Claims for Patent: 8,530,493

Summary for Patent: 8,530,493

Title:	Indolopyridines as Eg5 kinesin modulators
Abstract:	Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
Inventor(s):	Vennemann; Matthias (Constance, DE), Bar; Thomas (Reichenau, DE), Braunger; Jurgen (Constance, DE), Zimmermann; Astrid (Constance, DE), Gekeler; Volker (Constance, DE)
Assignee:	4SC AG (Planegg-Martinsried, DE)
Application Number:	12/280,424
Patent Claims:	1. A compound of formula I ##STR00966## in which R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11, in which R11 is --N(R111)R112, or halogen, in which R111 is hydrogen, 1-4C-alkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, 1N-(1-4C-alkyl)-pyrazolyl, 1N-(H)-pyrazolyl, isoxazolyl, or completely or partially fluorine-substituted 1-4C-alkyl, R112 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, or 3-7C-cycloalkyl-1-4C-alkyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, S-oxo-thiomorpholin-4-yl, S,S-dioxo-thiomorpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, 2,5-dihydro-pyrrol-1-yl, 1,2,3,6-tetrahydropyridin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, triazol-1-yl, or tetrazol-1-yl, in which R113 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkylcarbonyl, amidino, or completely or partially fluorine-substituted 1-4C-alkyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and 1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy or hydroxyl, R3 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl or 1-4C-alkoxy, R4 is 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R5 is 1-4C-alkoxy, phenyl-1-4C-alkoxy, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, R6 is hydrogen, 1-4C-alkyl or halogen, or a salt, stereoisomer or salt of a stereoisomer thereof. 2. A compound of formula I according to claim 1, in which R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11, in which R11 is --N(R111)R112, or halogen, in which R111 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, or completely or partially fluorine-substituted 1-4C-alkyl, R112 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, or 3-7C-cycloalkyl-1-4C-alkyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, S-oxo-thiomorpholin-4-yl, S,S-dioxo-thiomorpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, triazol-1-yl, or tetrazol-1-yl, in which R113 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkylcarbonyl, amidino, or completely or partially fluorine-substituted 1-4C-alkyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and 1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy or hydroxyl, R3 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl or 1-4C-alkoxy, R4 is 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R5 is 1-4C-alkoxy, phenyl-1-4C-alkoxy, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, R6 is hydrogen, 1-4C-alkyl or halogen, or a salt, stereoisomer or salt of a stereoisomer thereof. 3. A compound of formula I according to claim 1, in which R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11, in which R11 is --N(R111)R112, in which R111 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R112 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, S-oxo-thiomorpholin-4-yl, S,S-dioxo-thiomorpholin-4-yl, pyrrolidin-1-yl, 4N-(R113)-piperazin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl or triazol-1-yl, in which R113 is 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy or hydroxyl, R3 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl or 1-4C-alkoxy, R4 is 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R5 is 1-4C-alkoxy, phenyl-1-4C-alkoxy, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, R6 is hydrogen, 1-4C-alkyl or halogen, or a salt, stereoisomer or salt of a stereoisomer thereof. 4. A compound according to claim 1, wherein said compounds have with respect to the positions 3a and 10 the configuration shown in formula I* ##STR00967## or a salt thereof. 5. A compound of formula I according to claim 1, in which R1 is methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclopropylmethyl, ethyl substituted by R11, propyl substituted by R11, or butyl substituted by R11, in which R11 is --N(R111)R112, fluorine, chlorine, or bromine, in which either R111 is hydrogen, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is methyl, or R111 is ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is ethyl, isopropyl, or cyclopropyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, triazol-1-yl, or tetrazol-1-yl, in which R113 is hydrogen, methyl, ethyl, propyl, isopropyl, acetyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and methyl, R2 is hydrogen, R3 is hydrogen, R4 is methyl, ethyl, propyl, isopropyl, cyclopropyl or cyclopropylmethyl, R5 is methoxy, ethoxy, propoxy, isopropoxy, 2 methoxy-ethoxy, cyclopropyloxy, cyclopropylmethoxy, or completely or predominantly fluorine-substituted 1-2C-alkoxy, R6 is hydrogen, wherein R5 is bonded to the 6-position of the scaffold, or a salt, stereoisomer or salt of a stereoisomer thereof. 6. A compound according to claim 4, in which R1 is 2-(R11)-ethyl, or 3-(R11)-propyl, in which R11 is --N(R111)R112, in which either R111 is hydrogen, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, tertbutyl, allyl, propargyl, 1-methyl-propargyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, tertbutyl, allyl, propargyl, 1-methyl-propargyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is methyl, or R111 is ethyl, propyl, isopropyl, allyl, propargyl, 1-methyl-propargyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is ethyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which either Het is piperidin-1-yl, morpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, 2,5-dihydro-pyrrol-1-yl, 1,2,3,6-tetrahydropyridin-1-yl, 4-methyl-piperidin-1-yl, 4-fluoro-piperidin-1-yl, 4,4-difluoropiperidin-1-yl, (S)-3-fluoro-pyrrolidin-1-yl, (R)-3-fluoro-pyrrolidin-1-yl, or 3,3-difluoro-pyrrolidin-1-yl, in which R113 is methyl or acetyl, or Het is pyrazol-1-yl, or imidazol-1-yl, R2 is hydrogen, R3 is hydrogen, R4 is methyl, R5 is ethoxy, methoxy, difluoromethoxy or trifluoromethoxy, R6 is hydrogen or fluorine, wherein R5 is bonded to the 6-position of the scaffold, and wherein R6 is bonded to the 5- or 7-position of the scaffold, or a salt thereof. 7. A compound according to claim 4, in which R1 is 2-(R11)-ethyl, or 3-(R11)-propyl, in which R11 is --N(R111)R112, in which either R111 is methyl, ethyl, isopropyl, isobutyl, tertbutyl, allyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, or 2-methoxyethyl, and R112 is hydrogen, or R111 is methyl, ethyl, isopropyl, allyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, or 2-methoxyethyl, and R112 is methyl, or R111 is ethyl, 2-hydroxyethyl, or 2-methoxyethyl, and R112 is ethyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, pyrrolidin-1-yl, azetidin-1-yl, 2,5-dihydro-pyrrol-1-yl, or 1,2,3,6-tetrahydropyridin-1-yl, R2 is hydrogen, R3 is hydrogen, R4 is methyl, R5 is ethoxy, methoxy or difluoromethoxy, R6 is hydrogen or fluorine, wherein R5 is bonded to the 6-position of the scaffold, and wherein R6 is bonded to the 7-position of the scaffold, or a salt thereof. 8. A compound according to claim 4, in which R1 is methyl, 2-(R11)-ethyl, or 3-(R11)-propyl, in which R11 is --N(R111)R112, in which either R111 is hydrogen, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, cyclopropylmethyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is methyl, or R111 is ethyl, propyl, isopropyl, cyclopropyl, 2-hydroxyethyl, 2-methoxyethyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, and R112 is ethyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which either Het is piperidin-1-yl, morpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, or 4N-(R113)-piperazin-1-yl, in which R113 is hydrogen, methyl, ethyl, isopropyl, acetyl, 2-fluoroethyl, 2,2-difluoroethyl, or 2,2,2-trifluoroethyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and methyl, or Het is pyrazol-1-yl, imidazol-1-yl, or triazol-1-yl, R2 is hydrogen, R3 is hydrogen, R4 is methyl, ethyl, isopropyl or cyclopropyl, R5 is ethoxy, methoxy, propoxy, isopropoxy, cyclopropylmethoxy, or completely or predominantly fluorine-substituted 1-2C-alkoxy, R6 is hydrogen, wherein R5 is bonded to 6-position of the scaffold, or a salt thereof. 9. A compound according to claim 4, in which R1 is 2-(R11)-ethyl, or 3-(R11)-propyl, in which R11 is --N(R111)R112, in which either R111 is hydrogen, and R112 is hydrogen, or R111 is methyl, ethyl, propyl, isopropyl, isobutyl, cyclopropyl, cyclobutyl, or cyclopropylmethyl, and R112 is hydrogen, or R111 is methyl, ethyl, isopropyl, or cyclopropyl, and R112 is methyl, or R111 is ethyl, isopropyl, or cyclopropyl, and R112 is ethyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which either Het is piperidin-1-yl, morpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, 4N-(R113)-piperazin-1-yl, 4-methyl-piperidin-1-yl, 4-fluoro-piperidin-1-yl, 4,4-difluoropiperidin-1-yl, (S)-3-fluoro-pyrrolidin-1-yl, yl, 3,3-difluoro-pyrrolidin-1-yl, 3-fluoro-azetidin-1-yl, or 3,3-difluoro-azetidin-1-yl, in which R113 is hydrogen, methyl, or acetyl, or Het is pyrazol-1-yl, or imidazol-1-yl, R2 is hydrogen, R3 is hydrogen, R4 is methyl or ethyl, R5 is ethoxy, methoxy, or completely or predominantly fluorine-substituted 1-2C-alkoxy, R6 is hydrogen, wherein R5 is bonded to the 6-position of the scaffold, or a salt thereof. 10. A compound according to claim 4, in which R1 is methyl, 2-(R11)-ethyl, or 3-(R11)-propyl, in which R11 is --N(R111)R112, in which R111 is methyl, R112 is methyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, pyrrolidin-1-yl, 4-methyl-piperazin-1-yl, pyrazol-1-yl, imidazol-1-yl or triazol-1-yl, in which R2 is hydrogen, R3 is hydrogen, R4 is methyl, ethyl, isopropyl or cyclopropyl, R5 is methoxy, ethoxy, propoxy, isopropoxy, 2 methoxy-ethoxy, cyclopropylmethoxy, difluoromethoxy or trifluoromethoxy, R6 is hydrogen, wherein R5 is bonded to the 6-position of the scaffold, or a salt thereof. 