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Details for Patent: 7,220,736

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Details for Patent: 7,220,736

Title:Pyrimidine compounds
Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, ##STR00001## wherein X is .dbd.CH-- or .dbd.N--, Y is --NH--, --NR.sup.4--, --S--, --O--, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.dbd.CH--, etc., R.sup.1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R.sup.2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R.sup.3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R.sup.3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
Inventor(s): Yamada; Koichiro (Saitama-ken, JP), Matsuki; Kenji (Saitama-ken, JP), Omori; Kenji (Saitama, JP), Kikkawa; Kohei (Kawaguchi, JP)
Assignee: Tanabe Seiyaku Co., Ltd. (Osaka, JP)
Filing Date:Mar 15, 2001
Application Number:10/258,545
Claims:1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, ##STR00734## wherein X is .dbd.N--, Y is --N.dbd.CH--, R.sup.1 is (1) a lower alkoxy group which is optionally substituted by one to three, same or different, substituents selected from the group consisting of a cyclo lower alkyl group, a hydroxy group, a lower alkylamino group which is optionally protected, a lower alkoxy group, a hydroxy-substituted lower alkyl group, a phenyl group, a lower alkoxyphenyl group, a hydroxy-substituted lower alkylphenyl group, a furyl group, a pyridyl group, a lower alkoxypyridyl group, a hydroxy-substituted lower alkylpyridyl group, a lower alkylpyridyl group, a pyrimidinyl group, a lower alkoxypyrimidinyl group, or a morpholinyl group, (2) a lower alkylamino group which is optionally substituted by one to three, same or different, substituents selected from the group consisting of a hydroxy group, a lower alkoxy group, a lower alkyl group, a pyridyl group, a lower alkylamino group, a cyano group, a phenyl group which is optionally substituted by a lower alkoxy group and/or a halogen atom, or a hydroxy-substituted lower alkyl group, (3) an indanylamino group, (4) a hydroxy group which is optionally substituted by a pyridyl group, or (5) a cyano group, R.sup.2 is (1) a lower alkylamino group substituted by an aryl group which is optionally substituted by one to four, same or different, substituents selected from the group consisting of a lower alkoxy group, a halogen atom, an amino group, a lower alkanoylamino group, a formylamino group, a hydroxy group, a lower alkoxypyridyl group, a lower alkylamino group, a nitro group, a halogeno-substituted lower alkyl group, a lower alkylenedioxy group, a cyano group, a lower alkyl group substituted by a hydroxy group which is optionally protected, a lower alkylsulfonyl group, or a lower alkylsulfinyl group, (2) a lower alkoxy group substituted by one to four, same or different, substituents selected from the group consisting of a lower alkoxy group or a halogen atom, (3) a lower alkoxy group substituted by a pyridyl group, (4) a lower alkylamino group substituted by an indolyl group, a pyrimidinyl group, a benzofuranyl group, a dihydrobenzofuranyl group, a lower alkylpyrimidinyl group, a dihydrobenzoxazolyl or a dihydrobenzimidazolyl group, or (5) an indanylamino group, and R.sup.3 is (1) an aryl group which is optionally substituted by one to four, same or different, substituents selected from the group consisting of a lower alkoxy group and an lower alkylamino group, or an aryl group which is optionally substituted by one or two lower alkylenedioxy groups, (2) a heterocyclic ring containing N atom(s) which is optionally substituted by one to four, same or different, substituents selected from the group consisting of a lower alkyl group, a hydroxy group, an amino group, a chlorosulfinyloxy group and a piperidinyloxysulfinyloxy group, (3) a lower alkyl group which is optionally substituted by one to three, same or different, substituents selected from the group consisting of a morpholinyl group and a di-lower alkoxyphosphoryl group, (4) a lower alkoxy group which is optionally substituted by one to three, same or different, substituents selected from the group consisting of a pyridyl group, a lower alkoxypyridyl group, a pyrimidinyl group, a lower alkylamino group, a pyrazinyl group, a lower alkoxy group which is optionally substituted by a phenyl group, a pyrimidinyl-substituted oxy group, a pyridyl-substituted oxy group, a pyrimidinyl-substituted lower alkoxy group, a morpholinyl group, a lower alkylmorpholinyl group, a N-lower alkyl-N-pyrimidinylamino group, a lower alkyldioxolanyl group, a lower alkoxy-substituted lower alkoxy group, a pyridylcarbonylamino group, a hydroxy group, and a lower alkylpiperidyl group, (5) a cyclo lower alkoxy group which is optionally substituted by a hydroxy group, or (6) a piperidyl-substituted hydroxy group which is optionally substituted by one to four, same or different, substituents selected from the group consisting of a pyrimidinyl group, a lower alkyl group and a cyano-substituted lower alkyl group.

2. The compound claimed in claim 1, wherein an aryl group on R.sup.2 or R.sup.3 is a monocyclic, bicyclic or tricyclic 6 14 membered aryl group which may be partially saturated, or a heterocyclic ring containing N atom(s) on R.sup.3 is a monocyclic or bicyclic 5 to 14 membered heterocyclic containing N atom(s).

3. The compound claimed in claim 2, wherein the monocyclic, bicyclic or tricyclic 6 14 membered aryl group which may be partially saturated on R.sup.2 or R.sup.3 is phenyl, naphthyl, indenyl or indanyl.

4. The compound claimed in claim 2, wherein the monocyclic or bicyclic 5 to 14 membered heterocyclic ring containing N atom(s) on R.sup.3 is pyridyl, pyrimidinyl, imidazolyl, piperidyl, pyrazolyl, morpholinyl, piperazinyl, pyrrolidinyl, dihydroisoindolyl, tetrahydroimidazo[1,2-a]pyrazyl, tetrahydroisoquinolyl, dihydro-5H-pyrrolo[3,4-b]pyridyl, naphthylidinyl, pyrazo[3,4-d]pyridyl, tetrahydropyridyl, oxazolo[4,5-c]pyridyl, octahydropyrido[3,4-d]pyrimidinyl, thiazolo[4,5-d]pyridyl, imidazo[4,5-d]pyridyl, perhydrodiazepinyl, perhydropiperadino[3,4-c]piperadinyl, tetrahydroisoxazolo[4,5-c]pyridyl, hexahydropyrazolo[4,3-c]pyridyl, dihydropyridyl, tetrahydroxazolo[5,4-c]pyridyl, hexahydropyrido[3,4-d]pyrimidinyl, octahydropyrido[4,3-d]pyrimidinyl, tetrahydrothiazolo[5,4-c]pyridyl, imidazo[4,5-b]pyridyl, homopiperazinyl, perhydropyrazino[1,2-a]pyrazinyl, tetrahydropyrido[4,3-d]pyrimidinyl, tetrahydrothieno[3,2-c]pyridyl, or tetrahydronaphthylidinyl.

5. A pharmaceutical composition containing a compound claimed in claim 1, or its pharmacologically acceptable salt as an active ingredient.

6. A method for treating erectile dysfunction, comprising administering to a patient in need thereof an effective amount of a compound claimed in claim 1, or its pharmacologically acceptable salt.

7. A method for treating pulmonary hypertension, comprising administering to a patient in need thereof an effective amount of a compound claimed in claim 1, or its pharmacologically acceptable salt.

8. A method for treating diabetic gastroparesis comprising administering to a patient in need thereof an effective amount of a compound claimed in claim 1, or its pharmacologically acceptable salt.
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