoroethyl, trifluoroethyl, benzyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, --C(.dbd.O)--R.sup.8, and/or --S(.dbd.O).sub.2--R.sup.9, or represents isoxazolyl or pyrazolyl, which may optionally be substituted one or more times by identical or different C.sub.1-C.sub.2-alkyls, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen, and R.sup.2 represents methyl, and R.sup.3 represents methylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, hydroxy, cyano, chlorine, C.sub.1-C.sub.6-alkyl, methoxy, ethoxy or C.sub.1-C.sub.3-alkylcarbonylamino, or represent difluoromethoxy or trifluoromethoxy, and R.sup.6 and R.sup.7 independently of one another represent hydrogen, C.sub.1-C.sub.3-alkyl, cyclopropyl or di-C.sub.1-C.sub.3-alkylamino-C.sub.1-C.sub.3-alkyl, and R.sup.8 represents hydroxyl, C.sub.1-C.sub.3-alkyl, hydroxy-C.sub.1-C.sub.3-alkyl, trifluoromethyl, pyrrolidinyl, morpholinyl or piperidinyl, and R.sup.9 represents C.sub.1-C.sub.4-alkyl or C.sub.1-C.sub.4-alkoxy, or a tautomer or physiologically acceptable salt thereof, and where the stereocentre, which is represented by the carbon atom of the benzodiazepine skeleton which is bound to R.sup.2, is present either in racemic form or predominantly or completely in the (S) configuration. 13. A compound of formula (I), according to claim 1 in which X represents an oxygen atom, and A represents a phenyl ring, and R.sup.1a represents piperazinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl or azetidinyl, which may optionally be mono- or polysubstituted by identical or different substituents from the group consisting of hydoxy, oxo, C.sub.1-C.sub.3-alkyl, methoxy, dimethylamino, difluoroethyl, trifluoroethyl, --NR.sup.6C(.dbd.O)--R.sup.9, --C(.dbd.O)--NR.sup.6R.sup.7, and/or --C(.dbd.O)--R.sup.8, and R.sup.1b represents hydrogen, fluorine, bromine or cyano, and R.sup.1c represents hydrogen, and R.sup.2 represents methyl, and R.sup.3 represents methylamino, and R.sup.4 and R.sup.5 independently of one another represent hydrogen, chlorine, methoxy or ethoxy, or represent difluoromethoxy or trifluoromethoxy, and R.sup.6 and R.sup.7 independently of one another represent hydrogen or C.sub.1-C.sub.3-alkyl, and R.sup.8 represents methyl, and R.sup.9 represents methyl, or a tautomer or physiologically acceptable salt thereof, and where the stereocentre, which is represented by the carbon atom of the benzodiazepine skeleton which is bound to R.sup.2, is present either in racemic form or predominantly or completely in the (S) configuration. 14. A compound of formula (I) according to claim 1 in which A represents a phenyl ring and R.sup.4 represents hydrogen or chlorine and R.sup.5 represents trifluoromethoxy and R.sup.1a represents chlorine, and compounds of the formula (I) in which A represents a phenyl ring and R.sup.4 represents hydrogen and R.sup.5 represents C.sub.1-C.sub.3-alkoxy which may be substituted by morpholinyl, pyrrolidinyl, piperazinyl or pyridyl, where the piperazinyl or pyridinyl for its part may be substituted by C.sub.1-C.sub.3-alkyl, and R.sup.1a represents chlorine, or a tautomer or physiologically acceptable salt thereof. 15. A compound of formula (I) according to claim 1, selected from the group consisting of (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-(trifluoromethoxy)-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (4S)-1-(4-chlorophenyl)-N,4-dimethy-8-(trimethxy)-4,5-dimethyl-8-trifluor- omethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-(4-chlorophenyl)-N,4-dimethyl-8-(trifluoromethoxy)-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1H-pyrazol-3-yl)phenyl]-4,5-dihyd- ro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(2-chloropyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-5-(4-{7,8-dimethoxy-4-methyl-3-[(methylamino)carbonyl]-4,5-dihydro- -3H-2,3-benzodiazepin-1-yl}phenyl)thiophen-2-carboxylic acid, (.+-.)-4'-{7,8-dimethoxy-4-methyl-3-[(methylamino)carbonyl]-4,5-dihydro-3- H-2,3-benzodiazepin-1-yl}biphenyl-2-carboxylic acid, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-(pyridin-4-yl)-4,5-dihydro-3H-2,- 3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-8-cyclopropyl-N,4-dimethyl-4,5-dihydro-3H-2,3-b- enzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-{4-[(methylamino)sulphonyl]pheny- l}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-(morpholin-4-yl)-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (4S)-1-(4-chlorophenyl)-N,4-dimethyl-8-(morpholin-4-yl)-4,5-dihydro-3H-2,- 3-benzodiazepine-3-carboxamide, (4R)-1-(4-chlorophenyl)-N,4-dimethyl-8-(morpholin-4-yl)-4,5-dihydro-3H-2,- 3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-(4-methylpiperazin-1-yl)-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-(piperidin-1-yl)-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (.+-.)