Patent ID: 6229011
Filing Date: 2001-05-08
Classification: C07C,C07D

Abstract:
A compound of the formula: ##STR275##wherein:Z is hydrogen or lower alkyl, one of X and X' is hydrogen, halogen, or lower alkyl, the other is a group of the formula: ##STR276##wherein:R.sub.1 is hydrogen or lower alkyl,R.sub.15 is halogen, nitro, lower alkyl sulfonyl, cyano, lower alkyl, OH, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkyl aminosulfonyl, perfluorolower alkyl, lower alkylthio, hydroxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, alkylthio lower alkyl, alkylsulfinyl lower alkyl, alkylsufonyl lower alkyl, lower alkylsulfinyl, lower alkanoyl, aroy, aryloxy or a group of the formula R.sub.17 --C.tbd.C--,R.sub.16 is hydrogen, halogen, nitro, cyano, lower alkyl, OH, perfluoro lower alkyl, or lower alkylthio,R.sub.17 hydrogen, aryl, heteroaryl, or lower alkyl which is unsubstituted or substituted by OH, aryl, or heteroaryl; anda is 0 or 1;or one of X and X' is a group of the formula: ##STR277##whereinHet is a 5- or 6-membered heteroaromatic ring wherein the heteroatoms of such ring consist of 1, 2, or 3 heteroatoms selected from N, O, and S; orHet is a 9- or 10-membered bicyclic heteroaromatic ring wherein the heteroatoms of such ring consist of 1, 2, 3 or 4 heteroatoms selected from O, S, and N,a, R.sub.1, R.sub.15 and R.sub.16 are as above, andR.sub.30 is hydrogen or lower alkyl, or is absent;or one of X and X' is a group of the formula: ##STR278##wherein:R.sub.18 is hydrogen, lower alkyl, aryl, heteroaryl, arylalkyl, heteroaryl alkyl,R.sub.19 is lower alkyl, which is unsubstituted or substituted by one or more halogen, hydroxy, lower alkoxy, aryl, hetereoaryl, alkylthio, or R.sub.19 is aryl or heteroaryl, andR.sub.20 is lower alkyl or lower alkanoyl, orR.sub.19 and R.sub.20 taken together are tetramethylene; andY is a group of the formula: ##STR279##wherein:R.sub.22 and R.sub.23 are independently hydrogen, lower alkyl, lower alkoxy, lower alkoxylalkyl, lower alkylamino, aryl, arylalkyl, nitro, cyano, lower alkylthio, lower alkylsulfinyl, lower alkyl sulfonyl, lower alkanoyl, halogen, or perfluoro lower alkyl and at least one of R.sub.22 and R.sub.23 is other than hydrogen, andR.sub.24 is hydrogen, hydroxy, lower alkyl, lower alkoxy, amino, aryl, nitro, cyano, lower alkyl sulfonyl, halogen, or is a group of the formula: ##STR280##whereinR.sub.25 is hydrogen, lower alkyl, aryl, aryl lower alkyl, alkoxy lower alkyl and R.sub.26 is hydrogen or lower alkyl, orR.sub.22 and R.sub.24 taken together are a fused benzene ring; orY is a group Y-2 which is a five or six membered monocyclic heteroaromatic group wherein the heteroatoms of such group consist of 1, 2 or 3 heteroatoms selected from N, O, and S, or a 9- or 10-membered bicyclic heteroaromatic group wherein the heteroatoms of such group consist of 1, 2, 3 or 4 heteroatoms selected from O, S, and N, wherein said heteroaromatic group is bonded via a carbon atom to the amide carbonyl and one or two carbon atoms of said heteoaromatic group are substituted by lower alkyl, halogen, cyano, perfluoroalkyl, or aryl and at least one of said substituted carbon atoms is adjacent to the carbon atom bonded to the amide carbonyl;or the pharmaceutically acceptable salts or esters thereof.