Patent ID: 6444687
Filing Date: 2002-09-03
Classification: A61P,C07D

Abstract:
A compound having the structural formula or a pharmaceutically acceptable salt, solvate or N-oxide thereof, whereinX is &boxH;CHâ€” or &boxH;Nâ€”; Y is 1 to 3 substituents independently selected from the group consisting of H, halogen, trihaloalkyl, C1-C6 alkyl, C1-C6 alkenyl, C3-C7-cycloalkyl, C1-C6 alkyl substituted by C3-C7-cycloalkyl, â€”OH, â€”O(C1-C6)alkyl, â€”SH, â€”S(C1-C6)alkyl, or â€”CN; R is R4 is hydrogen or C1-C6 alkyl; R5 is C1-C6 alkyl, aryl or heteroaryl; provided R4 and R5 are not both C1-C6 alkyl, and provided that when R4 is hydrogen, R5 is not C1-C6 alkyl; or R4 and R5 together are C3-C6 alkylene and together with the nitrogen to which they are attached form a 4-7 membered ring; or R4 and R5, together with the nitrogen to which they are attached, form a 5, 6 or 7-membered ring, wherein 1 or 2 ring members are independently selected from the group consisting of â€”Oâ€”, â€”Sâ€” and â€”NR12â€”; R7 is C1-C6 alkyl, C3-C7 cycloalkyl, benzyl, aryl, or heteroaryl; R8 is hydrogen, C1-C6 alkyl, â€”C(O)â€”(C1-C6 alkyl), â€”C(O)â€”(C3-C7 cycloalkyl), â€”C(O)-aryl, â€”C(O)-heteroaryl, â€”SO2â€”R7, aryl, heteroaryl, â€”CONR4R5 or â€”C(O)â€”Oâ€”(C1-C6)alkyl; R9 is 1 to 3 substituents independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, halogeno and â€”CF3; and R12 is hydrogen, C1-C6 alkyl, â€”C(O)â€”(C1-C6 alkyl), â€”SO2â€”R7, R9-phenyl, â€”CONR4R5, â€”C(O)â€”Oâ€”(C1-C6)alkyl, â€”CHO, C3-C7 cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, benzyl, benzoyl, â€”C(O)(C3-C7)cycloalkyl, â€”C(O)(C1-C6)alkylphenyl, pyridylmethyl, â€”C(O)pyridyl, â€”C(O)N(di-(C1-C6)-alkyl) or 4-tetrahydropyranyl.