Patent ID: 6348466
Filing Date: 2002-02-19
Classification: A61P,C07D

Abstract:
A compound having the following structure: and stereoisomers and pharmaceutically acceptable salts thereof,wherein:n is 1; m is 0, 1, 2 or 3; X is N or CRâ€²; R is an optional substituent which, at each occurrence, is independently C1-6alkyl, C3-6alkenyl, C1-6alkylidenyl or ArC1-6alkyl; Râ€² is hydrogen, halogen or C1-6 alkyl; R1 is â€”C(H)0,1(R3)(R4); R2 is hydrogen or C1-6alkyl; R3 is hydrogen, keto, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, or C1-6alkyloxyC1-6alkyl, and R4 is hydrogen, Ar1, Ar1C1-6alkyl, OAr1, C1-8alkyl, C1-6alkyloxy, C3-6cycloalkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6alkenyl, C3-6alkynyl, C1-6alkyloxyC1-6alkyl, C1-6alkoxyAr1, hydroxyC1-6alkyl, thienylC1-6alkyl, furanylC1-6alkyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, amino, (C1-6alkyl)amino, di(C1-6alkyl)amino, (C1-6alkylAr1)amino, (C1-6alkyl)(Ar1)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, sulfonyl(C1-8alkyl), C(&boxH;O)C1-6alkyl, C1-8alkyl substituted with phthalimide, Ar1, OAr1, NHAr1, C(&boxH;O)Ar1, C(&boxH;O)NHAr1 or â€”C(&boxH;O)NH2, or a radical of the formula â€”(C1-6alkanediyl)-Yâ€”(CO)0,1â€”Ar1 where Y is O, NH or a direct bond, or R3 and R4 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl, a C5-8cycloalkenyl, a C3-12heterocycle, phenyl, naphthyl, or a C5-8cycloalkyl fused to Ar1, each of which being optionally substituted with one or more substituents independently selected from C1-6alkyl; Ar is phenyl, naphthyl or an aromatic C3-12heterocycle, each being optionally substituted with 1, 2 or 3 substituents independently selected from halo, C1-6alkyl, trifluoromethyl, O(trifluoromethyl), hydroxy, cyano, C1-6alkyloxy, phenyoxy, benzoxy, C1-6alkylthio, nitro, amino, mono- or di(C1-6alkyl)amino, (C1-6alkyl) (C1-6alkanoyl)amino, or piperidinyl, or wherein two substituents taken together are a C1-6alkylidinyl or a C6alkylidenyl having one, two or three carbon atoms replaced with a heteroatom individually selected from oxygen, nitrogen or and sulfur; and Ar1 is phenyl, naphthyl or an aromatic C3-12heterocycle, each of which being optionally substituted with 1, 2 or 3 substituents independently selected from halo, C1-6alkyl, C1-6alkyloxy, di(C1-6alkyl)amino, di(C1-6alkyl)aminoC1-6alkyl, trifluoromethyl, sulfonyl(C1-6alkyl) and C1-6alkyl substituted with morpholinyl.