Patent ID: 6469003
Filing Date: 2002-10-22
Classification: C07D

Abstract:
A pyridazinone derivative represented by formula (I): {whereinR1 represents a phenyl group, a substituted phenyl group having 1 to 5 substituents, which substitute the hydrogen atom(s) on the ring and are the same or different, selected from a (C1-C8)alkyl group, a halo (C1-C8)alkyl group, a (C1-C8)alkoxy group, a halo (C1-C8)alkoxy group, a (C1-C8)alkylthio group, a (C1-C8)alkoxycarbonyl group, a carbamoyl group, a cyano group, a nitro group, a halogen atom, a carboxyl group, a hydroxyl group, an amino group, an amino group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic amino group which contains a nitrogen atom, an oxygen atom or a sulfur atom selected from a pyrrolidino group, a piperidino group, a piperazino group, an N-methylpiperazino group, an N-phenylpiperazino group, a morpholino group, a thiomorpholino group, a hexamethyleneimino group, or a 3,3,5-trimethylhexahydroazepino group, an aminocarbonyl group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic aminocarbonyl group, a (C1-C8)alkylcarbonylamino group, a (C1-C8)alkoxycarbonylamino group, a hydroxyamino group, an N-acetylhydroxyamino group, an acetoxyamino group, a methylenedioxy group, an ethylenedioxy group, a (C1-C8)alkylsulfonylamino group, a phenylcarbonylamino group, a phenylcarbonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a cyano group, a nitro group or a halogen atom on the ring, an aromatic heterocyclic-carbonylamino group, an aromatic heterocyclic-carbonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a cyano group, a nitro group or a halogen atom on the ring, a phenylsulfonylamino group, a phenylsulfonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a cyano group, a nitro group or a halogen atom on the ring, an aromatic heterocyclic-sulfonylamino group, an aromatic heterocyclic-sulfonylamino group having 1 to 5 substituents which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, cyano group, nitro group or a halogen atom on the ring, an aromatic heterocyclic group or a substituted aromatic heterocyclic group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkylthio group, a (C1-C8)alkoxycarbonyl group, a carboxyl group, a carbamoyl group, a cyano group, a nitro group or a halogen atom; R2 represents a (C1-C8)alkyl group, a substituted (C1-C8)alkyl group having one or more substituents, which are the same or different, selected from a halogen atom, a hydroxyl group, a (C1-C8)alkoxy group, a (C1-C8)alkylthio group, a (C1-C8)alkoxycarbonyl group, a carboxyl group, a cyano group, a nitro group, an amino-group, a hydroxyamino group, an amino group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic amino group having the same meaning as described above, a (C1-C8)alkylcarbonylamino group, a carbamoyl group, an aminocarbonyl group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic aminocarbonyl group, a (C1-C8)alkylsulfonylamino group, a phenylcarbonylamino group, a phenylcarbonylamino having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkoxycarbonyl group, a cyano group, a nitro group or a halogen atom on the ring, an aromatic heterocyclic-carbonylamino group, an aromatic heterocyclic-carbonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkoxycarbonyl group, a cyano group, a nitro group or a halogen atom on the ring, a phenylsulfonylamino group, a phenylsulfonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkoxycarbonyl group, a cyano group, a nitro group or a halogen atom on the ring, an aromatic heterocyclic-sulfonylamino group, an aromatic heterocyclic-sulfonylamino group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkoxycarbonyl group, a cyano group, a nitro group or a halogen atom on the ring, a phenyl group, a substituted phenyl group having the same meaning as described above, an aralkyl group, a substituted aralkyl group having an aryl ring or aromatic heterocycle substituted with 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkoxycarbonyl group, a carboxyl group, a cyano group, a nitro group or a halogen atom, an aromatic heterocyclic group, a substituted aromatic heterocyclic group having the same meaning as described above, an amino group, an amino group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic amino group having the same meaning as described above, a cyano group, a carboxyl group, a (C1-C8)alkoxycarbonyl group, a carbamoyl group, a thiocarbamoyl group, an aminocarbonyl group, an aminocarbonyl group substituted with one or two (C1-C8)alkyl groups or substituted (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic aminocarbonyl group, a phenylaminocarbonyl group, a substituted phenylaminocarbonyl group wherein the aminocarbonyl group is substituted with a phenyl group having the same meaning as the above-described substituted phenyl group, an aromatic heterocyle-aminocarbonyl group or a substituted aromatic heterocyle-aminocarbonyl group wherein the aminocarbonyl group is substituted with an aromatic heterocyclic group having 1 to 5 substituents, which are the same or different, selected from a (C1-C8)alkyl group, a (C1-C8)alkoxy group, a (C1-C8)alkylthio group, a (C1-C8)alkoxycarbonyl group, a carboxyl group, a carbamoyl group, a cyano group, a nitro group or a halogen atom; R3 represents a hydrogen atom, a (C1-C8)alkyl group, a substituted (C1-C8)alkyl group having the same meaning as described above, a phenyl group, a substituted phenyl group having the same meaning as described above, an aromatic heterocyclic group or a substituted aromatic heterocyclic group having the same meaning as described above; R4 represents a cyano group, â€ƒ(wherein R5 represents a hydrogen atom, a (C1-C8)alkyl group, a substituted (C1-C8)alkyl group having the same meaning as described above, a (C1-C8)alkoxy group, a hydroxyl group, amino group, an amino group substituted with one or two (C1-C8)alkyl groups which are the same or different, a 4- to 10-membered cyclic amino group having the same meaning as described above, phenyl group, a substituted phenyl group having the same meaning as described above, an aromatic heterocyclic group or a substituted aromatic heterocyclic group having the same meaning as described above, or R5 may form (CR72)m (wherein R7 are the same or different and represents hydrogen atom, a (C1-C8)alkyl group, a substituted (C1-C8)alkyl group having the same meaning as described above, a phenyl group, a substituted phenyl group having the same meaning as described above, an aromatic heterocyclic group or a substituted aromatic heterocyclic group having the same meaning as described above, and m represents an integer of 2 to 7) together with R3 to form a ring; and Y represents NH, O or S) â€ƒ(wherein R6 represents a hydrogen atom, a (C1-C8)alkyl group, a substituted (C1-C8)alkyl group having the same meaning as described above, a phenyl group, a substituted phenyl group having the same meaning as described above, an aromatic heterocyclic group or a substituted aromatic heterocyclic group having the same meaning as described above, or R6 may form (CR72)m (wherein R7 and m have the same meanings as described above) together with R3 to form a ring; and R8 represents a hydrogen atom or a (C1-C8)alkylcarbonyl group), or â€ƒ(wherein R6 has the same meaning as described above; and R9 and R10 are the same or different and represent a (C1-C8)alkyl group or a substituted (C1-C8)alkyl group having the same meaning as described above, or R9 and R10 together form a (C2-C4)alkylene chain and may form a ring together with the atoms attached thereto); and X represents a single bond, O or S(O)n (wherein n represents an integer of 0, 1 or 2)}, or a pharmaceutically acceptable salt thereof.