Fluoralkylated carbapenem derivatives

Details Fluoralkylated carbapenem derivatives Fluoralkylated carbapenem derivatives

C - Chemistry, Metallurgy

07

D

167/208, 260/299

C07D 487/04 (2006.01) A61K 31/40 (2006.01) A61K 31/535 (2006.01) C07D 205/08 (2006.01) C07D 477/10 (2006.01) C07D 477/20 (2006.01) C07D 499/88 (2006.01) C07F 7/10 (2006.01)

Patent

CA 1250839

- 1 - Abstract of the Disclosure Compounds of formula Image wherein, R1 represents hydrogen or methyl and R2 represents hydrogen or lower alkyl, lower alkenyl or cycloalkyl each of which may be unsubstituted or mono- or poly-substituted by amino, mono- or di-(lower)-alkylamino, lower acylamino, carboxy, lower alkoxycarbonyl or carbamoyl; a group of formula IIc (CH2)p-R7 IIc wherein R7 represents phenyl or a 5- or 6-membered saturated or unsaturated heterocycle containing one or more heteroatoms selected from O, S and/or N and which may be unsubstituted or mono- or poly-substituted by fluoro, chloro, bromo, amino, mono- or di-(lower)-alkyl- amino, hydroxy, lower alkoxy, mercapto, alkylthio, phenylthio, sulfamoyl, guani- dino, nitro, cyano, lower acylamino, carboxyl, alkoxycarbonyl or carbamoyl and p is 0, 1, 2 or 3; or a group of formula Image II Image IIa Image IIb - 2 - wherein R4, R5 and R6 may different and each represents hydrogen or lower alkyl or R4 and R6 and/or R5 and one of the CH2 groups may be joined to form a ring as may R5 and R6 in formula II and R4 and R5 in IIa and IIb, which rings may be unsubstituted or mono- or poly-substituted by alkyl, hydroxy, carboxy or di-(lower)-alkyl- amino, m is 2 or 3, and n is 1, 2 or 3 with the proviso that when R1 is hydrogen and the group containing it has R-configuration, R2 is other than acetylaminoethyl; or protected forms and/or physiologically-hydrolysable and acceptable ester forms thereof; in free acid or salt form or in the form of zwitter-ions. The compounds exhibit chemotherapeutic properties and are particularly indicated for use as anti-bacterially active antibiotics.

433093

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