Fluoralkylatedcarbapenem derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/40 (2006.01) C07D 205/08 (2006.01) C07D 477/20 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1241656

Abstract Compounds of formula I Image I wherein, R1 represents hydrogen or methyl, R2 represents hydrogen or lower alkyl, lower alkynyl, 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-R5 IIc wherein R5 represents phenyl or a 5- or 6-membered saturated or unsaturated heterocycle containing one or more heteroatoms selected from 0, S and/or N and which may be unsubstituted or mono- or poly- substituted by fluoro, chloro, bromo, amino, mono- or di-(lower)-alkylamino, hydroxy, lower alkoxy, mercapto, alkylthio, phenylthio, sulfamoyl, guanidino, nitro, cyano, lower acylamino, carboxy , alkoxycarbonyl or carbamoyl and p is 0, 1, 2 or 3; or a group of formula Image II Image IIa Image IIb wherein R6, R7 and R8 may be the same or different and each represents hydrogen or lower alkyl or R6 and R8 and/or R7 and one of the CH2 groups may be joined to form a ring as may R7 and R8 in formula II and R6 and R7 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 R3 represents hydrogen or lower alkyl and R4 represents lower alkyl, which are indicated for use as pharmaceuticals particularly as anti- bacterially active antibiotics.

464654

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