-8-methoxy-N,4-dimethyl-1-(pyridin-3-yl)-4,5-dihydro-3H-2,3-benzodi- azepine-3-carboxamide, (.+-.)-7-chloro-1-(4-chlorophenyl)-N,4-dimethyl-8-(trifluoromethoxy)-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, 7-chloro-1-(4-chlorophenyl)-N,4-dimethyl-8-(trifluoromethoxy)-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl]-8-methoxy-N,4-dimethyl-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihydro-3H-2- ,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(4-isoxazolyl)phenyl]-8-methoxy-N,4-dimethyl-4,5-dihydro-3H-2,3- -benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(1-methyl-1H-pyrazol-5-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-8-methoxy-N,4-dimethyl-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(1-methyl-H-pyrazol-4-yl)phenyl]-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(1,3,5-trimethyl-H-pyrazol-4-yl)phenyl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(1H-pyrazol-5-yl)phenyl]-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3-cyclopropyl-5-ethyl-1H-pyrazol-1-yl)phenyl]-8-methoxy-N,4-di- methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(5-cyclopropyl-3-ethyl-1H-pyrazol-1-yl)phenyl]-8-methoxy-N,4-di- methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-1-{4-[3-(methoxymethyl)-5-methyl-1H-pyrazol-1-yl]phenyl}-N- ,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-1-{4-[5-(methoxymethyl)-3-methyl-1H-pyrazol-1-yl]phenyl}-N- ,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[5-cyclopropyl-3-(pyridin-2-yl)-1H-pyrazol-1-yl]phenyl}-8-metho- xy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[3-cyclopropyl-5-(pyridin-2-yl)-1H-pyrazol-1-yl]phenyl}-8-metho- xy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(1H-tetrazol-1-yl)phenyl]-4,5-dihydro-3H- -2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3-(3,5-dimethylisoxazol-4-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[2-(morpholin-4-yl)ethoxy]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[2-(pyrrolidin-1-yl)ethoxy]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxooxazolidin-3-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxooxazolidin-3-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-benzyl-2-oxopiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-2-oxo-1,4-diazepan-1-yl)- phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxo-1,3-oxazinan-3-yl)phenyl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxopyrrolidin-1-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(3-oxomorpholin-4-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(3-oxomorpholin-4-yl)phenyl]-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-methyl-5-oxomorpholin-4-yl)phen- yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide (stereoisomer mixture), (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-methyl-3-oxomorpholin- -4-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide (stereoisomer mixture), (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-2-oxopiperazin-1-yl)phen- yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-2-oxopiperazin-1-yl)phenyl- ]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-2-oxopiperazin-1-yl)phenyl- ]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-oxopiperazin-1-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1-methyl-1H-1,2,3-triazol-4-yl)ph- enyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1-methyl-H-1,2,3-triazol-4-yl)pheny- l]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(2,4-dimethylthiazol-5-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(2,4-dimethylthiazol-5-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(2,4-dimethylthiazol-5-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(1,2-dimethyl-H-imidazol-5-yl)phenyl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[2-(trifluoromethyl)pyridin-3-yl]p- henyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(6-hydroxypyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(6-hydroxypyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[6-(trifluoromethyl)pyridin-3-yl]p- henyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1,3,5-trimethyl-H-pyrazol-4-yl)ph- enyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1,3,5-trimethyl-1H-pyrazol-4-yl)phe- nyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1,3,5-trimethyl-1H-pyrazol-4-yl)phe- nyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(isoxazol-4-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3-(1,3,5-trimethyl-H-pyrazol-4-yl)ph- enyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3-(1-methyl-H-pyrazol-4-yl)phenyl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3-(1-methyl-1H-pyrazol-5-yl)phenyl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-fluoro-3-(1,3,5-trimethyl-1H-pyrazol-4-yl)phenyl]-7,8-dimetho- xy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-fluoro-3-(1-methyl-1H-pyrazol-4-yl)phenyl]-7,8-dimethoxy-N,4-- dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3-(3,5-dimethylisoxazol-4-yl)-4-fluorophenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-(3'-nitrobiphenyl-4-yl)-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(biphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-be- nzodiazepine-3-carboxamide, (.