11. A compound according to claim 1, which is a compound of formulae Ia*, Ib* or Ic* ##STR00968## in which R2 and R3 are both hydrogen, R4 is methyl or ethyl, and R1 and R5 have any of the following meanings: TABLE-US-00008 R1 R5 methyl --OCH.sub.3 methyl --OCH.sub.2CH.sub.3 methyl --OCH.sub.2CH.sub.2OCH.sub.3 methyl cyclopropylmethoxy methyl difluoromethoxy methyl trifluoromethoxy 2-(dimethylamino)-ethyl --OCH.sub.3 2-(dimethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(dimethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(dimethylamino)-ethyl cyclopropylmethoxy 2-(dimethylamino)-ethyl difluoromethoxy 2-(dimethylamino)-ethyl trifluoromethoxy 3-(dimethylamino)-propyl --OCH.sub.3 3-(dimethylamino)-propyl --OCH.sub.2CH.sub.3 3-(dimethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(dimethylamino)-propyl cyclopropylmethoxy 3-(dimethylamino)-propyl difluoromethoxy 3-(dimethylamino)-propyl trifluoromethoxy 2-(morpholin-4-yl)-ethyl --OCH.sub.3 2-(morpholin-4-yl)-ethyl --OCH.sub.2CH.sub.3 2-(morpholin-4-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(morpholin-4-yl)-ethyl cyclopropylmethoxy 2-(morpholin-4-yl)-ethyl difluoromethoxy 2-(morpholin-4-yl)-ethyl trifluoromethoxy 2-(pyrrolidin-1-yl)-ethyl --OCH.sub.3 2-(pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(pyrrolidin-1-yl)-ethyl cyclopropylmethoxy 2-(pyrrolidin-1-yl)-ethyl difluoromethoxy 2-(pyrrolidin-1-yl)-ethyl trifluoromethoxy 2-(imidazol-1-yl)-ethyl --OCH.sub.3 2-(imidazol-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(imidazol-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(imidazol-1-yl)-ethyl cyclopropylmethoxy 2-(imidazol-1-yl)-ethyl difluoromethoxy 2-(imidazol-1-yl)-ethyl trifluoromethoxy 2-(4-methyl-piperazin-1-yl)-ethyl --OCH.sub.3 2-(4-methyl-piperazin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(4-methyl-piperazin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(4-methyl-piperazin-1-yl)-ethyl cyclopropylmethoxy 2-(4-methyl-piperazin-1-yl)-ethyl difluoromethoxy 2-(4-methyl-piperazin-1-yl)-ethyl trifluoromethoxy 3-(morpholin-4-yl)-propyl --OCH.sub.3 3-(morpholin-4-yl)-propyl --OCH.sub.2CH.sub.3 3-(morpholin-4-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(morpholin-4-yl)-propyl cyclopropylmethoxy 3-(morpholin-4-yl)-propyl difluoromethoxy 3-(morpholin-4-yl)-propyl trifluoromethoxy 3-(pyrrolidin-1-yl)-propyl --OCH.sub.3 3-(pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(pyrrolidin-1-yl)-propyl cyclopropylmethoxy 3-(pyrrolidin-1-yl)-propyl difluoromethoxy 3-(pyrrolidin-1-yl)-propyl trifluoromethoxy 3-(imidazol-1-yl)-propyl --OCH.sub.3 3-(imidazol-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(imidazol-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(imidazol-1-yl)-propyl cyclopropylmethoxy 3-(imidazol-1-yl)-propyl difluoromethoxy 3-(imidazol-1-yl)-propyl trifluoromethoxy 3-(4-methyl-piperazin-1-yl)-propyl --OCH.sub.3 3-(4-methyl-piperazin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(4-methyl-piperazin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(4-methyl-piperazin-1-yl)-propyl cyclopropylmethoxy 3-(4-methyl-piperazin-1-yl)-propyl difluoromethoxy 3-(4-methyl-piperazin-1-yl)-propyl trifluoromethoxy 3-amino-propyl --OCH.sub.3 3-amino-propyl --OCH.sub.2CH.sub.3 3-amino-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-amino-propyl cyclopropylmethoxy 3-amino-propyl difluoromethoxy 3-amino-propyl trifluoromethoxy 2-amino-ethyl --OCH.sub.3 2-amino-ethyl --OCH.sub.2CH.sub.3 2-amino-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-amino-ethyl cyclopropylmethoxy 2-amino-ethyl difluoromethoxy 2-amino-ethyl trifluoromethoxy 2-(methylamino)-ethyl --OCH.sub.3 2-(methylamino)-ethyl --OCH.sub.2CH.sub.3 2-(methylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(methylamino)-ethyl cyclopropylmethoxy 2-(methylamino)-ethyl difluoromethoxy 2-(methylamino)-ethyl trifluoromethoxy 2-(ethylamino)-ethyl --OCH.sub.3 2-(ethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(ethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(ethylamino)-ethyl cyclopropylmethoxy 2-(ethylamino)-ethyl difluoromethoxy 2-(ethylamino)-ethyl trifluoromethoxy 2-(azetidin-1-yl)-ethyl --OCH.sub.3 2-(azetidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(azetidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(azetidin-1-yl)-ethyl cyclopropylmethoxy 2-(azetidin-1-yl)-ethyl difluoromethoxy 2-(azetidin-1-yl)-ethyl trifluoromethoxy 2-(4-acetyl-piperazin-1-yl)-ethyl --OCH.sub.3 2-(4-acetyl-piperazin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(4-acetyl-piperazin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(4-acetyl-piperazin-1-yl)-ethyl cyclopropylmethoxy 2-(4-acetyl-piperazin-1-yl)-ethyl difluoromethoxy 2-(4-acetyl-piperazin-1-yl)-ethyl trifluoromethoxy 2-(3,3-difluoropyrrolidin-1-yl)-ethyl --OCH.sub.3 2-(3,3-difluoropyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(3,3-difluoropyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(3,3-difluoropyrrolidin-1-yl)-ethyl cyclopropylmethoxy 2-(3,3-difluoropyrrolidin-1-yl)-ethyl difluoromethoxy 2-(3,3-difluoropyrrolidin-1-yl)-ethyl trifluoromethoxy 2-(2-fluoroethylamino)-ethyl --OCH.sub.3 2-(2-fluoroethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(2-fluoroethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(2-fluoroethylamino)-ethyl cyclopropylmethoxy 2-(2-fluoroethylamino)-ethyl difluoromethoxy 2-(2-fluoroethylamino)-ethyl trifluoromethoxy 2-(2,2-difluoroethylamino)-ethyl --OCH.sub.3 2-(2,2-difluoroethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(2,2-difluoroethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(2,2-difluoroethylamino)-ethyl cyclopropylmethoxy 2-(2,2-difluoroethylamino)-ethyl difluoromethoxy 2-(2,2-difluoroethylamino)-ethyl trifluoromethoxy 2-(2,2,2-trifluoroethylamino)-ethyl --OCH.sub.3 2-(2,2,2-trifluoroethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(2,2,2-trifluoroethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(2,2,2-trifluoroethylamino)-ethyl cyclopropylmethoxy 2-(2,2,2-trifluoroethylamino)-ethyl difluoromethoxy 2-(2,2,2-trifluoroethylamino)-ethyl trifluoromethoxy 2-(isopropylamino)-ethyl --OCH.sub.3 2-(isopropylamino)-ethyl --OCH.sub.2CH.sub.3 2-(isopropylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(isopropylamino)-ethyl cyclopropylmethoxy 2-(isopropylamino)-ethyl difluoromethoxy 2-(isopropylamino)-ethyl trifluoromethoxy 2-(isobutylamino)-ethyl --OCH.sub.3 2-(isobutylamino)-ethyl --OCH.sub.2CH.sub.3 2-(isobutylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(isobutylamino)-ethyl cyclopropylmethoxy 2-(isobutylamino)-ethyl difluoromethoxy 2-(isobutylamino)-ethyl trifluoromethoxy 2-(N-cyclopropylmethyl-amino)-ethyl --OCH.sub.3 2-(N-cyclopropylmethyl-amino)-ethyl --OCH.sub.2CH.sub.3 2-(N-cyclopropylmethyl-amino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(N-cyclopropylmethyl-amino)-ethyl cyclopropylmethoxy 2-(N-cyclopropylmethyl-amino)-ethyl difluoromethoxy 2-(N-cyclopropylmethyl-amino)-ethyl trifluoromethoxy 2-(cyclopropylamino)-ethyl --OCH.sub.3 2-(cyclopropylamino)-ethyl --OCH.sub.2CH.sub.3 2-(cyclopropylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(cyclopropylamino)-ethyl cyclopropylmethoxy 2-(cyclopropylamino)-ethyl difluoromethoxy 2-(cyclopropylamino)-ethyl trifluoromethoxy 2-(cyclobutylamino)-ethyl --OCH.sub.3 2-(cyclobutylamino)-ethyl --OCH.sub.2CH.sub.3 2-(cyclobutylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(cyclobutylamino)-ethyl cyclopropylmethoxy 2-(cyclobutylamino)-ethyl difluoromethoxy 2-(cyclobutylamino)-ethyl trifluoromethoxy 2-(N-ethyl-N-methyl-amino)-ethyl --OCH.sub.3 2-(N-ethyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.3 2-(N-ethyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(N-ethyl-N-methyl-amino)-ethyl cyclopropylmethoxy 2-(N-ethyl-N-methyl-amino)-ethyl difluoromethoxy 2-(N-ethyl-N-methyl-amino)-ethyl trifluoromethoxy 2-(diethylamino)-ethyl --OCH.sub.3 2-(diethylamino)-ethyl --OCH.sub.2CH.sub.3 2-(diethylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(diethylamino)-ethyl cyclopropylmethoxy 2-(diethylamino)-ethyl difluoromethoxy 2-(diethylamino)-ethyl trifluoromethoxy 2-(N-isopropyl-N-methyl-amino)-ethyl --OCH.sub.3 2-(N-isopropyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.3 2-(N-isopropyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(N-isopropyl-N-methyl-amino)-ethyl cyclopropylmethoxy 2-(N-isopropyl-N-methyl-amino)-ethyl difluoromethoxy 2-(N-isopropyl-N-methyl-amino)-ethyl trifluoromethoxy 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.3 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl cyclopropylmethoxy 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl difluoromethoxy 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl trifluoromethoxy 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.3 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl cyclopropylmethoxy 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl difluoromethoxy 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl trifluoromethoxy 2-(4-methyl-piperidin-1-yl)-ethyl --OCH.sub.3 2-(4-methyl-piperidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(4-methyl-piperidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(4-methyl-piperidin-1-yl)-ethyl cyclopropylmethoxy 2-(4-methyl-piperidin-1-yl)-ethyl difluoromethoxy 2-(4-methyl-piperidin-1-yl)-ethyl trifluoromethoxy 3-(methylamino)-propyl --OCH.sub.3 3-(methylamino)-propyl --OCH.sub.2CH.sub.3 3-(methylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(methylamino)-propyl cyclopropylmethoxy 3-(methylamino)-propyl difluoromethoxy 3-(methylamino)-propyl trifluoromethoxy 3-(ethylamino)-propyl --OCH.sub.3 3-(ethylamino)-propyl --OCH.sub.2CH.sub.3 3-(ethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(ethylamino)-propyl cyclopropylmethoxy 3-(ethylamino)-propyl difluoromethoxy 3-(ethylamino)-propyl trifluoromethoxy 3-(azetidin-1-yl)-propyl --OCH.sub.3 3-(azetidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(azetidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(azetidin-1-yl)-propyl cyclopropylmethoxy 3-(azetidin-1-yl)-propyl difluoromethoxy 3-(azetidin-1-yl)-propyl trifluoromethoxy 3-(4-acetyl-piperazin-1-yl)-propyl --OCH.sub.3 3-(4-acetyl-piperazin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(4-acetyl-piperazin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(4-acetyl-piperazin-1-yl)-propyl cyclopropylmethoxy 3-(4-acetyl-piperazin-1-yl)-propyl difluoromethoxy 3-(4-acetyl-piperazin-1-yl)-propyl trifluoromethoxy 3-(3,3-difluoropyrrolidin-1-yl)-propyl --OCH.sub.3 3-(3,3-difluoropyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(3,3-difluoropyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(3,3-difluoropyrrolidin-1-yl)-propyl cyclopropylmethoxy 3-(3,3-difluoropyrrolidin-1-yl)-propyl difluoromethoxy 3-(3,3-difluoropyrrolidin-1-yl)-propyl trifluoromethoxy 3-(2-fluoroethylamino)-propyl --OCH.sub.3 3-(2-fluoroethylamino)-propyl --OCH.sub.2CH.sub.3 3-(2-fluoroethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(2-fluoroethylamino)-propyl cyclopropylmethoxy 3-(2-fluoroethylamino)-propyl difluoromethoxy 3-(2-fluoroethylamino)-propyl trifluoromethoxy 3-(2,2-difluoroethylamino)-propyl --OCH.sub.3 3-(2,2-difluoroethylamino)-propyl --OCH.sub.2CH.sub.3 3-(2,2-difluoroethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(2,2-difluoroethylamino)-propyl cyclopropylmethoxy 3-(2,2-difluoroethylamino)-propyl difluoromethoxy 3-(2,2-difluoroethylamino)-propyl trifluoromethoxy 3-(2,2,2-trifluoroethylamino)-propyl --OCH.sub.3 3-(2,2,2-trifluoroethylamino)-propyl --OCH.sub.2CH.sub.3 3-(2,2,2-trifluoroethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(2,2,2-trifluoroethylamino)-propyl cyclopropylmethoxy 3-(2,2,2-trifluoroethylamino)-propyl difluoromethoxy 3-(2,2,2-trifluoroethylamino)-propyl trifluoromethoxy 3-(isopropylamino)-propyl --OCH.sub.3 3-(isopropylamino)-propyl --OCH.sub.2CH.sub.3 3-(isopropylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(isopropylamino)-propyl cyclopropylmethoxy 3-(isopropylamino)-propyl difluoromethoxy 3-(isopropylamino)-propyl trifluoromethoxy 3-(isobutylamino)-propyl --OCH.sub.3 3-(isobutylamino)-propyl --OCH.sub.2CH.sub.3 3-(isobutylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(isobutylamino)-propyl cyclopropylmethoxy 3-(isobutylamino)-propyl difluoromethoxy 3-(isobutylamino)-propyl trifluoromethoxy 3-(N-cyclopropylmethyl-amino)-propyl --OCH.sub.3 3-(N-cyclopropylmethyl-amino)-propyl --OCH.sub.2CH.sub.3 3-(N-cyclopropylmethyl-amino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(N-cyclopropylmethyl-amino)-propyl cyclopropylmethoxy 3-(N-cyclopropylmethyl-amino)-propyl difluoromethoxy 3-(N-cyclopropylmethyl-amino)-propyl trifluoromethoxy 3-(cyclopropylamino)-propyl --OCH.sub.3 3-(cyclopropylamino)-propyl --OCH.sub.2CH.sub.3 3-(cyclopropylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(cyclopropylamino)-propyl cyclopropylmethoxy 3-(cyclopropylamino)-propyl difluoromethoxy 3-(cyclopropylamino)-propyl