C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/118.5
C07D 499/00 (2006.01) C07D 209/48 (2006.01) C07D 211/18 (2006.01) C07D 211/22 (2006.01) C07D 211/28 (2006.01) C07D 221/20 (2006.01) C07D 221/22 (2006.01) C07D 223/04 (2006.01) C07D 233/04 (2006.01)
Patent
CA 1104126
Ry/1t/461 F Abstract of disclosure The present invention relates to a method for the preparation of a compound of the general formula I, II, or III Image I Image II Image III in which -A- stands for a straight or branched, saturated or unsaturated aliphcatic hydrocarbon radical, containing from 1 to 6 carbon atoms, which radical optionally can be substituted with an amino radical; R1 stands for hydrogen, or a lower alkyl radical with from 1 to 4 carbon atoms; R2 stands for hydrogen, a lower allkyl radical with from 1 to 4 carbon atoms, or a monoacyl radical derived from a mono- or dibasic carboxylic acid, sulphuric acid, a sulphonic acid, a sulphinic acid, phosphoric acid, or a phosphonic acid, and R2 can represent an unsubstituted or substituted carbamoyl, guanyl and guanylcarbamoyl radical; R1 and R2 together with the nitrogen atom can form a monocyclic, saturated ring having from 4 to 8 carbon atoms; furthermore R1 and R2 together can represent a radical of the formula Image , in which R3 and R4 each stands for hydrogen, lower alkyl, phenyl or phenyl-lower alkyl, or in which R3 and R4 together with the nitrogen atom form a mono- cyclic, saturated ring having from 4 to 7 carbon atoms; the groupings: Image ; Image ; Image ; repesent saturated, monocyclic, bicyclic or spirocyclic ring systems, respectively, containing from 4 to 11 carbon atoms in total; P stands for the penicillanic acid radical of the formula IV; Image IV and salts of the compounds of the formulae I, II, and III with pharmaceutically acceptable, non-toxic organic and inorganic acids or bases, and easily hydrolyzable pharma- ceutically acceptable, non-toxic esters of the penicillanic acid derivatives of formulae I, II, and III, including diesters of the formula V: Image V in which X and Y can be the same or different and stand for an acyl radical of one of the compounds of formulae I, II, and III, and Y furthermore can be the acyl radical of other known .beta.-lactam antibiotics, R5 stands for hydrogen, methyl, ethyl, or phenyl, and salts of such esters with pharmaceutically acceptable, non-toxic acids or bases. The compounds prepared according to the invention have shown increased activity against a series of bacteria which cause infections difficult to combat with the presently available antibiotics.
280167
Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik Prod
Marks & Clerk
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