Benzoheterocyclic derivatives

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:
• —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:
• —(O)m—A—(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:
• in 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:
• —(A)m—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:
• ═CH—
• provided that when X is a methylene group, then R is a group of the formula:
• wherein 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:
• —(A)m—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.