Patent ID: 6630504
Filing Date: 2003-10-07
Classification: A61K,A61P,C07D

Abstract:
A compound of formula (I), or a pharmaceutically acceptable salt, solvate or polymorph thereof; wherein: R1 is H or C1-C6 alkyl; R2 and R3, together with the interconnecting atoms thereof form a pyrrolidine ring; Z is CF3, OCF3, C1-C6alkylthio or C1-C6alkoxy; Y is hydrogen, halogen, â€”ORa, Ra or C1-C6alkylthio, and wherein Ra is C1-C4 alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: Aâ€”X, wherein A=â€”CH&boxH;CHâ€” or â€”(CH2)pâ€” where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(&boxH;O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O)R6, CO2R9, C(O)NHR6 or SO2NR6R7; R12 is F, OH, CO2H, C3-6cycloalkyl, NH2, CONH2, C1-6alkoxy, C1-6alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R13; or R6 and R7, together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R13; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, â€”NH2, â€”NH(C1-C6alkyl) or â€”N(C1-C6alkyl)2 with the proviso that R4 and R5 are not both hydrogen.