+-.)-1-(2',4'-dichlorobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4'-fluorobiphenyl-4-yl)-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4'-Chlorbiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-(4'-methylbiphenyl-4-yl)-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-(4'-methoxybiphenyl-4-yl)-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(6-methoxypyridin-3-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(methylsulphinyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{2'-[(methylsulphonyl)amino]biphenyl-- 4-yl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[2'-(methylsulphonyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4'-[(methylsulphonyl)amino]biphenyl-- 4-yl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{3'-[(methylsulphonyl)amino]biphenyl-- 4-yl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-(2'-methylbiphenyl-4-yl)-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(methylsulphonyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(2-methoxypyrimidin-5-yl)phenyl]-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-cyano-4'-fluorobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(2-methoxypyridin-3-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-carbamoylbiphenyl-4-yl)-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(pyrrolidin-1-ylcarbonyl)biphenyl- -4-yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(morpholin-4-ylcarbonyl)biphenyl-- 4-yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(5-methoxypyridin-3-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(5-methylpyridin-3-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpyridin-3-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4'-(cyclopropylcarbamoyl)biphenyl-4-yl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3-fluoropyridin-4-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(trifluoromethyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(trifluoromethyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-(3'-methoxybiphenyl-4-yl)-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4'-(5-chlorothien-2-yl)biphenyl-4-yl]-7,8-dimethoxy-N,4-dimethy- l-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-fluorobiphenyl-4-yl)-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-(2'-methoxybiphenyl-4-yl)-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[2'-(trifluoromethyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(2'-chlorobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(2'-fluorobiphenyl-4-yl)-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4'-(hydroxymethyl)biphenyl-4-yl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(trifluoromethoxy)biphenyl-4-yl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(pyrrolidin-1-ylcarbonyl)biphenyl- -4-yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(piperidin-1-ylcarbonyl)biphenyl-- 4-yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(morpholin-4-ylcarbonyl)biphenyl-- 4-yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3'-(cyclopropylcarbamoyl)biphenyl-4-yl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(2',4'-difluorobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1-methyl-1H-pyrazol-5-yl)phenyl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-(4'-nitrobiphenyl-4-yl)-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(pyridin-3-yl)phenyl]-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(4-methoxypyridin-3-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-cyanobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4'-cyanobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[2'-(trifluoromethoxy)biphenyl-4-yl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(methylsulphonyl)biphenyl-4-yl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(2'-cyanobiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(morpholin-4-yl)biphenyl-4-yl]-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(pyrimidin-5-yl)phenyl]-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[2'-(hydroxymethyl)biphenyl-4-yl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-{[2-(dimethylamino)ethyl]carb-amoyl}biphenyl-4-yl)-7,8-dimet- hoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-(3'-sulphamoylbiphenyl-4-yl)-4,5-dihy- dro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4'-(methylsulphamoyl)biphenyl-4-yl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1-methyl-1H-pyrrol-2-yl)phenyl