Patent ID: 6469021
Filing Date: 2002-10-22
Classification: A61P,C07D

Abstract:
A compound of formula: wherein:R1 is a phenyl or pyridyl group optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxyl, nitro, trifluoromethyl, cyano, C1-C6 alkyl, C2-C6 alkenyl, and C1-C6 alkoxy groups; R2 is: â€ƒwhere Râ€² is: hydrogen; a hydroxy group; â€”OR5, where R5 is a C1-C6 alkyl or C2-C6 alkenyl group optionally substituted with a hydroxy group or an amino, C1-C6 alkoxy, cycloalkyl, thioether, heterocycloalkyl, aryl, or heteroaryl group optionally substituted with one or more substituents independently selected from the group consisting of alkyl, hydroxyalkyl, carboxyl, C1-C6 alkoxycarbonyl, oxygen, halogen, and trifluoromethyl groups; or â€”NR6R7, where R6 and R7 are each independently hydrogen or a C1-C6 alkyl, C2-C6 alkenyl, amino, or imino group optionally substituted with a hydroxy group, a C1-C6 alkoxy group, or an amino, thioether, heterocycloalkyl, aryl, or heteroaryl group optionally substituted with one or more substituents independently selected from the group consisting of oxygen, halogen, trifluoromethyl, and carboxyl groups, or where â€”NR6R7 forms a 5- or 6-membered heterocyclic ring optionally containing, in addition to the nitrogen heteroatom, a heteroatom selected from the group consisting of O, N, and S; â€”(CH2)nâ€”Oâ€”Râ€³, where n is 1 or 2, and Râ€³ is hydrogen, a C5-C7heteroaryl group, or â€ƒwhere R8 is hydrogen, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, or a 5- or 6-membered heteroaryl group optionally substituted with one or more substituents independently selected from the group consisting of halogens, methyl, and trifluoromethyl; â€”(CH2)pâ€”N(Râ€³)(Râ€²â€³), where p is 1 or 2, Râ€³ is as defined above, and Râ€²â€³ is hydrogen or an alkyl or alkoxy group optionally substituted with a C3-C6 cycloalkyl group optionally substituted with cyano; â€”CH=Nâ€”Râ€³â€³, where Râ€³â€³ is hydrogen, a hydroxy group, or â€”OR9, where R9 is an alkyl, cycloalkyl, aryl, or heteroaryl group; or a 5- or 6-membered heterocyclic ring containing one to three heteroatoms independently selected from the group consisting of O, N, and S, the ring being optionally substituted with one or two substituents independently selected from the group consisting of methyl, methoxymethyl, oxygen, and C1-C6 alkoxy groups; R3 is hydrogen or a C1-C6 alkyl, C2-C6 alkenyl, or (C1-C3 alkoxy)C1-C3 alkyl group; or R2 and R3 together with the atoms to which they are bound form a 5- or 6-membered ring containing one or two heteroatoms selected from the group consisting of O, N, and S, the ring being optionally substituted with oxygen, hydroxyl, or a C1-C6 alkyl group optionally substituted with a 5- or 6-membered heterocycloalkyl containing one or two heteroatoms independently selected from the group consisting of O, N, and S; and R4 is hydrogen or an amino, halogen, hydroxyl, nitro, trifluoromethyl, cyano, C1-C6 alkyl, or C2-C6 alkenyl group: where when R1 is an unsubstituted phenyl, R2 is â€ƒR3 is H, and R4 is H, R5 is not an ethyl group; pharmaceutically acceptable salt or pharmaceutically acceptable solvate of said compound.