Pharmaceutical compounds

Details Pharmaceutical compounds Pharmaceutical compounds

C - Chemistry, Metallurgy

07

C

C07C 229/36 (2006.01) A61K 31/195 (2006.01) A61K 31/21 (2006.01) A61K 31/33 (2006.01) A61K 31/66 (2006.01) C07C 229/38 (2006.01) C07C 309/61 (2006.01) C07C 311/37 (2006.01) C07C 323/63 (2006.01) C07D 213/55 (2006.01) C07D 257/04 (2006.01) C07D 295/04 (2006.01) C07D 295/155 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01) C07F 9/02 (2006.01)

Patent

CA 2204846

A pharmaceutical compound of the formula: (see fig. I) in which R1 is hydrogen, hydroxy or C1-6 alkoxy, R2 is hydrogen, carboxy, tetrazolyl, -SO2H, -SO3H, -OSO3H, -CONHOH, or -P(OH)OR', -PO(OH)OR', -OP(OH)OR' or -OPO(OH)OR' where R' is hydrogen, C1-6 alkyl, C2-6 alkenyl or aryl C1-6 alkyl, R3 is hydrogen, hydroxy or C1-4 alkoxy, and R4 is fluoro, trifluoromethyl, nitro, C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C1-6 alkyl, optionally substituted aryl C2-6 alkenyl, optionally substituted aryl C2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C1-6 alkylthio or -CONR''R''', -SO2NR''R''', -NR''R''', -OCONR''R''' or -SONR''R''' where R'' and R''' are each hydrogen, C1-6 alkyl or aryl C1-6 alkyl, or R'' and R''' together form a C3-7 alkylene ring; provided that (i) R1, R2 and R3 are not all hydrogen,and (ii) when R2 and R3 are hydrogen and R1 is hydroxy, R4 is not fluoro; or a salt or ester thereof.

Composé pharmaceutique de formule (voir fig. I), dans laquelle R1 est un hydrogène, un hydroxy ou un alcoxy C1-6, R2 est un hydrogène, un carboxy, un tétrazolyle, un groupe -SO2H, -SO3H, -OSO3H, -CONHOH ou -P(OH)OR', -PO(OH)OR', -OP(OH)OR' ou -OPO(OH)OR' où R' est un hydrogène, un alkyle C1-6 , un alcényle C2-6 ou un aryle alkyle C1-6, R3 est un hydrogène, un hydroxy ou un alcoxy C1-4, R4 est un groupe fluoro, trifluorométhyle, nitro, alkyle C1-6, cycloalkyle C3-7, alcényle C2-6, alcynyle C2-6, alkylthio C1-6, hétéroaryle, aryle avec substitution facultative, aryle alkyle C1-6 avec substitution facultative, aryle alcényle C2-6 avec substitution facultative, aryle alcynyle C2-6 avec substitution facultative, aryloxy avec substitution facultative, aryle alcoxy C1-6 avec substitution facultative, arylthio avec substitution facultative, aryle alkylthio C1-6 avec substitution facultative, ou -CONR''R''', -SO2NR''R''', -NR''R''', -OCONR''R''' ou -SONR''R''' où R'' et R''' sont chacun de l'hydrogène, un groupe alkyle C1-6 ou aryle alkyle C1-6, où R'' et R''' forment ensemble un cycle alcylène C3-7; à la condition que (i) R1, R2 et R3 ne soient pas tous de l'hydrogène, et que (ii) lorsque R2 et R3 sont de l'hydrogène, avec R1 un hydroxy, R4 ne soit pas du fluor; ou encore un sel ou ester de ce composé.

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