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(6-methylpyridin-3-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4'-(cyclopropylsulphamoyl)biphenyl-4-yl]-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-fluoro-5'-hydroxybiphenyl-4-yl)-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(3'-fluoro-5'-methylbiphenyl-4-yl)-7,8-dimethoxy-N,4-dimethy-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3'-(methylsulphamoyl)biphenyl-4-yl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(5-fluoropyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-fluoropyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(2-methylpyridin-3-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(2-methoxypyridin-4-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(5-cyanopyridin-3-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7,8-dimethoxy-N,4-dimethyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(azetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(azetidin-1-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(azetidin-1-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3-fluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(3-fluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3-fluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-hydroxypiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(4-hydroxypiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(piperazin-1-yl)phenyl]-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(piperazin-1-yl)phenyl]-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-acetylpiperazin-1-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(4-acetylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(4-acetylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(trifluoracetyl)piperazin-1-yl]- phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]phenyl}-7,8-di- methoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(methylsulphonyl)piperazin-1-yl- ]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(1,1-dioxidothiomorpholin-4-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(3-oxopiperazin-1-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-3-oxopiperazin-1-yl)phen- yl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(piperidin-1-yl)phenyl]-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3-(morpholin-4-yl)phenyl]-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3-(3,3-difluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3-(azetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro- -3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[3-(4-methylpiperazin-1-yl)phenyl]-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-fluoro-3-(morpholin-4-yl)phenyl]-7,8-dimethoxy-N,4-dimethy-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[3-(3,3-difluoroazetidin-1-yl)-4-fluorophenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-fluoro-3-(4-hydroxypiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(5-methyl-3-phenyl-1H-pyrazol-1-yl- )phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(5-methyl-3-phenyl-1H-pyrazol-1-yl)p- henyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(5-cyclopropyl-3-phenyl-1H-pyrazol-1-yl)phenyl]-7,8-dimethoxy- -N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(5-cyclopropyl-3-phenyl-1H-pyrazol-1-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[3-phenyl-5-(trifluoromethyl)-1H-p- yrazol-1-yl]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[3-(4-fluorophenyl)-1H-pyrazol-1-yl]phenyl}-7,8-dimethoxy-N,4- -dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[3-(4-fluorophenyl)-1H-pyrazol-1-yl]phenyl}-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-{4-[3-(4-fluorophenyl)-1H-pyrazol-1-yl]phenyl}-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[5-methyl-3-(trifluoromethyl)-1H-p- yrazol-1-yl]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(1H-1,2,4-triazol-1-yl)phenyl]-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(5-methyl-1H-1,2,4-triazol-1-yl)ph- enyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)phenyl]-7,8-dimethoxy-N,4- -dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-tert-butyl-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(t- rifluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(tri- fluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(tri- fluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-7-methoxy-N,4-dim- ethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-7-methoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-8-chloro-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-7-methoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4,8-trimethyl-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-bis(difluoromethoxy)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N- ,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-7,8-diethoxy-N,4-dimethyl-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7-(difluoromethoxy)-1-[4-(3,5-dimethyl-4,5-dihydro-3H-2,3-benzodia- zepine-3-carboxamide, (4S)-7-(difluoromethoxy)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-8-methox- y-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7-(difluoromethoxy)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-8-methox- y-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7-(difluoromethoxy)-8-methoxy-N,4-dimethyl-1-[4-(4-methylpiperazin- -1-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7-(difluoromethoxy)-8-methoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1- -yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7-(difluoromethoxy)-8-methoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1- -yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[3-(4-methylpiperazin-1-yl)propo- xy]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-(4-chlorophenyl)-N,4-dimethyl-8-[3-(4-methylpiperazin-1-yl)propoxy- ]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[3-(morpholin-4-yl)propoxy]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[2-(4-methylpiperazin-1-yl)ethox- y]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-8-[(6-methylpyridin-2-yl)methoxy]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-8-hydroxy-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-[3-(morphol- in-4-yl)propoxy]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7-cyano-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-8-methoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-acetamido-N,4-dimethyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihydro-- 3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-acetamido-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-acetamido-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-8-(3,5-dimethyl-1H-pyrazol-1-yl)-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-8-(3,5-dimethyl-1H-pyrazol- -1-yl)-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(morpholin-- 4-yl)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(morphin-4-yl- )-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3,5-dimethylisoxazol-4-yl)phenyl]-N,4-dimethyl-8-(morpholin-4-- yl)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-8-methoxy-N,4-dimethyl-1-[4-(3-oxomorphin-4-yl)phenyl]-4,5-dihydro-3- H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl}-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(4-methoxypiperidin-1-yl)phenyl]-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7,8-dimethoxy-1-[4-(4-methoxypiperidin-1-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-1-[4-(4-methoxypiperidin-1-yl)phenyl]-N,4-dimethyl-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(dimethylamino)piperidin-1-yl]phenyl}-7,8-dimethoxy-N,4-di- methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-{4-[4-(dimethylamino)piperidin-1-yl]phenyl}-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[4-(dimethylamino)piperidin-1-yl]phenyl}-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,3-difluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-acetamidopiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(2-hydroxyethyl)piperidin-1-yl]phenyl}-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3-hydroxyazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3-hydroxy-3-methylazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-di- methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(3-hydroxy-3-methylazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(3-hydroxy-3-methylazetidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-isopropylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimethyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-1-[4-(3-methoxyazetidin-1-yl)phenyl]-N,4-dimethyl-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-hydroxy-4-methylpiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(4-hydroxy-4-methylpiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dim- ethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[4-(4-hydroxy-4-methylpiperidin-1-yl)phenyl]-7,8-dimethoxy-N,4-dim- ethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(methylcarbamoyl)piperidin-1-yl- ]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(methylcarbamoyl)piperidin-1-yl]p- henyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(methylcarbamoyl)piperidin-1-yl]p- henyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[(3S)-3-hydroxypyrrolidin-1-yl]phenyl}-7,8-dimethoxy-N,4-dime- thyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[(3S)-3-hydroxypyrrolidin-1-yl]phenyl}-7,8-dimethoxy-N,4-dimeth- yl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-tert-butyl (1-{4-[7,8-dimethoxy-4-methyl-3-(methylcarbamoyl)-4,5-dihydro-3H-2,3-benz- odiazepin-1-yl]phenyl}-4-methylpiperidin-4-yl)carbamate, (.