Patent ID: 6169090
Filing Date: 2001-01-02
Classification: A61P,C07D

Abstract:
A compound of formula (i) ##STR7## wherein X and Y are independently selected from the group consisting of CH, N and N-oxide, provided that X and Y do not both represent CH and provided that X and Y do not both represent N; Z is CO or CS; R.sub.1 is alkyl, optionally substituted with one or more halogens; R.sub.2 is selected from the group consisting of CF.sub.3, H, CN, C(.dbd.NOR.sub.9)R.sub.6, alkyl-C(.dbd.NOR.sub.9)R.sub.6, S(O).sub.p R.sub.6, SO.sub.2 NR.sub.12 R.sub.13, CONR.sub.12 R.sub.13, OR.sub.9, NR.sub.6 R.sub.15 ; alkyl, cycloalkyl or cycloalkylalkyl optionally substituted with one or more R.sub.8 ; aryl, heteroaryl, arylalkyl or heteroarylalkyl, the aryl/heteroaryl portions of which may be optionally substituted with one or more R.sub.7 or alkyl-R.sub.10 and the alkyl portions of which may be optionally substituted with one or more R.sub.8 ; and heterocyclo or heterocycloalkyl, the heterocyclo portion of which may be optionally substituted with one or more R.sub.11 or alkyl-R.sub.10 and the alkyl portion of which may be optionally substituted with one or more R.sub.8 ; R.sub.3 is selected from the group consisting of H, alkyl and halogen; R.sub.4 is H or alkyl; R.sub.5 is aryl or heteroaryl, optionally substituted at any position with (one or more) substituents alkyl-R.sub.10 or R.sub.7 ; R.sub.6 is selected from the group consisting of alkyl, aryl, heteroaryl, cycloalkyl, cycloalkylalkyl, arylalkyl, heteroarylalkyl, heterocyclo and heterocycloalkyl, the cycloalkyl/alkyl portions of which may be optionally substituted with one or more R.sub.8, the aryl/heteroaryl portions of which may be optionally substituted with one or more R.sub.7 or alkyl-R.sub.10 and the heterocyclo portions of which may be optionally substituted with one or more R.sub.11 or alkyl-R.sub.10 ; R.sub.7 is alkyl or R.sub.17 ; R.sub.8 is carbonyl oxygen (.dbd.O) or R.sub.10 ; R.sub.9 is H or R.sub.6 ; R.sub.10 is selected from the group consisting of CO.sub.2 R.sub.16, CONR.sub.12 R.sub.13, SO.sub.2 NR.sub.12 R.sub.13, OH, OR.sub.12, CN, CF.sub.3, NR.sub.12 R.sub.15, COR.sub.12, S(O).sub.p R.sub.12, NHSO.sub.2 CF.sub.3, and NO.sub.2 ; R.sub.11 is selected from the group consisting of carbonyl oxygen, alkyl and R.sub.10 ; R.sub.12 and R.sub.13 are the same or different and are selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, and heterocycloalkyl or NR.sub.12 R.sub.13 represents a heterocyclic ring, the aryl/heteroaryl portions of which may be optionally substituted with one or more R.sub.18 and the heterocyclo portions of which may be optionally substituted with one or more R.sub.19 ; R.sub.15 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, heterocycloalkyl, alkylcarbonyl, alkoxycarbonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl, alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, and heterocyclosulfonyl, the aryl/heteroaryl portions of which may be optionally substituted with one or more R.sub.18 and the heterocyclo portions of which may be optionally substituted with one or more R.sub.19 ; R.sub.16 is selected from the group consisting of H, alkyl, cycloalkyl, cycloalkylalkyl, arylalkyl, heteroarylalkyl, heterocyclo and heterocycloalkyl; R.sub.17 is halogen or R.sub.10 ; R.sub.18 is selected from the group consisting of alkyl, alkoxy, CF.sub.3, halogen, CN and CO.sub.2 R.sub.16 ; R.sub.19 is selected from the group consisting of alkyl, alkoxy, CF.sub.3, arylalkyl, carbonyl oxygen, CN or CO.sub.2 R.sub.16 ; and p is 0-2; and N-oxides and pharmaceutically-acceptable salts thereof.