Patent ID: 6335329
Filing Date: 2002-01-01
Classification: A61P,C07D

Abstract:
A compound of formula or a pharmacutically acceptable salt thereof, whereinm is 1; and n is 1; R1 is (1) an alkyl, alkenyl, alkynyl, cycloalkyl or heterocyclyl radical optionally substituted by 1-3 radicals of â€”OH, â€”OR3, â€”SR3, â€”S(O)R3, â€”S(O)2R3, â€”C(O)R3â€”NR3R4, 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, â€”OR3, â€”SR3, â€”S(O)R3, â€”S(O)2R3, â€”C(O)R3, â€”NR3R4, 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 R1 is 0-3; wherein each R3 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 R4 is independently a hydrogen or alkyl radical; R11 is a â€”C(O)â€”R31, â€”C(O)â€”OR30, â€”C(O)â€”NR32R31, â€”S(O)2â€”R30 or â€”S(O)2â€”NR32R31 radical; R5 and R6 are each independently a hydrogen or alkyl radical; or CR5â€”CR6 is C&boxH;C; wherein R9 and R10 are each independently â€”Bâ€”A, provided that the combined total number of aryl, heteroaryl, cycloalkyl and heterocyclyl radicals in R9, R10 and R11 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) â€”C(O)â€”R30, â€”C(O)â€”OR31, â€”C(O)â€”NR32R31 or â€”C(NR32)â€”NR32R31 radical; (4) â€”OR31, â€”Oâ€”C(O)â€”R31, â€”Oâ€”C(O)â€”NR32R31 or â€”Oâ€”C(O)â€”NR33â€”S(O)2â€”R30 radical; (5) â€”SR31, â€”S(O)â€”R30, â€”S(O)2â€”R30, â€”S(O)2â€”NR32R31, â€”S(O)2â€”NR33â€”C(O)â€”R31, â€”S(O)2â€”NR33â€”C(O)â€”OR30 or â€”S(O)2â€”NR33â€”C(O)â€”NR32R31 radical; or (6) â€”NR32R31, â€”NR33â€”C(O)â€”R31, â€”NR33â€”C(O)â€”OR30, â€”NR33â€”C(O)â€”NR32R31, â€”NR33â€”C(NR32)â€”NR32R31, â€”NR33â€”S(O)2â€”R30 or â€”NR33â€”S(O)2â€”NR32R31 radical; wherein each R30 is independently (1) alkyl, alkenyl or alkynyl radical optionally substituted by 1-3 radicals of â€”CO2R34, 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 R31 is independently hydrogen radical or R30; wherein each R32 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; and each R33 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; and each R3 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.