主权项 |
1. A compound of formula (I) or their tautomers, stereoisomers, pharmaceutically acceptable salts, wherein, A represents a five membered aromatic ring having upto two heteroatoms selected from O, N or S; or a six membered aromatic ring optionally having upto three heteroatoms selected from N; B represents a fused heterocycle selected from: represents a single bond or a double bond provided that R2 is absent when the bond between N to which it is attached and Y1 represents a double bond; Y1, Y3, Y4 and Y5 independently represents N or CR4; Y2 represents NR4′ or CR4R4′ provided that R4′ is absent when the bond between Y1 and Y2 represents a double bond; R1 is selected from hydrogen, alkyl, alkenyl, alkynyl, alkoxy, acyl, acylamino, acyloxy, —(CRaRb)nC(O)R5, —(CRaRb)nNR6R7, aminocarbonyl, alkoxycarbonylamino, alkylsulfonylamino, aminocarbonylamino, hydroxyamino, alkoxyamino, azido, cyano, halogen, hydroxy, hydroxyalkyl, haloalkyl, perhaloalkyl, thiocarbonyl, carboxy, alkylcarboxy, carboxyalkyl, carboxyalkyloxy, alkylcarboxyalkyloxy —SO3H, alkylthio, aminosulfonyl, alkylsulfonyl, or nitro; R2 is selected from hydrogen, alkyl, cycloalkyl, aryl, heterocyclyl or heteroaryl; R3 is selected from the group consisting of hydrogen, hydroxyalkyl, amino, monoalkylamino, dialkylamino, halogen, perhaloalkyl, cyano, nitro, alkoxyalkyl, carboxy, carboxyalkyl, acyl, aminocarbonyl, alkyl, alkenyl, alkynyl, hydroxyalkyl, carboxyalkyl, haloalkyl and haloalkyloxy; R4 and R4′ are independently selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, carboxyalkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl;
wherein alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, arylalkyl, aryl, heteroaryl, heteroarylalkyl, heterocyclyl, and heterocyclylalkyl are independently unsubstituted or substituted with upto four substituents independently selected from alkyl, alkenyl, alkynyl, alkoxy, acyl, acyloxy, acylamino, amino, halogen, hydroxy, hydroxyalkyl, keto, thiocarbonyl, carboxy, alkylcarboxy, carboxyalkyl, —SO3H, aminocarbonyl, aminocarbonylamino, alkoxycarbonylamino, hydroxyamino, alkoxyamino, nitro, azido, cyano, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl cycloalkenyl, cycloalkylamino, arylamino, heterocyclylamino, heteroarylamino, cycloalkyloxy, aryloxy, heterocyclyloxy or heteroaryloxy; Z is a bond or is selected from cycloalkylene, cycloalkylenealkyl, cycloalkenylene, cycloalkyleneoxo, cycloalkyleneamino, arylene, arylenealkyl, arylenethio, aryleneoxy, aryleneamino, arylenealkoxycarbonylamino, arylenesulfonyl, arylenesulfonylamino, heterocyclylene, heterocyclylenealkyl, heterocyclyleneoxy, heterocyclylenealkyloxy, heterocyclyleneamino, heterocyclylenethio, heterocyclylenealkylamino heteroarylene, heteroarylenealkyl, heteroaryleneoxy, heteroaryleneamino, spirocyclyl, (C1-6)alkylene, (C1-6)alkenylene or (C1-6)alkynylene wherein one or more than one methylene groups from alkylene, alkenylene or alkynylene are optionally replaced by hetero atoms or groups such as —O—, —S(O)p, —N(R5)—, or —C(O); D is a bond or is selected from cycloalkylene, cycloalkenylene, cycloalkylenecarbonyl, cycloalkylenealkoxy, cycloalkyleneamino, arylene, arylenecarbonyl, arylenealkoxycarbonyl, arylenealkoxycarbonylamino, aryleneaminocarbonyl, heterocyclylene, heterocyclyl ene alkyl, heterocyclylenecarbonyl, heterocyclylenealkylamino, heteroarylene, heteroarylenecarbonyl, heteroarylenealkylamino, (C1-6)alkylene, (C1-6)alkenylene or (C1-6)alkynylene wherein one or more than one methylene groups from alkylene, alkenylene or alkynylene are optionally replaced by hetero atoms or groups such as —O—, —S(O)p-, —N(R5)—, —C(O) or —C(═NR″)— wherein R″ is H, alkyl, cyano, hydroxy, hydroxyalkyl, haloalkyl or perhaloalkyl; E is selected from hydrogen, hydroxy, alkoxy, alkoxyalkyl, cyano, halogen, haloalkyl, perhaloalkyl, alkyl, alkenyl, alkynyl, carboxy, carboxyalkyl, cyanoalkyl, acyl, cyanoalkylarbonyl, cyanoalkenylcarbonyl, —(CRaRb)nOR5, —SR5, —(CRaRb)nCOOR5, —(CRaRb)nNR6R7, —(CRaRb)nC(O)NR6R7, —(CRaRb)nNR5C(O)NR6R7, thiocarbonyl, S(O)2NR6R7, —NR5S(O)2R5, —S(O)pR5, —SO3H, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkyloxy, cycloalkylamino, aryl, arylalkyl, aryloxy, arylamino, heterocyclyl, heterocyclylalkyl, heterocyclyloxy, heterocycloalkylamino, heteroaryl, heteroarylalkyl, heteroaryloxy, or heteroarylamino; R5 is selected from the group consisting of hydrogen, —(CRaRb)nOR8, halogen, haloalkyl, —(CRaRb)nC(O)R8, alkyl, alkenyl, alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl and heterocyclylalkyl;
wherein alkyl, alkenyl, alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl or heterocyclylalkyl are optionally substituted with one or more substituents selected from hydroxy, alkyl, alkoxy, alkoxyalkyl, halogen, haloalkyl, perhaloalkyl, cyano, cyanoalkyl, amino, carboxy, carboxyalkyl, OR8, —OC(O)R8, —(CRaRb)nC(O)NR6R7, —NR8C(O)R8, —SR8, —S(O)pR8, —S(O)2NR6R7 or —NR8S(O)2R8; R6 and R7 are independently selected from the group consisting of hydrogen, —(CRaRb)nOR5, haloalkyl, —(CRaRb)nC(O)R5, alkyl, alkenyl, alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl and heterocyclylalkyl, or R6 and R7 taken together form a monocyclic or a bicyclic ring system which is saturated or partially unsaturated and optionally have additional heteroatoms selected from O, N or S, the said ring system is further optionally substituted with 1 to 4 substituents independently selected from halo, alkyl, alkenyl, alkynyl, nitro, cyano, —(CRaRb)nOR5, —SR5, —(CRaRb)nNR6R7, oxo, alkylsulfonyl, —(CRaRb)nCOOR5, —(CRaRb)nC(O)NR6R7, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl; Z, D and E may be optionally substituted with one or more substituents independently selected from cyano, nitro, keto, oxo, halogen, haloalkyl, perhaloalkyl, hydroxyamino, —(CRaRb)nOR5, —(CRaRb)nC(O)R5, —OC(O)R5, —SR5, —(CRaRb)nCOOR5, —(CRaRb)nNR6R7, —(CRaRb)nC(O)NR6R7, —(CRaRb)nNR5C(O)NR6R7, —NR5C(O)R5, thiocarbonyl, —S(O)2NR6R7, —NR5S(O)2R5, —S(O)pR5, —SO3H, —OP(O)(R9)q, alkyl, alkenyl, alkynyl, cycloalkyl, cyclkenyl, cycloalkylalkyl, aryl, heterocyclyl or heteroaryl;
wherein alkyl, alkenyl, alkynyl, cycloalkyl, cyclkenyl, cycloalkylalkyl, aryl, heterocyclyl or heteroaryl are optionally substituted with one or more substituents selected from hydroxy, alkyl, alkoxy, alkoxyalkyl, halogen, haloalkyl, perhaloalkyl, cyano, cyanoalkyl, amino, carboxy, carboxyalkyl, —OC(O)R5, —(CRaRb)nC(O)NR6R7, —NR5C(O)R5, —SR5, —S(O)pR5, —S(O)2NR6R7 or —NR5S(O)2R5; R8 is selected from the group consisting of hydrogen, alkyl, alkoxy, haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl and heterocyclylalkyl;
wherein alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl or heterocyclylalkyl are optionally substituted with one or more substituents selected from hydroxy, alkyl, alkoxy, alkoxyalkyl, halogen, haloalkyl, perhaloalkyl, cyano, cyanoalkyl, amino, carboxy or carboxyalkyl; R9 is selected from the group consisting of hydroxy and alkoxy; Ra and Rb are independently selected from the group consisting of hydrogen, —OR5, halogen, haloalkyl, perhaloalkyl and alkyl; n is 0-6; m is 0, 1 or 2; p is 0, 1 or 2; and q is 1 or 2; with the proviso that in (IIc) when Y5 is CR4, then Y3 and Y4 cannot be CR4. |