Patent ID: 6291450
Filing Date: 2001-09-18
Classification: A61P,C07D

Abstract:
A compound of formula ##STR19##or a pharmaceutically acceptable salt thereof, whereinR.sup.1 is (1) an alkyl, alkenyl, alkynyl, cycloalkyl or heterocyclyl radical optionally substituted by 1-3 radicals of --OH, --OR.sup.3, --SR.sup.3, --S(O)R.sup.3, --S(O).sub.2 R.sup.3, --C(O)R.sup.3, --NR.sup.3 R.sup.4 aryl, heteroaryl, cycloalkyl or heterocyclyl; or (2) an aryl radical optionally substituted by an optionally substituted monocyclic heteroaryl or heterocyclyl radical of 5-6 ring members which is optionally substituted by a phenyl radical or monocyclic heteroaryl radical of 5-6 ring members; or (3) a heteroaryl radical optionally substituted by an optionally substituted phenyl or a monocyclic heteroaryl or heterocyclyl radical of 5-6 ring members which is optionally substituted by a phenyl radical or monocyclic heteroaryl radical of 5-6 ring members; wherein the phenyl, aryl, heteroaryl, cycloalkyl and heterocyclyl radicals of (1), (2) and (3) are optionally substituted by 1-3 radicals of hydroxy, --OR.sup.3, --SR.sup.3, --S(O)R.sup.3, --S(O).sub.2 R.sup.3, --C(O)R.sup.3, --NR.sup.3 R.sup.4, amino, alkanoylamino, alkylsulfonylamino, alkoxycarbonylamino, alkoxycarbonyl, cyano, halo, azido, alkyl or haloalkyl; provided that the total number of phenyl, aryl, heteroaryl, cycloalkyl and heterocyclyl radicals in R.sup.1 is 0-3;wherein each R.sup.3 is independently an alkyl, haloalkyl, aryl, heteroaryl, aryl-alkyl or heteroaryl-alkyl radical, wherein the aryl and heteroaryl radicals are optionally substituted by 1-3 radicals of hydroxy, alkoxy, alkylthiol, amino, alkanoylamino, alkylsulfonylamino, alkylsulfinyl, alkylsulfonyl, alkoxycarbonylamino, alkoxycarbonyl, cyano, halo, azido, alkyl, haloalkyl or haloalkoxy; and each R.sup.4 is independently a hydrogen or alkyl radical;R.sup.11 is a --C(O)--R.sup.31, --C(O)--OR.sup.30, --C(O)--NR.sup.32 R.sup.31, --S(O).sub.2 --R.sup.30 or --S(O).sub.2 --NR.sup.32 R.sup.31 radical;R.sup.5 and R.sup.6 are each independently a hydrogen or alkyl radical; or CR.sup.5 --CR.sup.6 is C.dbd.C;wherein R.sup.9 and R.sup.10 are each independently --B--A, provided that the combined total number of aryl, heteroaryl, cycloalkyl and heterocyclyl radicals in R.sup.9, R.sup.10 and R.sup.11 is 0-3;wherein each B is independently a(1) bond;(2) alkyl, alkenyl or alkynyl radical optionally substituted by (a) 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, cyano or halo, and/or (b) 1-2 radicals of heterocyclyl, aryl or heteroaryl optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, cyano, halo, alkyl, haloalkyl or haloalkoxy;(3) heterocyclyl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, cyano, alkyl, haloalkyl or haloalkoxy; or(4) aryl or heteroaryl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, cyano, halo, alkyl, haloalkyl or haloalkoxy;each A is independently a(1) hydrogen radical;(2) halo, cyano or nitro radical;(3) --C(O)--R.sup.30, --C(O)--OR.sup.31, --C(O)--NR.sup.32 R.sup.31 or --C(NR.sup.32)--NR.sup.32 R.sup.31 radical;(4) --OR.sup.31, --O--C(O)--R.sup.31, --O--C(O)--NR.sup.32 R.sup.31 or --O--C(O)--NR.sup.33 --S(O).sub.2 --R.sup.+ radical;(5) --SR.sup.31, --S(O)--R.sup.30, --S(O).sub.2 --R.sup.30, --S(O).sub.2 --NR.sup.32 R.sup.31, --S(O).sub.2 --NR.sup.33 --C(O)--R.sup.31, --S(O).sub.2 --NR.sup.33 --C(O)--OR.sup.30 or --S(O).sub.2 --NR.sup.33 --C(O)--NR.sup.32 R.sup.- radical; or(6) --NR.sup.32 R.sup.31, --NR.sup.33 --C(O)--R.sup.31, --NR.sup.33 --C(O)--OR.sup.30, --NR.sup.33 --C(O)--NR.sup.32 R.sup.31 --NR.sup.33 --C(NR.sup.32)--NR.sup.32 R.sup.31, --NR.sup.33 --S(O).sub.2 --R.sup.30 or --NR.sup.33 --S(O).sub.2 --NR.sup.32 R.sup.31 radical;wherein each R.sup.30 is independently(1) alkyl, alkenyl or alkynyl radical optionally substituted by 1-3 radicals of --CO.sub.2 R.sup.34, amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, N-(alkoxycarbonyl)-N-(alkyl)amino, aminocarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, halo or aralkoxy, arylalkylthio, arylalkylsulfonyl, cycloalkyl, heterocyclyl, aryl or heteroaryl radicals, wherein the cycloalkyl, heterocyclyl, aryl and heteroaryl radicals are optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, alkanoyl, alkoxycarbonyl, hydroxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, halo, alkyl, haloalkyl or haloalkoxy;(2) heterocyclyl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, alkoxycarbonyl, hydroxy, alkoxy, alkylthio, cyano, alkyl, haloalkyl or haloalkoxy; or(3) aryl or heteroaryl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, alkoxycarbonyl, hydroxy, alkoxy, alkylthio, cyano, halo, azido, alkyl, haloalkyl or haloalkoxy;each R.sup.31 is independently hydrogen radical or R.sup.30 ;wherein each R.sup.32 is independently(1) hydrogen radical;(2) alkyl, alkenyl or alkynyl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, hydroxy, alkoxy, alkylthio, cyano or halo; or(3) aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl or cycloalkylalkyl radicals optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, hydroxy, alkoxy, alkylthio, cyano, alkyl, haloalkyl or haloalkoxy; andeach R.sup.33 is independently(1) hydrogen radical;(2) alkyl radical optionally substituted by a radical of heterocyclyl, aryl or heteroaryl which is optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, halo, alkyl, haloalkyl or haloalkoxy; or(3) heterocyclyl, aryl or heteroaryl radical optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, halo, alkyl, haloalkyl or haloalkoxy; andeach R.sup.34 is independently hydrogen, alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl radical, wherein the aryl and heteroaryl radicals are optionally substituted by 1-3 radicals of amino, alkylamino, dialkylamino, alkanoylamino, alkoxycarbonylamino, alkylsulfonylamino, hydroxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, halo, alkyl, haloalkyl or haloalkoxy.