trifluoromethoxy 3-(cyclobutylamino)-propyl --OCH.sub.3 3-(cyclobutylamino)-propyl --OCH.sub.2CH.sub.3 3-(cyclobutylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(cyclobutylamino)-propyl cyclopropylmethoxy 3-(cyclobutylamino)-propyl difluoromethoxy 3-(cyclobutylamino)-propyl trifluoromethoxy 3-(N-ethyl-N-methyl-amino)-propyl --OCH.sub.3 3-(N-ethyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.3 3-(N-ethyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(N-ethyl-N-methyl-amino)-propyl cyclopropylmethoxy 3-(N-ethyl-N-methyl-amino)-propyl difluoromethoxy 3-(N-ethyl-N-methyl-amino)-propyl trifluoromethoxy 3-(diethylamino)-propyl --OCH.sub.3 3-(diethylamino)-propyl --OCH.sub.2CH.sub.3 3-(diethylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(diethylamino)-propyl cyclopropylmethoxy 3-(diethylamino)-propyl difluoromethoxy 3-(diethylamino)-propyl trifluoromethoxy 3-(N-isopropyl-N-methyl-amino)-propyl --OCH.sub.3 3-(N-isopropyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.3 3-(N-isopropyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(N-isopropyl-N-methyl-amino)-propyl cyclopropylmethoxy 3-(N-isopropyl-N-methyl-amino)-propyl difluoromethoxy 3-(N-isopropyl-N-methyl-amino)-propyl trifluoromethoxy 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.3 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl cyclopropylmethoxy 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl difluoromethoxy 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl trifluoromethoxy 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.3 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl cyclopropylmethoxy 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl difluoromethoxy 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl trifluoromethoxy 3-(4-methyl-piperidin-1-yl)-propyl --OCH.sub.3 3-(4-methyl-piperidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(4-methyl-piperidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(4-methyl-piperidin-1-yl)-propyl cyclopropylmethoxy 3-(4-methyl-piperidin-1-yl)-propyl difluoromethoxy 3-(4-methyl-piperidin-1-yl)-propyl trifluoromethoxy 3-[N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.3 3-[N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-(2-hydroxyethyl)-amino]-propyl cyclopropylmethoxy 3-[N-(2-hydroxyethyl)-amino]-propyl difluoromethoxy 3-[N-(2-hydroxyethyl)-amino]-propyl trifluoromethoxy 3-[N-(2-methoxyethyl)-amino]-propyl --OCH.sub.3 3-[N-(2-methoxyethyl)-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-(2-methoxyethyl)-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-(2-methoxyethyl)-amino]-propyl cyclopropylmethoxy 3-[N-(2-methoxyethyl)-amino]-propyl difluoromethoxy 3-[N-(2-methoxyethyl)-amino]-propyl trifluoromethoxy 3-(tertbutylamino)-propyl --OCH.sub.3 3-(tertbutylamino)-propyl --OCH.sub.2CH.sub.3 3-(tertbutylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(tertbutylamino)-propyl cyclopropylmethoxy 3-(tertbutylamino)-propyl difluoromethoxy 3-(tertbutylamino)-propyl trifluoromethoxy 3-(allylamino)-propyl --OCH.sub.3 3-(allylamino)-propyl --OCH.sub.2CH.sub.3 3-(allylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(allylamino)-propyl cyclopropylmethoxy 3-(allylamino)-propyl difluoromethoxy 3-(allylamino)-propyl trifluoromethoxy 3-(propargylamino)-propyl --OCH.sub.3 3-(propargylamino)-propyl --OCH.sub.2CH.sub.3 3-(propargylamino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(propargylamino)-propyl cyclopropylmethoxy 3-(propargylamino)-propyl difluoromethoxy 3-(propargylamino)-propyl trifluoromethoxy 3-(N-allyl-N-methyl-amino)-propyl --OCH.sub.3 3-(N-allyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.3 3-(N-allyl-N-methyl-amino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(N-allyl-N-methyl-amino)-propyl cyclopropylmethoxy 3-(N-allyl-N-methyl-amino)-propyl difluoromethoxy 3-(N-allyl-N-methyl-amino)-propyl trifluoromethoxy 3-(N-methyl-N-propargyl-amino)-propyl --OCH.sub.3 3-(N-methyl-N-propargyl-amino)-propyl --OCH.sub.2CH.sub.3 3-(N-methyl-N-propargyl-amino)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(N-methyl-N-propargyl-amino)-propyl cyclopropylmethoxy 3-(N-methyl-N-propargyl-amino)-propyl difluoromethoxy 3-(N-methyl-N-propargyl-amino)-propyl trifluoromethoxy 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl --OCH.sub.3 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl cyclopropylmethoxy 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl difluoromethoxy 3-[N-(2-hydroxyethyl)-N-methyl-amino]-propyl trifluoromethoxy 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl --OCH.sub.3 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl cyclopropylmethoxy 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl difluoromethoxy 3-[N-(2-methoxyethyl)-N-methyl-amino]-propyl trifluoromethoxy 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.3 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl cyclopropylmethoxy 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl difluoromethoxy 3-[N-ethyl-N-(2-hydroxyethyl)-amino]-propyl trifluoromethoxy 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl --OCH.sub.3 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl --OCH.sub.2CH.sub.3 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl cyclopropylmethoxy 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl difluoromethoxy 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl trifluoromethoxy 3-(piperidin-1-yl)-propyl --OCH.sub.3 3-(piperidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(piperidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(piperidin-1-yl)-propyl cyclopropylmethoxy 3-(piperidin-1-yl)-propyl difluoromethoxy 3-(piperidin-1-yl)-propyl trifluoromethoxy 3-(homopiperidin-1-yl)-propyl --OCH.sub.3 3-(homopiperidin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(homopiperidin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(homopiperidin-1-yl)-propyl cyclopropylmethoxy 3-(homopiperidin-1-yl)-propyl difluoromethoxy 3-(homopiperidin-1-yl)-propyl trifluoromethoxy 3-(2,5-dihydropyrrol-1-yl)-propyl --OCH.sub.3 3-(2,5-dihydropyrrol-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(2,5-dihydropyrrol-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(2,5-dihydropyrrol-1-yl)-propyl cyclopropylmethoxy 3-(2,5-dihydropyrrol-1-yl)-propyl difluoromethoxy 3-(2,5-dihydropyrrol-1-yl)-propyl trifluoromethoxy 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl --OCH.sub.3 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl --OCH.sub.2CH.sub.3 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl --OCH.sub.2CH.sub.2OCH.sub.3 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl cyclopropylmethoxy 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl difluoromethoxy 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl trifluoromethoxy 2-[N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.3 2-[N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-(2-hydroxyethyl)-amino]-ethyl cyclopropylmethoxy 2-[N-(2-hydroxyethyl)-amino]-ethyl difluoromethoxy 2-[N-(2-hydroxyethyl)-amino]-ethyl trifluoromethoxy 2-[N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.3 2-[N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-(2-methoxyethyl)-amino]-ethyl cyclopropylmethoxy 2-[N-(2-methoxyethyl)-amino]-ethyl difluoromethoxy 2-[N-(2-methoxyethyl)-amino]-ethyl trifluoromethoxy 2-(tertbutylamino)-ethyl --OCH.sub.3 2-(tertbutylamino)-ethyl --OCH.sub.2CH.sub.3 2-(tertbutylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(tertbutylamino)-ethyl cyclopropylmethoxy 2-(tertbutylamino)-ethyl difluoromethoxy 2-(tertbutylamino)-ethyl trifluoromethoxy 2-(allylamino)-ethyl --OCH.sub.3 2-(allylamino)-ethyl --OCH.sub.2CH.sub.3 2-(allylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(allylamino)-ethyl cyclopropylmethoxy 2-(allylamino)-ethyl difluoromethoxy 2-(allylamino)-ethyl trifluoromethoxy 2-(propargylamino)-ethyl --OCH.sub.3 2-(propargylamino)-ethyl --OCH.sub.2CH.sub.3 2-(propargylamino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(propargylamino)-ethyl cyclopropylmethoxy 2-(propargylamino)-ethyl difluoromethoxy 2-(propargylamino)-ethyl trifluoromethoxy 2-(N-allyl-N-methyl-amino)-ethyl --OCH.sub.3 2-(N-allyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.3 2-(N-allyl-N-methyl-amino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(N-allyl-N-methyl-amino)-ethyl cyclopropylmethoxy 2-(N-allyl-N-methyl-amino)-ethyl difluoromethoxy 2-(N-allyl-N-methyl-amino)-ethyl trifluoromethoxy 2-(N-methyl-N-propargyl-amino)-ethyl --OCH.sub.3 2-(N-methyl-N-propargyl-amino)-ethyl --OCH.sub.2CH.sub.3 2-(N-methyl-N-propargyl-amino)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(N-methyl-N-propargyl-amino)-ethyl cyclopropylmethoxy 2-(N-methyl-N-propargyl-amino)-ethyl difluoromethoxy 2-(N-methyl-N-propargyl-amino)-ethyl trifluoromethoxy 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl --OCH.sub.3 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl cyclopropylmethoxy 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl difluoromethoxy 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl trifluoromethoxy 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl --OCH.sub.3 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl cyclopropylmethoxy 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl difluoromethoxy 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl trifluoromethoxy 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.3 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl cyclopropylmethoxy 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl difluoromethoxy 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl trifluoromethoxy 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.3 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.3 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl cyclopropylmethoxy 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl difluoromethoxy 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl trifluoromethoxy 2-(piperidin-1-yl)-ethyl --OCH.sub.3 2-(piperidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(piperidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(piperidin-1-yl)-ethyl cyclopropylmethoxy 2-(piperidin-1-yl)-ethyl difluoromethoxy 2-(piperidin-1-yl)-ethyl trifluoromethoxy 2-(homopiperidin-1-yl)-ethyl --OCH.sub.3 2-(homopiperidin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(homopiperidin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(homopiperidin-1-yl)-ethyl cyclopropylmethoxy 2-(homopiperidin-1-yl)-ethyl difluoromethoxy 2-(homopiperidin-1-yl)-ethyl trifluoromethoxy 2-(2,5)-dihydropyrrol-1-yl)-ethyl --OCH.sub.3 2-(2,5)-dihydropyrrol-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(2,5)-dihydropyrrol-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(2,5)-dihydropyrrol-1-yl)-ethyl cyclopropylmethoxy 2-(2,5)-dihydropyrrol-1-yl)-ethyl difluoromethoxy 2-(2,5)-dihydropyrrol-1-yl)-ethyl trifluoromethoxy 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl --OCH.sub.3 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl --OCH.sub.2CH.sub.3 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl --OCH.sub.2CH.sub.2OCH.sub.3 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl cyclopropylmethoxy 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl difluoromethoxy 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl trifluoromethoxy or a salt thereof. 12. A compound, which is one of the following compounds 1. