Patent ID: 6479497
Filing Date: 2002-11-12
Classification: A61P,C07D

Abstract:
A compound of formula (I) whereinX is N; Y is CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H or C1-C6 alkyl; R3 is (CH2)n-phenyl, wherein the phenyl may be mono- or di-substituted with R4 and/or R5; wherein R4 is selected from the group consisting of a) H, b) C1-C6 alkyl, c) C3-C6 cycloalkyl, d) halogen, e) CN, f) CF3, g) OH, h) C1-C6 alkoxy, i) NR6R7, j) OCF3, k) SO3CH3, l) SO3CF3, m) SO2NR6R7, n) phenyl, o) phenyl-C1-C6 alkyl, p) phenoxy, q) C1-C6 alkylphenyl, r) an optionally substituted 5- or 6-membered heterocyclic ring containing one or two heteroatoms which is (are) N, wherein the substituent(s) is (are) selected from the group consisting of C1-C6 alkyl, C3-C6 cycloalkyl, phenyl-C1-C6 alkyl, (CH2)mOR9 wherein m is 2-6 and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl or phenyl-C1-C6 alkyl, and COR8, s) an optionally substituted 5- or 6-membered heteroaromatic ring containing one or two heteroatoms which is (are) N, wherein the substituent(s) is (are) selected from the group consisting of C1-C6 alkyl, C3C6 cycloalkyl and phenyl-C1-C6 alkyl, and t) COR8; wherein R6 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R7 is H, C1-C6 alkyl or C3-C6 cycloalkyl; and R8 is C1-C6 alkyl, C3-C6 cycloalkyl, CF3, NR6R7 or phenyl; R5 is selected from the group consisting of H, OH, CF3, OCF3, halogen, C1-C6 alkyl and C1-C6 alkoxy; and n is 0-4; wherein the compound is an (R)-enantiomer, an (S)-enantiomer, or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof.