Patent ID: 6498159
Filing Date: 2002-12-24
Classification: A61P,C07D

Abstract:
A phthalazine compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a hydroxyl group, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; l is an integer of 1 to 3;X represents a cyano group, a nitro group, a halogen atom, a thiocarbamoyl group, a hydroxyimino group which may be substituted with a C1 to C4 alkyl group, a phenyl C1 to C4 alkyl group or a carboxy C1 to C4 alkyl group, or a heteroaryl group selected from the group consisting of pyrrole, pyrazole, imidazole, triazole, tetrazole, thiazole, isothiazole, thiadiazole, pyridine, pyrimidine, and triazine, said heteroaryl group optionally substituted with 1 to 3 substituents selected from the group consisting of C1 to C4 alkyl group which may be substituted with a halogen atom, a cyano group, a nitro group or a hydroxyl group; a C1 to C4 alkoxy group which may be substituted with a halogen atom, a cyano group, a nitro group or a hydroxyl group; a cyano group; a nitro group; a carboxyl group which may have a protective group which can be degraded by any means in vivo to form a carboxylic acid; a hydroxyl group which may have a protective group which can be degraded by any means in vivo to form a hydroxyl group; a carbamoyl group which may be substituted with a lower alkyl group; a halogen atom; and an amino group which may be substituted with a C1 to C4 acyl group, a C1 to C4 alkylsulfonyl group or a phenylsulfonyl group; Y represents: i) a group represented by the formula (III): â€ƒwherein ring B represents a 5- to 6-memberred amine ring which may have a double bond, and n and p are the same as or different from each other and represent an integer of 0 or 1 to 3; or ii) a group represented by the formula (IV): â€ƒwherein ring G represents a 5- to 6-memberred amine ring which may have a double bond, E represents a hydroxyl group, a halogen atom, a C1 to C4 alkyl group or a C1 to C4 alkoxy group, J is represented by the formula â€”(CHR4)qâ€”Q wherein R4 represents a hydrogen atom or a C1 to C4 alkyl group, Q represents a hydroxyl group, a halogen atom, a carboxyl group which may have a protective group which can be degraded by any means in vivo to form a carboxyl group, a carbamoyl group or an azolyl group not containing a heteroatom other than a nitrogen atom, q is an integer of 0 or 1 to 4; or E and J may form a 3- to 6-memberred ring together with the carbon atom to which they are bound, and the ring optionally having an oxygen or nitrogen atom and optionally having a substituent group selected from the group consisting of hydroxyl group, carboxyl group which may have a protective group which can be degraded by any means in vivo to form a carboxyl group, C1-C4 alkyl group, C1-C4 alkyl group substituted with a hydroxyl group, oxo group, and halogen group; provided that the following compounds are excluded: the compound wherein l is 1, E and Q are hydroxyl groups, and q is 0; the compound where l is 1, ring B is a 5- or 6-memberred amine ring, and both n and p are 0; and the compound wherein l is 1, q is 0, and E is a C1 to C2 alkyl group and Q is a hydroxyl group.