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2,3a-dimethyl-3a,4,9,10-tetrahyd- ro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 2. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-(2-methoxy-ethoxy)-2,3a-dimethyl-3a,4,9- ,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 3. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-2,3a-dimethyl-3a,4,9,10-tetrahy- dro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 6. (3aS,10R)-2-(2-Dimethylamino-ethyl)-10-(3-hydroxy-phenyl)-6-(2-methoxy-et- hoxy)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 7. (3aS,10R)-2-(2-Dimethylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 10. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-morpholin-4-- yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-di- one 11. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-pyrrolidi- n-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 12. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-methyl-pipera- zin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 13. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(2-imidazol-1-yl-ethyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 14. (3aS,10R)-2-(4-Dimethylamino-butyl)-10-(3-hydroxy-phenyl)-6-methoxy-3- a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dio- ne 15. (3aS,10R)-2-(3-Dimethylamino-propyl)-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 18. (3aS,10R)-2-(2-Dimethylamino-ethyl)-3a-ethyl-10-(3-hydroxy-pheny- l)-6-methoxy-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 19. (3aS,10R)-2-(3-Dimethylamino-propyl)-3a-ethyl-10-(3-hydroxy-phe- nyl)-6-methoxy-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 20. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(3-imidazol-1-yl-propyl)-6-methoxy-3a-m- ethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 21. (3aS,10R)-6-Cyclopropylmethoxy-10-(3-hydroxy-phenyl)-2,3a-dimethyl-3a- ,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 22. (3aS,10R)-2-(2-Bromo-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-3a,4- ,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 23. (3aS,10R)-2-(2-Dimethylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-met- hyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 24. (3aS,10R)-2-(2-Bromo-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl- -3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 25. (3aS,10R)-2-(2-Amino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-3a,- 4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 27. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-methylamino-ethy- l)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 32. (3aS,10R)-2-[2-(4-Acetyl-piperazin-1-yl)-ethyl]-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 33. (3aS,10R)-2-(2-Azetidin-1-yl-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 34. (3aS,10R)-2-[2-(3,3-Difluoro-pyrrolidin-1-yl)-ethyl]-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 35. (3aS,10R)-2-(2-Ethylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-methy- l-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 36. (3aS,10R)-2-(2-Bromo-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy-phenyl- )-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 41. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-methylam- ino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 42. (3aS, OR)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-methyla- mino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 43. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-(2-dimethylamino-ethyl)-10-- (3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopent- a[b]fluorene-1,3-dione 44. (3aS,10R)-2-(2-Azetidin-1-yl-ethyl)-6-(1-difluoro-methoxy)-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 45. (3aS,10R)-2-(2-Amino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-3a,4- ,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 46. (3aS,10R)-2-(2-Azetidin-1-yl-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-met- hyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 47. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(2-isopropylamino-ethyl)-6-methoxy-- 3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-di- one 48. (3aS,10R)-2-[2-(Cyclopropylmethyl-amino)-ethyl]-10-(3-hydroxy-phen- yl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 49. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(2-isobutylamino-ethyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 50. (3aS,10R)-2-(2-Cyclobutylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 51. (3aS,10R)-2-(3-Ethylamino-propyl)-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 52. (3aS,10R)-2-[2-(Ethyl-methyl-amino)-ethyl]-10-(3-hydroxy-phenyl)-- 6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluor- ene-1,3-dione, 53. (3aS,10R)-2-(2-Cyclopropylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e, 55. (3aS,10R)-2-(3-Chloro-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 56. (3aS,10R)-2-(3-Chloro-propyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 59. (3aS,10R)-2-(3-Chloro-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-3a- ,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 60. (3aS,10R)-2-(2-Bromo-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-m- ethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 62. (3aS,10R)-2-(2-Bromo-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-methoxy-- 3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-di- one 63. (3aS,10R)-2-(3-Chloro-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 65. (3aS,10R)-2-(3-Chloro-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 67. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(3-isopropylamino-propyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 68. (3aS,10R)-2-[2-(3,6-Dihydro-2H-pyridin-1-yl)-ethyl]-10-(3-hydrox- y-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopen- ta[b]fluorene-1,3-dione 69. (3aS,10R)-2-(2-Diethylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-met- hyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 70. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-[2-(isopropyl-methyl-amino)-ethyl]-- 6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluor- ene-1,3-dione 71. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-piperidin-1-yl-e- thyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 72. (3aS,10R)-2-(2-tert-Butylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 73. (3aS, OR)-2-[2-(2,2-Difluoro-ethylamino)-ethyl]-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 74. (3aS,10R)-2-(2-Azepan-1-yl-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 75. (3aS, OR)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-methyl-piperidin-1-- yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 76. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-methylam- ino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 77. (3aS, OR)-2-[3-(Ethyl-methyl-amino)-propyl]-10-(3-hydroxy-phenyl)-6-methoxy-3a-- methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 78. (3aS,10R)-2-{2-[Ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 79. (3aS,10R)-2-{2-[Ethyl-(2-methoxy-ethyl)-amino]-ethyl}-10-(3-hydroxy-pheny- l)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 80. (3aS,10R)-2-[2-(Allyl-methyl-amino)-ethyl]-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 81. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(methyl- -prop-2-ynyl-amino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 82. (3aS,10R)-2-[2-(2-Hydroxy-ethylamino)-ethyl]-10-(3-hydroxy-phenyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 83. (3aS, OR)-10-(3-Hydroxy-phenyl)-6-methoxy-2-[2-(2-methoxy-ethylamino)-ethyl]-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 84. (3aS,10R)-2-(2-Allylamino-ethyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-- methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 85. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-prop-2-ynyla- mino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 86. (3aS,10R)-2-(3-Cyclobutylamino-propyl)-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 87. (3aS,10R)-2-(3-Azetidin-1-yl-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-m- ethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 88. (3aS,10R)-2-[3-(Allyl-methyl-amino)-propyl]-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 89. (3aS,10R)-2-{3-[Ethyl-(2-hydroxy-ethyl)-amino]-propyl}-10-(3-hydroxy-phen- yl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 90. (3aS,10R)-2-{3-[Ethyl-(2-methoxy-ethyl)-amino]-propyl}-10-(3-hydroxy-phen- yl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 91. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(1-methyl-1H-pyr- azol-3-ylamino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 92. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-(3-isobutylamino-propyl)-6-methoxy-3a-m- ethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 93. (3aS,10R)-2-(3-Cyclopropylamino-propyl)-10-(3-hydroxy-phenyl)-6-metho- xy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 94. (3aS,10R)-10-(3-Hydroxy-phenyl)-2-[3-(isopropyl-methyl-amino)-p- ropyl]-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 95. (3aS,10R)-2-[3-(Cyclopropylmethyl-amino)-propyl]-10-(3-hydroxy-phenyl)-6-- methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 96. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-pyrrolidin-1-yl-- propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 105. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-piperidin-- 1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 106. (3aS,10R)-2-[3-(3,6-Dihydro-2H-pyridin-1-yl)-propyl]-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 107. (3aS,10R)-2-(3-Diethylamino-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 112. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-methyl-p- iperidin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 113. (3aS,10R)-2-(3-Azepan-1-yl-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-met- hyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 118. (3aS,10R)-2-{2-[(2-Hydroxy-ethyl)-methyl-amino]-ethyl}-10-(3-hydroxy- -phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopent- a[b]fluorene-1,3-dione 119. (3aS,10R)-2-[2-(2,5-Dihydro-pyrrol-1-yl)-ethyl]-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 134. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(2-methyl-2H-pyr- azol-3-ylamino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 142. (3aS,10R)-2-[3-(2,2-Difluoro-ethylamino)-propyl]-10-(3-hydroxy-phenyl)-6-- methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 143. (3aS,10R)-2-{3-[(2-Hydroxy-ethyl)-methyl-amino]-propyl}-10-(3-hydroxy-phe- nyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]- fluorene-1,3-dione 144. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(methyl-prop-2-y- nyl-amino)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluore- ne-1,3-dione 145. (3aS,10R)-2-[3-(2-Hydroxy-ethylamino)-propyl]-10-(3-hydroxy-phenyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 146. (3aS,10R)-2-(3-Allylamino-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a-meth- yl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 147. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-prop-2-ynyl- amino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 148. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-morpholin-4-yl-p- ropyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 149. (3aS,10R)-2-[3-(2,5-Dihydro-pyrrol-1-yl)-propyl]-10-(3-hydroxy-pheny- l)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 150. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-methyl-pipera- zin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 151. (3aS,10R)-2-[3-(4-Acetyl-piperazin-1-yl)-propyl]-10-(3-hydroxy-phenyl)-6-- methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 152. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-(2-isopropylamino-ethyl)-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 153. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-(2-isobutylamino-ethyl)-3- a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dio- ne 154. (3aS,10R)-2-[2-(Cyclopropylmethyl-amino)-ethyl]-6-ethoxy-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 155. (3aS,10R)-2-(2-Cyclobutylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-m- ethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 156. (3aS,10R)-2-(2-tert-Butylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 157. (3aS,10R)-2-(2-Allylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-- 3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-di- one 158. (3aS,10R)-6-Ethoxy-2-[2-(ethyl-methyl-amino)-ethyl]-10-(3-hydroxy- -phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluore- ne-1,3-dione 159. (3aS,10R)-6-Ethoxy-2-[2-(2-hydroxy-ethylamino)-ethyl]-10-(3-hydroxy-pheny- l)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 160. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-[2-(2-methoxy-ethylamino)-ethy- l]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 161. (3aS,10R)-2-(2-Cyclopropylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-- methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 162. (3aS,10R)-2-(2-Diethylamino-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 163. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-[2-(isopropyl-methyl-ami- no)-ethyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 164. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-piperidin-1-yl-et- hyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 165. (3aS,10R)-2-[2-(3,6-Dihydro-2H-pyridin-1-yl)-ethyl]-6-ethoxy-10-(3-h- ydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]- fluorene-1,3-dione 166. (3aS,10R)-2-(2-Azepan-1-yl-ethyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-methy- l-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 167. (3aS,10R)-2-(3-tert-Butylamino-propyl)-10-(3-hydroxy-phenyl)-6-methoxy-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 176. (3aS,10R)-2-(3-Diethylamino-propyl)-6-(1,1-difluoro-methoxy)-10-(3-- hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 177. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{3-[ethyl-(2-hydroxy-ethyl)-amino]-p- ropyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza- -cyclopenta[b]fluorene-1,3-dione 178. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{3-[ethyl-(2-methoxy-ethyl)-amino]-p- ropyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza- -cyclopenta[b]fluorene-1,3-dione 179. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-[3-(isopropyl-- methyl-amino)-propyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 182. (3aS,10R)-2-(3-tert-Butylamino-propyl)-6-(1,1-difluoro-methoxy)-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 183. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(- methyl-prop-2-ynyl-amino)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cycl- openta[b]fluorene-1,3-dione 184. (3aS,10R)-2-[3-(Allyl-methyl-amino)-propyl]-6-(1,1-difluoro-methoxy)-10-(- 3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta- [b]fluorene-1,3-dione 186. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-methylamino-propy- l)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 187. (3aS,10R)-6-Ethoxy-2-(3-ethylamino-propyl)-10-(3-hydroxy-phenyl)-3a-- methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 188. (3aS,10R)-2-[3-(Cyclopropylmethyl-amino)-propyl]-6-ethoxy-10-(3-hydr- oxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 189. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-[3-(2-methoxy-ethylamino)-prop- yl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 190. (3aS,10R)-2-(3-Cyclopropylamino-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 191. (3aS,10R)-2-(3-Allylamino-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a- -methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 192. (3aS,10R)-6-Ethoxy-2-[3-(ethyl-methyl-amino)-propyl]-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 193. (3aS,10R)-6-Ethoxy-2-{3-[(2-hydroxy-ethyl)-methyl-amino]-propyl}-10-(3-hy- droxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 194. (3aS,10R)-6-Ethoxy-2-{3-[ethyl-(2-hydroxy-ethyl)-amino]-propyl}-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 195. (3aS,10R)-6-Ethoxy-2-{3-[ethyl-(2-methoxy-ethyl)-amino]-propyl}-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 196. (3aS,10R)-2-[3-(Allyl-methyl-amino)-propyl]-6-ethoxy-10-(3-hydroxy-phenyl- )-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 197. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-2-[3-(isopropyl-methyl- -amino)-propyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 198. (3aS,10R)-2-(3-Azetidin-1-yl-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-me- thyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 199. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-(3-isobut- ylamino-propyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 200. (3aS,10R)-2-[3-(Cyclopropylmethyl-amino)-propyl]-6-(1,1-difluoro-methoxy)- -10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 201. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[3-(2-hydroxy-ethylamino)-propyl]-10- -(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopen- ta[b]fluorene-1,3-dione 202. (3aS,10R)-2-(3-Cyclopropylamino-propyl)-6-(1,1-difluoro-methoxy)-10-(3-hy- droxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 203. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-m- ethylamino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluore- ne-1,3-dione 204. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-(3-ethylamino-propyl)-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 205. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-[3-(2-methoxy-- ethylamino)-propyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopen- ta[b]fluorene-1,3-dione 206. (3aS,10R)-2-(3-Allylamino-propyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 207. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-morpholin-4-yl-pr- opyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 208. (3aS,10R)-2-[3-(3,6-Dihydro-2H-pyridin-1-yl)-propyl]-6-ethoxy-10-(3-- hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 209. (3aS,10R)-2-[3-(4-Acetyl-piperazin-1-yl)-propyl]-6-ethoxy-10-(3-hydroxy-p- henyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 210. (3aS,10R)-2-(3-Azepan-1-yl-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)-3a-meth- yl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 221. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-pyrrolidin-1- -yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 222. (3aS,10R)-2-[3-(2,5-Dihydro-pyrrol-1-yl)-propyl]-6-ethoxy-10-(3- -hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 223. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-piperidin-1-yl-pr- opyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 224. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(4-methyl-pi- peridin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 225. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-prop-2-ynylamino-- propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dion- e 226. (3aS,10R)-2-(3-Dimethylamino-propyl)-6-ethoxy-10-(3-hydroxy-phenyl)- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 227. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(methyl-- prop-2-ynyl-amino)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 229. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(4-methyl-piperaz- in-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 236. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-m- orpholin-4-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 237. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-p- yrrolidin-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 238. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[3-(2,5-dihydro-pyrrol-1-yl)-propyl]- -10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 239. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(3-p- iperidin-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 240. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(- 4-methyl-piperazin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 241. (3aS,10R)-2-[3-(4-Acetyl-piperazin-1-yl)-propyl]-6-(1,1-difluoro-methoxy)- -10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 242. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[3-(3,6-dihydro-2H-pyridin-1-yl)-pro- pyl]-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-c- yclopenta[b]fluorene-1,3-dione 243. (3aS,10R)-2-(3-Azepan-1-yl-propyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy- -phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluore- ne-1,3-dione 244. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[3-(- 4-methyl-piperidin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 245. (3aS,10R)-7-Fluoro-2-[2-(2-hydroxy-ethylamino)-ethyl]-10-(3-hydroxy-pheny- l)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 246. (3aS,10R)-7-Fluoro-2-{2-[(2-hydroxy-ethyl)-methyl-amino]-ethyl}-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 247. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[3-(ethyl-methyl-amino)-propyl]hydro- xy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 248. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-methyla- mino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 249. (3aS,10R)-2-(2-Ethylamino-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 250. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-(2-isopropylamino-ethyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 251. (3aS,10R)-2-[2-(Cyclopropylmethyl-amino)-ethyl]-7-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 252. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-(2-isobutylamino-ethyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 253. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-2-[2-(2-methoxy-ethyla- mino)-ethyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 254. (3aS,10R)-2-(2-Allylamino-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 255. (3aS,10R)-2-(2-Dimethylamino-ethyl)-7-fluoro-10-(3-hydroxy-pheny- l)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 256. (3aS,10R)-2-(2-tert-Butylamino-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-me- thoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 257. (3aS,10R)-2-[2-(Ethyl-methyl-amino)-ethyl]-7-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 258. (3aS,10R)-2-(2-Diethylamino-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-metho- xy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 259. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-[2-(isopropyl-methyl-amino)-et- hyl]-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]- fluorene-1,3-dione 260. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-morphol- in-4-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 261. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-pyrroli- din-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 262. (3aS,10R)-2-[2-(2,5-Dihydro-pyrrol-1-yl)-ethyl]-7-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 263. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-piperid- in-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 264. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-meth- yl-piperidin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 265. (3aS,10R)-2-[2-(3,6-Dihydro-2H-pyridin-1-yl)-ethyl]-7-fluoro-10-(3-hydrox- y-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopen- ta[b]fluorene-1,3-dione 266. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-meth- yl-piperazin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 267. (3aS,10R)-2-[2-(4-Acetyl-piperazin-1-yl)-ethyl]-7-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 268. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-(2-isopropylam- ino-ethyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 269. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-(2-isobutylami- no-ethyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluor- ene-1,3-dione 270. (3aS,10R)-2-[2-(Cyclopropylmethyl-amino)-ethyl]-6-(1,1-difluoro-methoxy)-- 10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 271. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-[2-(2-methoxy-- ethylamino)-ethyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopent- a[b]fluorene-1,3-dione 272. (3aS,10R)-2-(2-Cyclobutylamino-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydr- oxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 273. (3aS,10R)-2-(2-tert-Butylamino-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydr- oxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 274. (3aS,10R)-2-(2-Allylamino-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy-p- henyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 275. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[2-(ethyl-methyl-amino)-ethyl]hydrox- y-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluor- ene-1,3-dione 276. (3aS,10R)-2-(2-Diethylamino-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy- -phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluore- ne-1,3-dione 277. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{2-[ethyl-(2-hydroxy-ethyl)-amino]-e- thyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-- cyclopenta[b]fluorene-1,3-dione 278. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-2-[2-(isopropyl-- methyl-amino)-ethyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclope- nta[b]fluorene-1,3-dione 279. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-p- yrrolidin-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 280. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-p- iperidin-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 281. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[2-(3,6-dihydro-2H-pyridin-1-yl)-eth- yl]hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopent- a[b]fluorene-1,3-dione 282. (3aS,10R)-2-(2-Azepan-1-yl-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hydroxy-- phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 283. (3aS,10R)-2-(2-Amino-ethyl)-6-(1-difluoro-methoxy)-10-(3-hydroxy-phenyl)-- 3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-di- one 284. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-(2-ethylamino-ethyl)-10-(3-h- ydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]- fluorene-1,3-dione 285. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-[2-(2-hydroxy-ethylamino)-ethyl]-10-- (3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopent- a[b]fluorene-1,3-dione 286. (3aS,10R)-2-(2-Cyclopropylamino-ethyl)-6-(1,1-difluoro-methoxy)-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 287. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-p- rop-2-ynylamino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 288. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{2-[(2-hydroxy-ethyl)-methyl-amino]-- ethyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza- -cyclopenta[b]fluorene-1,3-dione 289. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{2-[ethyl-(2-methoxy-ethyl)-amino]-e- thyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-- cyclopenta[b]fluorene-1,3-dione 290. (3aS,10R)-2-[2-(Allyl-methyl-amino)-ethyl]-6-(1,1-difluoro-methoxy)-10-(3- -hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 291. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[2-(- methyl-prop-2-ynyl-amino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 292. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-(2-m- orpholin-4-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 293. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[2-(- 4-methyl-piperidin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 294. (3aS,10R)-6-(1,1-Difluoro-methoxy)-10-(3-hydroxy-phenyl)-3a-methyl-2-[2-(- 4-methyl-piperazin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 295. (3aS,10R)-2-[2-(4-Acetyl-piperazin-1-yl)-ethyl]-6-(1,1-difluoro-methoxy)-- 10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 296. (3aS,10R)-6-Ethoxy-2-(2-ethylamino-ethyl)-10-(3-hydroxy-phenyl)-3a-methyl- -3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione 297. (3aS,10R)-6-Ethoxy-2-{2-[(2-hydroxy-ethyl)-methyl-amino]-ethyl}-10-(3-hyd- roxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 298. (3aS,10R)-6-Ethoxy-2-{2-[ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-10-(3-hydr- oxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 299. (3aS,10R)-6-Ethoxy-2-{2-[ethyl-(2-methoxy-ethyl)-amino]-ethyl}-10-(3-hydr- oxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 300. (3aS,10R)-2-[2-(Allyl-methyl-amino)-ethyl]-6-ethoxy-10-(3-hydroxy-phenyl)- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 301. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-[2-(methyl-- prop-2-ynyl-amino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 302. (3aS,10R)-6-Ethoxy-10-(3-hydroxy-phenyl)-3a-methyl-2-[2-(4-methyl-piperid- in-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 303. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-methyla- mino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 304. (3aS,10R)-2-[3-(Cyclopropylmethyl-amino)-propyl]-7-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 305. (3aS,10R)-7-Fluoro-2-[3-(2-hydroxy-ethylamino)-propyl]-10-(3-hydroxy-phen- yl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 306. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-2-[3-(2-methoxy-ethyla- mino)-propyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 307. (3aS,10R)-2-(3-Cyclopropylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-- methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 308. (3aS,10R)-2-(3-tert-Butylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 309. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-prop-2-- ynylamino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 310. (3aS,10R)-2-(3-Dimethylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 311. (3aS,10R)-2-[3-(Ethyl-methyl-amino)-propyl]-7-fluoro-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 312. (3aS,10R)-7-Fluoro-2-{3-[(2-hydroxy-ethyl)-methyl-amino]-propyl}-10-(3-hy- droxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cycl- openta[b]fluorene-1,3-dione 313. (3aS,10R)-2-(3-Diethylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 314. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-(3-dimethylamino-propyl)-10-(3-hydro- xy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 315. (3aS,10R)-2-[3-[Ethyl-(2-hydroxy-ethyl)-amino]-propyl]-7-fluoro-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 316. (3aS,10R)-2-{3-[Ethyl-(2-methoxy-ethyl)-amino]-propyl}-7-fluoro-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 317. (3aS,10R)-2-[3-(Allyl-methyl-amino)-propyl]-7-fluoro-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 318. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(methyl- -prop-2-ynyl-amino)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta- [b]fluorene-1,3-dione 319. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-[3-(isopropyl-methyl-amino)-pr- opyl]-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 320. (3aS,10R)-2-(3-Azetidin-1-yl-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 321. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-morphol- in-4-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 322. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-pyrroli- din-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 323. (3aS,10R)-2-[3-(2,5-Dihydro-pyrrol-1-yl)-propyl]-7-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 324. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-piperid- in-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 325. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-meth- yl-piperazin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 326. (3aS,10R)-2-[3-(3,6-Dihydro-2H-pyridin-1-yl)-propyl]-7-fluoro-10-(3-hydro- xy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclope- nta[b]fluorene-1,3-dione 327. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-meth- yl-piperidin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 328. (3aS,10R)-2-[3-(4-Acetyl-piperazin-1-yl)-propyl]-7-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 329. (3aS,10R)-2-(3-Azepan-1-yl-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-metho- xy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 330. (3aS,10R)-2-(3-Ethylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 331. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-(3-isopropylamino-pr- opyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 332. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-2-(3-isobutylamino-propyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 333. (3aS,10R)-2-(3-Cyclobutylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 334. (3aS,10R)-2-(3-Allylamino-propyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 363. (3aS,10R)-2-(3-Allylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 364. (3aS,10R)-2-[3-(Ethyl-methyl-amino)-propyl]-5-fluoro-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 365. (3aS,10R)-2-{3-[Ethyl-(2-methoxy-ethyl)-amino]-propyl}-5-fluoro-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 366. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-piperid- in-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 367. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-meth- yl-piperidin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 368. (3aS,10R)-2-[3-(3,6-Dihydro-2H-pyridin-1-yl)-propyl]-5-fluoro-10-(3-hydro- xy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclope- nta[b]fluorene-1,3-dione 398. (3aS,10R)-2-(2-Azepan-1-yl-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 399. (3aS,10R)-2-[2-(4-Acetyl-piperazin-1-yl)-ethyl]-5-fluoro-10-(3-- hydroxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cy- clopenta[b]fluorene-1,3-dione 400. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-meth- yl-piperazin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 401. (3aS,10R)-2-[2-(3,6-Dihydro-2H-pyridin-1-yl)-ethyl]-5-fluoro-10-(3-hydrox- y-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopen- ta[b]fluorene-1,3-dione 402. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(4-meth- yl-piperidin-1-yl)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 403. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-piperid- in-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 404. (3aS,10R)-2-[2-(2,5-Dihydro-pyrrol-1-yl)-ethyl]-5-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 405. