Patent ID: 6642223
Filing Date: 2003-11-04
Classification: A61P,C07D

Abstract:
A compound of formula 1:wherein G is a group of the formula: R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxy group, a lower alkanoyloxy group, an amino group having optionally a lower alkyl substituent, a carboxy-substituted lower alkoxy group, a lower alkoxycarbonyl-substituted lower alkoxy group, or an aminocarbonyl-lower alkoxy group having optionally a lower alkyl substituent, R2 is a group of the formula: â€”NR4R5, in which R4 and R5 are the same or different and each a hydrogen atom, a lower alkyl group having optionally a hydroxy substituent, or a benzoyl group having optionally a halogen substituent on the phenyl ring; a hydrogen atom; a hydroxy group; a lower alkoxy group; a carboxy-substituted lower alkyl group; a cyano-substituted lower alkyl group; a tetrazolyl-substituted lower alkyl group; a lower alkanoyloxy-substituted lower alkyl group; a lower alkoxycarbonyl-substituted lower alkyl group; an amino-substituted lower alkanoyloxy group having optionally a lower alkyl substituent; a lower alkoxycarbonyl-substituted lower alkoxy group; a carboxy-substituted lower alkoxy group; a lower alkanoyl group; or a group of the formula: â€”(O)mâ€”Aâ€”(CO)uNR6R7, in which m and u are each 0 or 1, but both m and u are not simultaneously 0, A is a lower alkylene group, R6 and R7 are the same or different and each a hydrogen atom, a lower alkoxy group, a lower alkyl group, an amino-substituted lower alkyl group having optionally a lower alkyl substituent, a carbamoyl-substituted lower alkyl group, an adamantyl-substituted lower alkyl group, a lower alkylsulfonyl group, or a phenyl group having optionally a halogen substituent, or R6 and R7 may bind together with the nitrogen atom to which they bond to form a 5- to 7-membered saturated heterocyclic group with or without being intervened with another nitrogen atom or an oxygen atom, said heterocyclic group being optionally substituted by a lower alkyl group or a phenyl-lower alkyl group, R3 is a hydrogen atom or a hydroxy-substituted lower alkyl group, or R2 and R3 may bind together to form an oxo group, a lower alkylidene group, a lower alkoxy-substituted lower alkylidene group, a lower alkoxycarbonyl-substituted lower alkylidene group, or a phenyl-substituted lower alkylidene group, R is a group of the formula: â€ƒin which p is 1 or 2, R8 is a hydrogen atom, a lower alkyl group, a hydroxy group, an amino group having optionally a lower alkanoyl substituent, a nitro group, a halogen atom or a lower alkoxy group, R2 a lower alkanoyloxy group; a benzoyl group having optionally a lower alkyl substituent on the phenyl group; a cycloalkyl group; a phenyl group having optionally a substituent selected from lower alkyl group, a lower alkoxy group, a phenyl-lower alkoxy group, a hydroxy group, a lower alkanoyloxy group, a halogen-substituted-lower alkoxy group, a nitro group, an amino group having optionally a lower alkanoyl substituent, a phenyl group, and an amino-substituted lower alkoxy group having optionally a lower alkyl substituent; a phenoxy group; a phenyl-lower alkyl group having optionally a lower alkyl substituent on the phenyl ring; a phenyl-lower alkylamino-carbonyl group; an aminosulfonyloxy group having optionally a lower alkyl substituent; or a group of the formula: â€”(A)mâ€”CHR12R13, in which A is the same as defined above, R12 is a hydrogen atom, a hydroxy group or a lower alkanoyloxy group, R13 is a phenyl group having optionally a lower alkyl substituent or a phenyl-lower alkyl group having optionally a lower alkyl substituent on the phenyl ring, and m is 0 or 1, X is a methylene group, or a group of the formula: &boxH;CHâ€”provided that when X is a methylene group, then R is a group of the formula: â€ƒwherein R8 and p are as defined above and R9 is a lower alkanoyloxy group; a benzoyl group having optionally a lower alkyl substituent on the phenyl group; a phenoxy group; a phenyl-lower alkyl group having optionally a lower alkyl substituent on the phenyl ring; a phenyl-lower alkylaminocarbonyl group; an aminosulfonyloxy group having optionally a lower alkyl substituent; or a group of the formula: â€”(A)mâ€”CHR12R13, in which A is the same as defined above, R12 is a hydrogen atom, a hydroxy group or a lower alkanoyloxy group, R13 is a phenyl group having optionally a lower alkyl substituent or a phenyl-lower alkyl group having optionally a lower alkyl substituent on the phenyl ring, and m is 0 or 1, when R1 is a hydrogen atom and R2 is a hydrogen atom, an amino group, a mono-lower alkylamino group or a di-lower alkylamino group, or R2 and R3 may bind together to form an oxo group, then R9 should not be a phenyl group having optionally a substituent selected from a hydroxy group, a lower alkyl group, a lower alkoxy group and a lower alkanoyloxy group on the phenyl ring, or or a pharmaceutically acceptable salt thereof.