Patent ID: 6562851
Filing Date: 2003-05-13
Classification: A61P,C07D

Abstract:
A compound of formula (Ia): wherein:R1 represents aryl, heteroaryl, optionally substituted alkyl, alkenyl or alkynyl where each is optionally substituted by R3, â€”Z2R4, â€”Z3H, â€”C(&boxH;O)â€”R4, â€”NR5â€”C(&boxH;Z3)â€”R4, â€”NR5â€”C(&boxH;O)â€”OR4, â€”NR5â€”SO2â€”R4, â€”SO2â€”NY1Y2, â€”NY1Y2 or â€”C(&boxH;Z3)â€”NY1Y2; or cycloalkyl or heterocycloalkyl, each optionally substituted by R4, â€”Z2R4, â€”Z3H, â€”C(&boxH;O)â€”R4, â€”NR5â€”C(&boxH;Z3)â€”R4, â€”NR5â€”C(&boxH;O)â€”OR4, â€”NR5â€”SO2â€”R4, â€”SO2â€”NY1Y2, â€”NY1Y2 or â€”C(&boxH;Z3)â€”NY1Y2; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; R3 represents aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycloalkyl; R4 represents alkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, heterocycloalkyl or heterocycloalkylalkyl; R5 represents hydrogen or C1-4alkyl; R6 is an alkylene chain, an alkenylene chain or an alkynylene chain; R8 is hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R9 is alkyl, aryl, cycloalkyl, heteroaryl or heterocycloalkyl, or alkyl substituted by aryl, an acidic functional group or corresponding protected derivative, cycloalkyl, heteroaryl, heterocycloalkyl, â€”Z3H, â€”Z2R4, â€”C(&boxH;O)â€”NY3Y4 or â€”NY3Y4; R12 is hydrogen, acyl, acylamino, alkoxy, alkoxycarbonyl, alkylenedioxy, alkylsulphinyl, alkylsulphonyl, alkylthio, aroyl, aroylamino, aryl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxycarbonyl, arylsulphinyl, arylsulphonyl, arylthio, carboxy, cyano, halo, heteroaroyl, heteroaryl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, hydroxy, nitro, trifluoromethyl, Y1Y2Nâ€”, Y1Y2NCOâ€”, Y1Y2NSO2â€”, Y1Y2Nâ€”C2-6alkylene-Zâ€”, alkylC(&boxH;O)â€”Y1Nâ€”, alkylSO2â€”Y1Nâ€” or alkyl optionally substituted with aryl, heteroaryl, hydroxy, or Y1Y2Nâ€”; L2 represents an alkylene chain substituted by hydroxy, oxo, â€”OR4, â€”Oâ€”C(&boxH;O)â€”R4, â€”N(R8)â€”C(&boxH;O)â€”R9, â€”N(R8)â€”C(&boxH;O)â€”OR9, â€”N(R8)â€”SO2â€”R9, or â€”NY3Y4; X is O; Y is carboxy; Y1 and Y2 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heteroarylalkyl; or the group â€”NY1Y2 may form a cyclic amine; Y3 and Y4 are independently hydrogen, alkenyl, alkyl, alkynyl, aryl, cycloalkenyl, cycloalkyl, heteroaryl, heterocycloalkyl, or alkyl substituted by alkoxy, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, hydroxy, oxo, â€”NY1Y2, or one or more â€”CO2R8 or â€”C(&boxH;O)â€”NY1Y2 groups; or the group â€”NY3Y4 may form a cyclic amine; Z1 represents NR5; Z2 is O or S(O)n; Z3 is O or S; and n is zero or an integer 1 or 2; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts, and solvates of such compounds and their N-oxides and prodrugs.