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-pyrroli- din-1-yl-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 406. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(2-methyla- mino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 407. (3aS,10R)-2-(2-Ethylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 408. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-(2-isopropylamino-ethyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 409. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-(2-isobutylamino-ethyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 410. (3aS,10R)-2-[2-(Cyclopropylmethyl-amino)-ethyl]-5-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 411. (3aS,10R)-2-[2-(2,5-Dihydro-pyrrol-1-yl)-ethyl]-5-fluoro-10-(3-hydroxy-ph- enyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 412. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-2-[2-(2-methoxy-ethyla- mino)-ethyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fl- uorene-1,3-dione 413. (3aS,10R)-2-(2-Cyclobutylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-me- thoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 414. (3aS,10R)-2-(2-tert-Butylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-me- thoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 415. (3aS,10R)-2-(2-Allylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-methoxy- -3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-d- ione 416. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(- 2-prop-2-ynylamino-ethyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 417. (3aS,10R)-2-(2-Dimethylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 418. (3aS,10R)-2-[2-(Ethyl-methyl-amino)-ethyl]-5-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 419. (3aS,10R)-5-Fluoro-2-{2-[(2-hydroxy-ethyl)-methyl-amino]-ethyl}-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 420. (3aS,10R)-2-(2-Diethylamino-ethyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-metho- xy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 421. (3aS,10R)-2-{2-[Ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-5-fluoro-10-(3-hydr- oxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 422. (3aS,10R)-2-{2-[Ethyl-(2-methoxy-ethyl)-amino]-ethyl}-5-fluoro-10-(3-hydr- oxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 423. (3aS,10R)-2-[2-(Allyl-methyl-amino)-ethyl]-5-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 424. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(methyl- -prop-2-ynyl-amino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 425. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-[2-(isopropyl-methyl-amino)-et- hyl]-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]- fluorene-1,3-dione 426. (3aS,10R)-2-(2-Cyclobutylamino-ethyl)-7-fluoro-10-(3-hydroxy-phenyl)-6-me- thoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 427. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-methyla- mino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 428. (3aS,10R)-2-(3-Ethylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-methox- y-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-- dione 429. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-(3-isopropylamino-pr- opyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 430. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-(3-isobutylamino-propyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 431. (3aS,10R)-2-[3-(Cyclopropylmethyl-amino)-propyl]-5-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 432. (3aS,10R)-5-Fluoro-2-[3-(2-hydroxy-ethylamino)-propyl]-10-(3-hydroxy-phen- yl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 433. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-2-[3-(2-methoxy-ethyla- mino)-propyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]f- luorene-1,3-dione 434. (3aS,10R)-2-(3-Cyclopropylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-- methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 435. (3aS,10R)-2-(3-Cyclobutylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 436. (3aS,10R)-2-(3-tert-Butylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-m- ethoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 437. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-prop-2-- ynylamino-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluoren- e-1,3-dione 438. (3aS,10R)-2-(3-Dimethylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-met- hoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione 439. (3aS,10R)-5-Fluoro-2-{3-[(2-hydroxy-ethyl)-methyl-amino]-propyl}-10-(3-hy- droxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cycl- openta[b]fluorene-1,3-dione 440. (3aS,10R)-2-(3-Diethylamino-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-meth- oxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,- 3-dione 441. (3aS,10R)-2-{3-[Ethyl-(2-hydroxy-ethyl)-amino]-propyl}-5-fluoro-10-(3-hyd- roxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclo- penta[b]fluorene-1,3-dione 442. (3aS,10R)-2-[3-(Allyl-methyl-amino)-propyl]-5-fluoro-10-(3-hydroxy-phenyl- )-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]flu- orene-1,3-dione 443. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(methyl- -prop-2-ynyl-amino)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta- [b]fluorene-1,3-dione 444. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-2-[3-(isopropyl-methyl-amino)-pr- opyl]-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b- ]fluorene-1,3-dione 445. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-morphol- in-4-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-- 1,3-dione 446. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-(3-pyrroli- din-1-yl-propyl)-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene- -1,3-dione 447. (3aS,10R)-2-[3-(2,5-Dihydro-pyrrol-1-yl)-propyl]-5-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 448. (3aS,10R)-5-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[3-(4-meth- yl-piperazin-1-yl)-propyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 449. (3aS,10R)-2-[3-(4-Acetyl-piperazin-1-yl)-propyl]-5-fluoro-10-(3-hydroxy-p- henyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 450. (3aS,10R)-2-(3-Azepan-1-yl-propyl)-5-fluoro-10-(3-hydroxy-phenyl)-6-metho- xy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3- -dione 451. (3aS,10R)-2-{2-[Ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-7-fluoro-10-(3-hydr- oxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 452. (3aS,10R)-2-[2-(Allyl-methyl-amino)-ethyl]-7-fluoro-10-(3-hydroxy-phenyl)- -6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluo- rene-1,3-dione 453. (3aS,10R)-6-(1,1-Difluoro-methoxy)-2-{3-[(2-hydroxy-ethyl)-methyl-amino]-- propyl}-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaz- a-cyclopenta[b]fluorene-1,3-dione 454. (3aS,10R)-2-{2-[Ethyl-(2-methoxy-ethyl)-amino]-ethyl}-7-fluoro-10-(3-hydr- oxy-phenyl)-6-methoxy-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclop- enta[b]fluorene-1,3-dione 455. (3aS,10R)-7-Fluoro-10-(3-hydroxy-phenyl)-6-methoxy-3a-methyl-2-[2-(methyl- -prop-2-ynyl-amino)-ethyl]-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[- b]fluorene-1,3-dione 490. (3aS,10R)-10-(3-Hydroxy-phenyl)-6-methoxy-2-[3-(2-methoxy-ethylamino)-pro- pyl]-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1- ,3-dione, or a salt thereof. 13. A compound according to claim 1, wherein R1 is 2-(R11)-ethyl or 3-(R11)-propyl; R2 and R3 are both hydrogen; R4 is methyl; R5 is bonded to the 6-position of the scaffold, and is chlorine, bromine, ethoxy, methoxy or difluoromethoxy; and R6 is hydrogen; or a salt, stereoisomer or salt of a stereoisomer thereof. 14. A compound according to claim 1, wherein R1 is 2-(R11)-ethyl; R2 and R3 are both hydrogen; R4 is methyl; R5 is bonded to the 6-position of the scaffold, and is chlorine, ethoxy, methoxy or difluoromethoxy; and R6 is hydrogen; or a salt, stereoisomer or salt of a stereoisomer thereof. 15. A method for treating a disease selected from the group consisting of benign neoplasia and malignant neoplasia, comprising administering to a patient in need thereof an effective amount of a compound according to claim 1. 16. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier, auxiliary and/or excipient. 17. A method for treating a (hyper)proliferative disease and/or disorder responsive to induction of apoptosis selected from the group consisting of tumors; tumors selected from the group consisting of tumors of the breast, bladder, bone, brain, central and peripheral nervous system, colon, endocrine glands, thyroid, adrenal cortex, esophagus, endometrium, germ cells, head and neck, kidney, liver, lung, larynx, hypopharynx, mesothelioma, sarcoma, ovary, pancreas, prostate, rectum, renal, small intestine, soft tissue, testis, stomach, skin, ureter, vagina, and vulva; malignant neoplasia; malignant neoplasia selected from the group consisting of inherited cancers, retinoblastoma, Wilms tumor, primary tumors and secondary tumors; hematological tumors; hematological tumors selected from the group consisting of aggressive forms of leukemia, aggressive forms of lymphoma, indolent forms of leukemia, indolent forms of lymphoma, non-Hodgkins disease, chronic myeloid leukemia, acute myeloid leukemia, acute lymphoblastic leukemia, Hodgkins disease, multiple myeloma and T-cell lymphoma; myelodysplastic syndrome; plasma cell neoplasia; paraneoplastic syndromes; cancers of unknown primary site, and AIDS related malignancies, in a mammal, comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to said mammal in need thereof. 18. A method for treating or ameliorating a (hyper)proliferative disease and/or disorder responsive to induction of apoptosis selected from the group consisting of benign hyperplasia, benign hyperplasia of the prostate and benign hyperplasia of the colon epithelium, in a mammal comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to said mammal in need thereof. 19. A method for modulating Eg5 kinesin activity comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to a mammal in need of said modulation. 20. A combination comprising a first active ingredient, which is at least one compound according to claim 1, and a second active ingredient, which is at least one anti-cancer agent selected from the group consisting of chemotherapeutic anti-cancer agents and target-specific anti-cancer agents. 21. A method for treating or ameliorating a disease selected from the group consisting of benign neoplasia and malignant neoplasia, in a patient, comprising administering separately, simultaneously, concurrently, sequentially or chronologically staggered to said patient in need thereof an amount of a first active compound, which is a compound according to claim 1, and an amount of at least one second active compound, said second active compound being an anti-cancer agent selected from the group consisting of chemotherapeutic anti-cancer agents and target-specific anti-cancer agents, wherein the amounts of the first active compound and said second active compound result in a therapeutic effect. 