Patent ID: 6656934
Filing Date: 2003-12-02
Classification: A61P,C07C,C07D

Abstract:
A compound of formula (IIa): or a pharmaceutically acceptable salt, ester, amide or prodrug therof;wherein: R1a represents (i) a C10-30 branched or unbranched alkyl, C2-30 alkenyl, C2-30 alkynyl, cycloalkenyl, aryl-C10-30 alkyl, aryl-C10-30 alkenyl, heteroaryl, heteroaryl-C1-30 alkyl, heteroaryl-C2-30 alkenyl, reduced aryl, reduced heteroaryl, reduced heteroaryl-C1-30 alkyl or a substituted derivative therof wherein the substituents are one or more independently chosen from the group consisting of halogen, C1-10 alkyl, halosubstituted C1-10 alkyl, aryl, aryl-C1-10 alkyl, heteroaryl, reduced heteroaryl, reduced heteroaryl-C1-10 alkyl, aryl-C1-10 alkoxy, cyano, nitro, â€”C(O)R13, â€”CO2R13, â€”SOR13, â€”SO2R13, â€”N13R14, â€”OR13, â€”SR13, â€”C(O)NR13R14, and â€”NR14C(O)R13, with the proviso that any hetero atom substituent in R1a must be separated from the exocyclic nitrogen atom by at least two carbon atoms; or (ii) aryl substituted by one or more independently chosen from the group consisting of halosubstituted C1-10 alkyl, aryl, aryl-C1-10 alkyl, heteroaryl, reduced heteroaryl, reduced hetcroaryl-C1-10 alkyl, aryl-C1-10 alkoxy, cyano, â€”C(O)R13, â€”CO2R13, â€”SOR13, â€”SO2R13, â€”NR13R14, â€”OR13(providing that in this instance R13 does not represent aryl or alkyl), â€”SR13, â€”C(O)NR13R14,and â€”NR14C(O)R13 wherein: R13 and R14 each independently represents hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C3-6cycloalkyl, C3-6cycloalkenyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10alkyl, reduced heteroaryl or reduced heteroarylC1-10alkyl; R2a is hydrogen or an R1 group wherein: R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, aryl alkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative therof wherein the substituents are one or more independently chosen from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, heteroaryl, reduced heteroaryl, reduced heteroarylalkyl, arylalkoxy, cyano, nitro, â€”C(O)R4, â€”CO2R4, â€”SOR4, â€”SO2R4, â€”NR6R7, â€”OR6, â€”SR6, â€”C(O)CX1X2NR6R7, â€”C(O)NR4R5, â€”C(O)N(OR5)R6, â€”NR6C(O)R4, â€”CR6(NH2)CO2R6, â€”NHCX1X2CO2R6, â€”N(OH)C(O)NR6R7, â€”N(OH)C(O)R4, â€”NHC(O)NR6R7, â€”C(O)NHNR6R7, â€”C(O)N(OR5)R6, or a lipid or steroid (natural or synthetic), with the proviso that any hetero atom substituent in R1 must be separated from the exocyclic nitrogen atom by at least two carbon atoms; wherein: R4 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, reduced heteroaryl, reduced heteroarylalkyl, â€”OR6, â€”NHCX1X2CO2R6 or â€”NR6R7; R5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, reduced heteroaryl or reduced heteroarylalkyl; R6 and R7 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, reduced heteroaryl, heteroarylalkyl, reduced heteroarylalkyl or â€”(CH2)n(OR5)m wherein n is 1 to 12, and m is 1-3; and X1 and X2 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, reduced heteroaryl or reduced heteroarylalkyl; and R8a, R9a, and R11a are each independently hydrogen, halo, hydroxy, amino, nitro, cyano, or a group R1, as defined above; or a group R12Q where Q is O, CO, CONH, NHCO, S, SO, SO2, or SO2NH2 and R12 is hydrogen or a group as defined above; or a group R1R2N where R1 is as defined above and R2 is hydrogen or an group as defined above, with the proviso that any hetero atom substituent in R1 and/or R2 must be separated from the aromatic hetero atom substituent by at least two carbon atoms; and R10a is independently halo, hydroxy, amino, nitro, cyano or a group R1 as defined above; or a group R12Q wherein Q is O, CO, CONE, NECO, S, SO, SO2 or SO2NH and R12 is hydrogen or a group R1 as defined above; provided that: when R1a represents a heteroaryl group it is not thiadiazolyl, triazolyl or thiazolyl; and when R1a represents a reduced heteroaryl group it is not thiazolidinyl.