+-.)-1-{4-[(2S,5R)-2,5-dimethylpiperazin-1-yl]phenyl}-7,8-dimethoxy-N,4- -dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(2,2-difluoroethyl)piperazin-1-yl]phenyl}-7,8-dimethoxy-N,- 4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(3-oxopiperazin-1-yl)phenyl]-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[(2R,6S)-2,6-dimethylmorpholin-4-yl]phenyl}-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-oxopiperidin-1-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-{4-[4-(2,2,2-trifluoroethyl)piperazin- -1-yl]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-{4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]phenyl}-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dihydroxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,- 5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-diethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl- ]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(piperazin-1-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-4-ethyl-7, 8-dimethoxy-N-methyl-1-[4-(piperazin-1-yl)phenyl]-4,5-dihydro-3H-2,3-benz- odiazepine-3-carboxamide, (4R)-4-ethyl-7, 8-dimethoxy-N-methyl-1-[4-(piperazin-1-yl)phenyl]-4,5-dihydro-3H-2,3-benz- odiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-{4-[4-(methylsulphonyl)piperazin-- 1-yl]phenyl}-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-4-ethyl-7, 8-dimethoxy-N-methyl-1-{4-[4-(methylsulphonyl)piperazin-1-yl]phenyl}-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-4-ethyl-7, 8-dimethoxy-N-methyl-1-{4-[4-(methylsulphonyl)piperazin-1-yl]phenyl}-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-1-[4-(3-fluoroazetidin-1-yl)phenyl]-7,8-dimethoxy-N-methyl- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-acetylpiperazin-1-yl)phenyl]-4-ethyl-7, 8-dimethoxy-N-methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(1,1-dioxidothiomorpholin-4-yl)phenyl]-4-ethyl-7,8-dimethoxy-- N-methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-1-[4-(4-hydroxypiperidin-1-yl)phenyl]-7, 8-dimethoxy-N-methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(morpholin-4-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(morpholin-4-yl)phenyl]-4,5-dihy- dro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-1-[4-(1,1-dioxidothiomorpholin-4-yl)phenyl]-N,4-dimethyl-- 7-(trifluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-N,4-dimethyl-1-[4-(piperazin-1-yl)phenyl]-7-(trifluoromet- hoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-1-[4-(4-hydroxypiperidin-1-yl)phenyl]-N,4-dimethyl-7-(tri- fluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-7-(trif- luoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-chloro-N,4-dimethyl-1-{4-[4-(methylsulphonyl)piperazin-1-yl]phen- yl}-7-(trifluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-(1,1-dioxidothiomorpholin-4-yl)-1-[4-(1,1-dioxidothiomorpholin-4- -yl)phenyl]-N,4-dimethyl-7-(trifluoromethoxy)-4,5-dihydro-3H-2,3-benzodiaz- epine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-8-(1,1-dioxidothiomorpholin-4-yl)-N,4-dimethyl-- 7-(trifluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-acetylpiperazin-1-yl)phenyl]-N,4-dimethyl-7-(trifluorometh- oxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl}-N,4-dimethyl-7-(tri- fluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-8-methoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-7-(tri- fluoromethoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(1,3,5-trimethyl-1H-pyrazol-4-- yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-1-(4'-fluorobiphenyl-4-yl)-7,8-dimethoxy-N-methyl-4,5-dihy- dro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(1-methyl-1H-1,2,3-triazol-4-y- l)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-4-ethyl-7, 8-dimethoxy-N-methyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-isopropyl-7,8-dimethoxy-N-methyl-1-[4-(1,3,5-trimethyl-1H-pyrazo- l-4-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(2-oxopyrrolidin-1-yl)phenyl]-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(3-oxomorpholin-4-yl)phenyl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(2-oxopiperidin-1-yl)phenyl]-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-4-ethyl-7,8-dimethoxy-N-methyl-1-[4-(2-oxo-1,3-oxazolidin-3-yl)phe- nyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methyl-2-oxo-1,4-diazepan-1-yl)ph- enyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(2-oxo-1,3-oxazolidin-3-yl)-4,5-- dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-(4-chlorophenyl)-N,4-dimethyl-7-(2-oxo-1,3-oxazolidin-3-yl)-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(2-oxopiperidin-1-yl)-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(3-oxomorpholin-4-yl)-4,5-dihydr- o-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(morpholin-4-yl)-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(pyrrolidin-1-yl)-4,5-dihydro-3H- -2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-7-(1,1-dioxidothiomorpholin-4-yl)-N,4-dimethyl-- 4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(4-methylpiperazin-1-yl)-4,5-dih- ydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-N,4-dimethyl-7-(4-methylpiperazin-1-yl)-1-[4-(4-methylpiperazin-1-- yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-N,4-dimethyl-7-(4-methyl-3-oxopiperazin-1-yl)-1-[4-(4-methyl-3-oxo- piperazin-1-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-7-(4-fluorophenyl)-N,4-dimethyl-4,5-dihydro-3H-- 2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(pyridin-4-yl)-4,5-dihydro-3H-2,- 3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-7-(6-hydroxypyridin-3-yl)-N,4-dimethyl-4,5-dihy- dro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N,4-dimethyl-4- ,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-(4-chlorophenyl)-N,4-dimethyl-7-(1-methyl-1H-1,2,3-triazol-4-yl)- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-1-[4-(4-hydroxypiperidin-1-yl)phenyl]-7, 8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)-7, 8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5- -dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(1,1-dioxido-1,2-thiazolidin-2-yl)phenyl]-7,8-dimethoxy-N,4-d- imethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-{7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5- -dihydro-3H-2,3-benzodiazepin-3-yl}ethanone, 1-{(4S)-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-d- ihydro-3H-2,3-benzodiazepin-3-yl}ethanone, (.+-.)-1-{1-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-7,8-dimethoxy-4-meth- yl-4,5-dihydro-3H-2,3-benzodiazepin-3-yl}ethanone, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(5-methyl-1,3,4-oxadiazol-2-yl)phe- nyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(3-methyl-1,2,4-oxadiazol-5-yl)phe- nyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-N,4-dimethyl-8-(trifluoromethoxy)-1-[4-(1,3,5-trimethyl-1H-pyrazol- -4-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)--N,4-dimethyl-8-(trifluoromethoxy)-1-[4-(1,3,5-trimethyl-1H-pyrazol-- 4-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)--N,4-dimethyl-8-(trifluoromethoxy)-1-[4-(1,3,5-trimethyl-1H-pyrazol-- 4-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-N,4-dimethyl-1-[4-(4-methyl-1-piperazinyl)phenyl]-8-(trifluorometh- oxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4R)--N,4-dimethyl-1-[4-(4-methyl-1-piperazinyl)phenyl]-8-(trifluorometho- xy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)--N,4-dimethyl-1-[4-(4-methyl-1-piperazinyl)phenyl]-8-(trifluorometho- xy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[4-(4-hydroxy-1-piperidinyl)phenyl]-N,4-dimethyl-8-(trifluoromet- hoxy)-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-1-[2,4-dibromo-5-(4-methylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4- -dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[3-bromo-4-(4-methylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (4S)-1-[3-cyano-4-(4-methylpiperazin-1-yl)phenyl]-7,8-dimethoxy-N,4-dimet- hyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, (.+-.)-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-3-(1-o- xopropyl)-4,5-dihydro-3H-2,3-benzodiazepine, (.+-.)-3-(cyclopropylcarbonyl)-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiper- azin-1-yl)phenyl]-4,5-dihydro-3H-2,3-benzodiazepine, (.+-.)-N-cyclopropyl-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)- phenyl]-4,5-dihydro-3H-2,3-benzodiazepine, (.+-.)-7,8-dimethoxy-N,4-dimethyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,- 5-dihydro-3H-2,3-benzodiazepin-3-carbothioamide, methyl (.+-.)-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxylate, ethyl (.+-.)-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]-4,5-di- hydro-3H-2,3-benzodiazepine-3-carboxylate, (.+-.)-N-ethyl-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl- ]-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide, and (4S)--N-ethyl-7,8-dimethoxy-4-methyl-1-[4-(4-methylpiperazin-1-yl)phenyl]- -4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide. 16. A method for the control of male fertility comprising administering to a human or mammal in need thereof an effective amount of a compound according to claim 1, or an enantiomer, diastereomer, racemate, tautomer or physiologically acceptable salt thereof. 17. A method for the treatment of a leukaemia, prostate carcinoma, breast carcinoma, melanoma or multiple myeloma responsive to inhibition of BRD4 comprising administering to a human or mammal in need thereof an effective amount of a compound according to claim 1, or an enantiomer, diastereomer, racemate, tautomer or physiologically acceptable salt thereof. 