C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/224, 167/238
C07D 237/32 (2006.01) A61K 31/415 (2006.01) A61K 31/50 (2006.01) C07D 417/06 (2006.01)
Patent
CA 2032231
Substituted oxophthalazinyl acetic acids possessing aldose reductase inhibitory activity have the formula Image I wherein A1, A2, B, R1, R2, and R3 are as defined herein, including the pharmaceutically acceptable base salts thereof when R1 is hydrogen. (Wherein A1 and A2 are indepen- dently N or CH; B is a covalent bond or C=O; R1 is hydrogen or C1-C6 alkyl; R2 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 alkylthio; R3 is Image or Image wherein R4 is phenyl optionally indpendently substituted by one, two or three substituents each independently selected from the group consisting of fluoro, chloro, bromo, trifluoromethyl, trifluoromethylthio, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl- thio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl and nitro; with the proviso that when R4 is disubstituted phenyl, the substitution is at the 3 and 4, or the 3 and 5, or the 2 and 5 positions in the phenyl; X is oxygen or sulphur; Y is hydro- gen; or Y forms an indole group with the carbon on the ortho position of the phenyl in R4; or a pharmaceutically acceptable base salt thereof when R1 is hydrogen; with the proviso that when B is a covalent bond, A1 and A2 are each CH).
Pfizer Inc.
Smart & Biggar
LandOfFree
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