22. The combination according to claim 20, in which said chemotherapeutic anti-cancer agents are selected from the group consisting of alkylating/carbamylating agents, Cyclophosphamid, Ifosfamid, Thiotepa, Melphalan, chloroethylnitrosourea; platinum derivatives, cis-platin, oxaliplatin, satraplatin, carboplatin; antimitotic agents/tubulin inhibitors, vinca alkaloids, vincristine, vinblastine, vinorelbine, taxanes, Paclitaxel, Docetaxel, analogs and formulations and conjugates of taxanes Abraxane, epothilones, Epothilone B, Azaepothilone, ZK-EPO; topoisomerase inhibitors, anthracyclines, Doxorubicin, epipodophyllotoxines, Etoposide, camptothecin, camptothecin analogs, Irinotecan, Topotecan; pyrimidine antagonists, 5-fluorouracil, Capecitabine, Arabinosylcytosine/Cytarabin, Gemcitabine; purin antagonists, 6-mercaptopurine, 6-thioguanine, fludarabine; folic acid antagonists, methotrexate and pemetrexed. 23. The combination according to claim 20, in which said target-specific anti-cancer agents are selected from the group consisting of kinase inhibitors, Imatinib, ZD-1839/Gefitinib, BAY43-9006/Sorafenib, SU11248/Sunitinib, OSI-774/Erlotinib, Dasatinib, Lapatinib, Vatalanib, Vandetanib, Pazopanib; proteasome inhibitors, PS-341/Bortezomib; histone deacetylase inhibitors, SAHA, PXD101, MS275, MGCD0103, Depsipeptide/FK228, NVP-LBH589, NVP-LAQ824, Valproic acid (VPA), CRA/PCI-24781, ITF2357, SB939, butyrates; heat shock protein 90 inhibitors, 17-allylaminogeldanamycin (17-AAG), 17-dimethylaminogeldanmycin (17-DMAG); vascular targeting agents (VAT), combretastatin A4 phosphate, AVE8062/AC7700, anti-angiogenic drugs, VEGF antibodies, Bevacizumab, KDR tyrosine kinase inhibitors, PTK787/ZK222584 (Vatalanib), Vandetanib, Pazopanib; monoclonal antibodies, Trastuzumab, Rituximab, Alemtuzumab, Tositumomab, Cetuximab, Bevacizumab, Panitumumab, mutants of monoclonal antibodies, conjugates of monoclonal antibodies, Gemtuzumab ozogamicin, Ibritumomab tiuxetan, antibody fragments; oligonucleotide based therapeutics, G-3139/Oblimersen, DNMT1 inhibitor MG98; Toll-like receptor/TLR 9 agonists, CPG-7909, TLR 7 agonists, Imiquimod, Isatoribine, analogues of TLR 7 agonists, TLR 7/8 agonists, Resiquimod, immunostimulatory RNA as TLR 7/8 agonists; protease inhibitors; hormonal therapeutics, anti-estrogens, Tamoxifen, Raloxifen, anti-androgens, Flutamide, Casodex, LHRH analogs, Luprolide, Goserelin, Triptorelin, aromatase inhibitors; bleomycin; retinoids, all-trans retinoic acid (ATRA); DNA methyltransferase inhibitors, 2-deoxycytidine derivative Decitabine, 5-azacytidine; alanosine; cytokines, interleukin-2; interferons, interferon .alpha.2, interferon-.gamma.; death receptor agonists, TRAIL, DR4/5 agonistic antibodies, FasL, TNF-R agonists, TRAIL receptor agonists, mapatumumab and lexatumumab. 24. A method for treating cancer selected from the group consisting of cancer of the breast, bladder, bone, brain, central peripheral nervous system, peripheral nervous system, colon, endocrine glands, esophagus, endometrium, germ cells, head and neck, kidney, liver, lung, larynx, hypopharynx, mesothelioma, sarcoma, ovary, pancreas, prostate, rectum, renal, small intestine, soft tissue, testis, stomach, skin, ureter, vagina, vulva; inherited cancers, retinomblastoma, Wilms tumor; leukemia, lymphoma, non-Hodgkins disease, chronic myeloid leukaemia, acute myeloid leukaemia, acute lymphoblastic leukemia, Hodgkins disease, multiple myeloma, T-cell lymphoma; myelodysplastic syndrome, plasma cell neoplasia, paraneoplastic syndromes, cancers of unknown primary site and AIDS related malignancies, in a mammal, comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to said mammal in need thereof. 25. A method for treating colon cancer in a mammal, comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to said mammal in need thereof. 26. A method for treating cancer of the breast, bladder, bone, brain, central peripheral nervous system, peripheral nervous system, colon, endocrine glands, esophagus, endometrium, germ cells, head and neck, kidney, liver, lung, larynx, hypopharynx, mesothelioma, sarcoma, ovary, pancreas, prostate, rectum, renal, small intestine, soft tissue, testis, stomach, skin, ureter, vagina, or vulva; retinomblastoma, Wilms tumor; leukemia, lymphoma, non-Hodgkins disease, chronic myeloid leukaemia, acute myeloid leukaemia, acute lymphoblastic leukemia, Hodgkins disease, multiple myeloma, or T-cell lymphoma, comprising administering a therapeutically effective and tolerable amount of one or more compounds according to claim 1 to said mammal in need thereof. 27. A compound of formula I according to claim 1, in which R1 is 2-4C-alkenyl, 2-4C-alkinyl or 3-7C-cycloalkyl-1-4C-alkyl, or a salt thereof. 28. A compound of formula I ##STR00969## in which R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11, in which R11 is --N(R111)R112, or halogen, in which R111 is hydrogen, 1-4C-alkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, 1N-(1-4C-alkyl)-pyrazolyl, 1N-(H)-pyrazolyl, isoxazolyl, or completely or partially fluorine-substituted 1-4C-alkyl, R112 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, or 3-7C-cycloalkyl-1-4C-alkyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, S-oxo-thiomorpholin-4-yl, S,S-dioxo-thiomorpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, 2,5-dihydro-pyrrol-1-yl, 1,2,3,6-tetrahydropyridin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, triazol-1-yl, or tetrazol-1-yl, in which R113 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkylcarbonyl, amidino, or completely or partially fluorine-substituted 1-4C-alkyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and 1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy or hydroxyl, R3 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl or 1-4C-alkoxy, R4 is 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R5 is 3-4C-alkyl, halogen, 1-4C-alkoxy, trifluoromethyl, cyano, hydroxyl, phenyl-1-4C-alkoxy, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, and R6 is hydrogen, 1-4C-alkyl or halogen, or a salt thereof. 29. A compound of formula I ##STR00970## in which R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11, in which R11 is --N(R111)R112, or halogen, in which R111 is hydrogen, 1-4C-alkyl, 2-4C-alkenyl, 2-4C-alkinyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, 1N-(1-4C-alkyl)-pyrazolyl, 1N-(H)-pyrazolyl, isoxazolyl, or completely or partially fluorine-substituted 1-4C-alkyl, R112 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, or 3-7C-cycloalkyl-1-4C-alkyl, or R111 and R112 together and with inclusion of the nitrogen atom, to which they are bonded, form a ring Het, in which Het is piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, S-oxo-thiomorpholin-4-yl, S,S-dioxo-thiomorpholin-4-yl, pyrrolidin-1-yl, azetidin-1-yl, homopiperidin-1-yl, 4N-(R113)-piperazin-1-yl, 4N-(R113)-homopiperazin-1-yl, 2,5-dihydro-pyrrol-1-yl, 1,2,3,6-tetrahydropyridin-1-yl, pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, triazol-1-yl, or tetrazol-1-yl, in which R113 is hydrogen, 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkylcarbonyl, amidino, or completely or partially fluorine-substituted 1-4C-alkyl, wherein said Het may be optionally substituted by one or two substituents independently selected from fluorine and 1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy or hydroxyl, R3 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl or 1-4C-alkoxy, R4 is 1-4C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkyl-1-4C-alkyl, R5 is 3-4C-alkyl, halogen, 1-4C-alkoxy, trifluoromethyl, cyano, hydroxyl, phenyl-1-4C-alkoxy, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, and R6 is 1-4C-alkyl or halogen, or a salt thereof. 30. A compound of formula I according to claim 1, in which R5 is 1-4C-alkoxy-2-4C-alkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy. 31. A compound of formula I according to claim 1, in which R5 is 1-4C-alkoxy. 32. A compound of formula I according to claim 1, in which R5 is methoxy. 33. A compound, which is a compound of formulae Ib* or Ic* ##STR00971## in which R2 and R3 are both hydrogen, R4 is methyl or ethyl, and R1 and R5 have any of the following meanings: TABLE-US-00009 R1 R5 methyl --CH.sub.3 2-(dimethylamino)-ethyl --CH.sub.3 3-(dimethylamino)-propyl --CH.sub.3 2-(morpholin-4-yl)-ethyl --CH.sub.3 2-(pyrrolidin-1-yl)-ethyl --CH.sub.3 2-(imidazol-1-yl)-ethyl --CH.sub.3 2-(4-methyl-piperazin-1-yl)-ethyl --CH.sub.3 3-(morpholin-4-yl)-propyl --CH.sub.3 3-(pyrrolidin-1-yl)-propyl --CH.sub.3 3-(imidazol-1-yl)-propyl --CH.sub.3 3-(4-methyl-piperazin-1-yl)-propyl --CH.sub.3 3-amino-propyl --CH.sub.3 2-amino-ethyl --CH.sub.3 2-(methylamino)-ethyl --CH.sub.3 2-(ethylamino)-ethyl --CH.sub.3 2-(azetidin-1-yl)-ethyl --CH.sub.3 2-(4-acetyl-piperazin-1-yl)-ethyl --CH.sub.3 2-(3,3-difluoropyrrolidin-1-yl)-ethyl --CH.sub.3 2-(2-fluoroethylamino)-ethyl --CH.sub.3 2-(2,2-difluoroethylamino)-ethyl --CH.sub.3 2-(2,2,2-trifluoroethylamino)-ethyl --CH.sub.3 2-(isopropylamino)-ethyl --CH.sub.3 2-(isobutylamino)-ethyl --CH.sub.3 2-(N-cyclopropylmethyl-amino)-ethyl --CH.sub.3 2-(cyclopropylamino)-ethyl --CH.sub.3 2-(cyclobutylamino)-ethyl --CH.sub.3 2-(N-ethyl-N-methyl-amino)-ethyl --CH.sub.3 2-(diethylamino)-ethyl --CH.sub.3 2-(N-isopropyl-N-methyl-amino)-ethyl --CH.sub.3 2-((R)-3-fluoro-pyrrolidin-1-yl)-ethyl --CH.sub.3 2-((S)-3-fluoro-pyrrolidin-1-yl)-ethyl --CH.sub.3 2-(4-methyl-piperidin-l-yl)-ethyl --CH.sub.3 3-(methylamino)-propyl --CH.sub.3 3-(ethylamino)-propyl --CH.sub.3 3-(azetidin-1-yl)-propyl --CH.sub.3 3-(4-acetyl-piperazin-1-yl)-propyl --CH.sub.3 3-(3,3-difluoropyrrolidin-1-yl)-propyl --CH.sub.3 3-(2-fluoroethylamino)-propyl --CH.sub.3 3-(2,2-difluoroethylamino)-propyl diploma --CH.sub.3 3-(2,2,2-trifluoroethylamino)-propyl --CH.sub.3 3-(isopropylamino)-propyl --CH.sub.3 3-(isobutylamino)-propyl --CH.sub.3 3-(N-cyclopropylmethyl-amino)-propyl versitale --CH.sub.3 3-(cyclopropylamino)-propyl --CH.sub.3 3-(cyclobutylamino)-propyl --CH.sub.3 3-(N-ethyl-N-methyl-amino)-propyl --CH.sub.3 3-(diethylamino)-propyl --CH.sub.3 3-(N-isopropyl-N-methyl-amino)-propyl --CH.sub.3 3-((R)-3-fluoro-pyrrolidin-1-yl)-propyl --CH.sub.3 3-((S)-3-fluoro-pyrrolidin-1-yl)-propyl --CH.sub.3 3-(4-methyl-piperidin-l-yl)-propyl --CH.sub.3 3-[N-(2-hydroxyethyl)-amino]-propyl --CH.sub.3 3-[N-(2-methoxyethyl)-amino]-propyl --CH.sub.3 3-(tertbutylamino)-propyl --CH.sub.3 3-(allylamino)-propyl --CH.sub.3 3-(propargylamino)-propyl --CH.sub.3 3-(N-allyl-N-methyl-amino)-propyl --CH.sub.3 3-(N-methyl-N-propargyl-amino)-propyl --CH.sub.3 3-[N-(2-hydroxyethyl)-N-methyl-amino]- --CH.sub.3 propyl 3-[N-(2-methoxyethyl)-N-methyl-amino]- --CH.sub.3 propyl 3-[N-ethyl-N-(2-hydroxyethyp-amino]-propyl --CH.sub.3 3-[N-ethyl-N-(2-methoxyethyl)-amino]-propyl --CH.sub.3 3-(piperidin-1-yl)-propyl --CH.sub.3 3-(homopiperidin-1-yl)-propyl --CH.sub.3 3-(2,5-dihydropyrrol-1-yl)-propyl --CH.sub.3 3-(1,2,3,6-tetrahydropyridin-1-yl)-propyl --CH.sub.3 2-[N-(2-hydroxyethyl)-amino]-ethyl --CH.sub.3 2-[N-(2-methoxyethyl)-amino]-ethyl --CH.sub.3 2-(tertbutylamino)-ethyl --CH.sub.3 2-(allylamino)-ethyl --CH.sub.3 2-(propargylamino)-ethyl --CH.sub.3 2-(N-allyl-N-methyl-amino)-ethyl --CH.sub.3 2-(N-methyl-N-propargyl-amino)-ethyl --CH.sub.3 2-[N-(2-hydroxyethyl)-N-methyl-amino]-ethyl --CH.sub.3 2-[N-(2-methoxyethyl)-N-methyl-amino]-ethyl --CH.sub.3 2-[N-ethyl-N-(2-hydroxyethyl)-amino]-ethyl --CH.sub.3 2-[N-ethyl-N-(2-methoxyethyl)-amino]-ethyl --CH.sub.3 2-(piperidin-1-yl)-ethyl --CH.sub.3 2-(homopiperidin-1-yl)-ethyl --CH.sub.3 2-(2,5-dihydropyrrol-1-yl)-ethyl --CH.sub.3 2-(1,2,3,6-tetrahydropyridin-1-yl)-ethyl --CH.sub.3 or a salt thereof.

Details for Patent 8,530,493

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2026-02-22
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2026-02-22
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2026-02-22