18. A pharmaceutical formulation comprising a compound according to claim 1, or an enantiomer, diastereomer, racemate, tautomer or physiologically acceptable salt thereof, in combination with an antihyperproliferative, cytostatic or cytotoxic substance selected from abiraterone acetate, acolbifene, actinomycin D (dactinomycin), afatinib, aldesleukin, alendronic acid, alitretinoin, allopurinol, altretamine, aminoglutethimide, aminopterin, amifostine, amrubicin, amsacrine, anastrozole, apatinib, arglabin, arsenic trioxide, arzoxifene, asoprisnil, L-asparaginase, atamestane, atrasentan, axitinib, 5-azacytidine, azathioprine, bendamustine, bestatin, betamethasone acetate, betamethasone sodium phosphate, bexarotene, bicalutamide, bleomycin sulphate, broxuridine, bortezomib, bosutinib, busulfan, cabazitaxel, calcitonin, camptothecin, capecitabin, carboplatin, carfilzomib, carmustine, cediranib, celmoleukin, chlorambucil, cisplatin, cladribine, clodronic acid, clofarabine, colaspase, crisnatol, crizotinib, cyclophosphamide, cyproterone acetate, cytarabine, dacarbazine, dactinomycin, dasatinib, daunorubicin, decitabine, degarelix, denileukin diftitox, deslorelin, dexrazoxane, diethylstilbestrol, 2',2'-difluorodeoxycytidine, docetaxel, doxifluridine, doxorubicin, dronabinol, dutasteride, edotecarin, eflornithine, enzalutamide, epirubicin, epoetin-alfa, epothilone, eptaplatin, erlotinib, erythro-hydroxynonyladenine, estradiol, estramustine sodium phosphate, ethynylestradiol, etidronic acid, etoposide, everolimus, exatecan, exemestan, fadrozole, fenretinide, filgrastim, finasteride, floxuridine, fluconazole, fludarabine, 5-fluordeoxyuridine monophosphate, 5-fluorouracil (5-FU), fluoxymesterone, flutamide, formestane, fosteabine, fotemustin, fulvestrant, gefitinib, gemcitabine, gemtuzumab, goserelin, gossypol, granisetron-hydrochloride, hexamethylmelamine, histamine dihydrochloride, histrelin, hydroxyurea, hydroxyprogesterone caproate, ibandronic acid, ibritumomab tiuxetan, idarubicin, ifosfamide, imatinib, iniparib, irinotecan, ixabepilone, keyhole limpet haemocyanin, lanreotide, lapatinib, lasofoxifene, lentinan sulphate, lestaurtinib, letrozole, leucovorin, leuprolide, leuprolide acetate, levamisole, levofolinic acid calcium salt, liposomal MTP-PE, lomustine, lonafarnib, lonidamine, mechlorethamine, mecobalamin, medroxyprogesterone acetate, megestrol acetate, melphalan, 6-mercaptopurine, mesna, methotrexate, miltefosine, minocycline, minodronate, miproxifene, mitomycin C, mitotane, mitoxantrone, nafarelin, nedaplatin, nelarabine, nemorubicin, neratinib, nilotinib, nilutamide, nimustine, nolatrexed, obatoclax, oblimersen, octreotide, olaparib, ondansetron hydrochloride, oxaliplatin, paclitaxel, pamidronate disodium, pazopanib, pegaspargase, pemetrexed, pentostatin, N-phosphonoacetyl-L-aspartate, picibanil, pilocarpine hydrochloride, pirarubicin, plerixafor, plicamycin, porfimer sodium, prednimustine, prednisolone, prednisone, procarbazine, quazepam, raloxifene, raltitrexed, ranpirnase, refametinib, regorafenib, 13-cis-retinoic acid, rhenium-186 etidronate, rituximab, romidepsin, romurtide, ruxolitinib, salinomycin, sargramostim, satraplatin, semaxatinib, semustine, seocalcitol, sipuleucel-T, sizofiran, sobuzoxane, sorafenib, streptozocin, strontium-89 chloride, sunitinib, batabulin, tamoxifen, tamsulosin, tasonermin, testolactone, teceleukin, temozolomide, temsirolimus, teniposide, testosterone propionate, thalidomide, thymosin alpha 1, thioguanine, thiotepa, thyrotropin, tiazofurin, tiludronic acid, tipifarnib, tirapazamine, canfosfamide, toceranib, topotecan, toremifene, tositumomab, tastuzumab, treosulfan, tretinoin, trimethylmelamine, trimetrexate, triptorelin acetate, triptorelin pamoate, trofosfamide, uridine, valrubicin, valspodar, vandetanib, vapreotid, vatalanib, vemurafinib, verteporfin, vesnarinon, vinblastine, vincristine, vindesine, vinflunine, vinorelbine, vismodegib, zinostatin stimalamer, and zoledronic acid. 19. A pharmaceutical formulation comprising a compound according to claim 1, or an enantiomer, diastereomer, racemate, tautomer or physiologically acceptable salt thereof, and a pharmaceutically acceptable excipient. |
Details for Patent 9,890,147
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Recordati Rare Diseases, Inc. | ELSPAR | asparaginase | For Injection | 101063 | 01/10/1978 | ⤷ Try a Trial | 2032-08-16 |
Amgen, Inc. | EPOGEN/PROCRIT | epoetin alfa | Injection | 103234 | 06/01/1989 | ⤷ Try a Trial | 2032-08-16 |
Amgen, Inc. | EPOGEN/PROCRIT | epoetin alfa | Injection | 103234 | ⤷ Try a Trial | 2032-08-16 | |
Amgen, Inc. | PROCRIT | epoetin alfa | Injection | 103234 | ⤷ Try a Trial | 2032-08-16 | |
Clinigen, Inc. | PROLEUKIN | aldesleukin | For Injection | 103293 | 05/05/1992 | ⤷ Try a Trial | 2032-08-16 |
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