Patent ID: 6313118
Filing Date: 2001-11-06
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula I ##STR67##whereinX is N;Y is NR.sub.2 CH.sub.2, CH.sub.2 --NR.sub.2, NR.sub.2 --CO, CO--NR.sub.2 or NR.sub.2 SO.sub.2wherein R.sub.2 is H or C.sub.1 -C.sub.6 alkyl;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or (CH.sub.2).sub.n -aromatic ring,wherein the aromatic ring is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from the group consisting of N, O and S and wherein the aromatic ring may be mono- or di-substituted with R.sub.4 and/or R.sub.5 ;wherein R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halogen, CN, CF.sub.3, OH, C.sub.1 -C.sub.6 alkoxy, NR.sub.6 R.sub.7, OCF.sub.3, SO.sub.3 CH.sub.3, SO.sub.3 CF.sub.3, SO.sub.2 NR.sub.6 R.sub.7, phenyl, phenyl-C.sub.1 -C.sub.6 alkyl, phenoxy, C.sub.1 -C.sub.6 alkyl phenyl, an optionally substituted heterocyclic ring containing one or two heteroatoms selected from the group consisting of N, O, S, SO and SO.sub.2 wherein the substituent(s) is(are) selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl and phenyl-C.sub.1 -C.sub.6 alkyl, an optionally substituted heteroaromatic ring containing one or two heteroatoms selected from the group consisting of N, O and S wherein the substituent(s) is(are) selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl and phenyl-C.sub.1 -C.sub.6 alkyl, or COR.sub.8 ;wherein R.sub.6 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl; R.sub.7 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl; and R.sub.8 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, CF.sub.3, NR.sub.6 R.sub.7, phenyl, a heteroaromatic ring containing one or two heteroatoms selected from the group consisting of N, O and S, or a heterocyclic ring containing one or two heteroatoms selected from the group consisting of N, O, S, SO and SO.sub.2 ;wherein R.sub.5 is H, OH, CF.sub.3, OCF.sub.3, halogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;n is 0-4;R.sub.9 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, OCF.sub.3, OCHF.sub.2, OCH.sub.2 F, halogen, CN, CF.sub.3, OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, NR.sub.6 R.sub.7, Sa.sub.3 CH.sub.3, SO.sub.3 CF.sub.3, SO.sub.2 NR.sub.6 R.sub.7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from the group consisting of N, O and S, wherein the substituent(s) is(are) C.sub.1 -C.sub.6 alkyl; or COR.sub.8 ; wherein R.sub.6, R.sub.7 and R.sub.8 are as defined above,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.