C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
167/226, 260/283
C07C 211/29 (2006.01) A61K 31/47 (2006.01) C07C 211/52 (2006.01) C07C 229/30 (2006.01) C07D 215/56 (2006.01) C07D 405/06 (2006.01)
Patent
CA 1334756
Disclosed are novel 1,7-disubstituted-6-fluoro-1,4- dihydroquinol-4-one-3-carboxylic acid derivatives of the formula Image ---I wherein R5 is H, F, Cl, OCH3 or Z; R1 is H, (C1-C7) alkyl, benzyl or a pharmaceutically acceptable cation; R2 is vinyl, W substituted vinyl, CH3C-C-, W-CH2C-C-, cyclo- propyl or W Image ; W is R3-(CH2)m-;m is 1 or 2; R3 is OH, NH2, NH(C1-C3) alkyl, SO2 (C1-C3) alkyl, SO2NH(C1-C3)alkyl or SO2NH2; Y is (C1-C3)alkyl, (C1-C3) haloalkyl, cyclopropyl, vinyl, p-fluorophenyl or o,p-difluorophenyl; or R5 is Z and Z is taken together with Y and have the formula -X-(CH2)n-CHR4- wherein X is CH2 or O and is bonded to position 8 of the quinolone ring; n is 0, 1 or 2; and R4 is selected from the group consisting of hydrogen, alkyl and haloalkyl of 1 to 3 carbons, hydroxymethyl, hydroxyethyl, aminomethyl, phenyl and methylene; and the pharma- ceutically acceptable salts thereof. They have antibacterial activities and useful as antibacterial agents. Also disclosed are a novel process for preparing novel N-cyclopropyl intermediates useful for preparing certain of the 1,7-disubstituted-6-fluoro- 1,4-dihydroquinol-4-one-3-carboxylic acid derivatives which contain a cyclopropyl substituent at the 1 position as well as other 1,4-dihydroquinol-4-one-3-carboxylic acid derivatives so substituted with cyclopropyl.
603221
Limited Pfizer
Smart & Biggar
LandOfFree
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