Carbapenem derivatives

Details Carbapenem derivatives Carbapenem derivatives

C - Chemistry, Metallurgy

07

D

C07D 477/00 (2006.01) C07D 477/20 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2111974

Prior art carbapenem derivatives including thienamycin have disadvantages in that they are physico- chemically unstable and apt to be decomposed by DHP and the like enzyme in the kidney, thereby causing side-effects such as renal toxicity. In addition, 1-b-methylcarbapenem compounds which exhibit stable and strong antibacterial activity are still unsatisfactory in terms of their stability and antibacterial activity against DHP. The present invention provides an antibiotic which shows strong antibacterial activity against various bacterial strains including Pseudomonas aeruginosa and is excellent in terms of safety and stable against hydrolases such as DHP. A compound represented by formula (I): Image (I) wherein R1 represents a lower alkyl group or a hydroxy lower alkyl group which may have a protecting group; R1 represents a hydrogen atom or a lower alkyl group; R3 represents a carboxyl group which may be esterified; R4 represents an amino group-protecting group, a hydrogen atom or a lower - 76 - alkyl group; R5 and R6, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a hydroxy lower alkyl group or a halogen atom, and R5 and R6 may together form an alkylene group having 2 to 6 carbon atoms; R7 represents a hydrogen atom, a lower alkyl group, a carboxyl group, a carbamoyl group, a carboxyl group which may have a protecting group, or a partial structure represented by -CON71R72 where R71 and R72, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; R8 represents a hydrogen atom, a lower alkyl group or a hydroxy lower alkyl group, and R7 and R8 may together form an alkylene group having 2 to 6 carbon atoms; R9 and R10, which may be the same or different, each represents an amino group-protecting group, a hydrogen atom or a lower alkyl group; Z represents a single bond, an oxygen atom, a sulfur atom, or a partial structure represented by - CR11R12-, -NR13CO-, -CONR14- or -NR15- where R11 and R12, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a hydroxy lower alkyl group or a halogen atom, and R11 and R12 may together form an alkylene group having 2 to 6 carbon atoms, R13 and R14, which may be the same or different, each represents a hydrogen atom or a lower alkyl group and R15 represents an amino group-protecting group, a hydrogen atom or a lower alkyl group; and each of m and n represents an integer of 0 to 6, and a salt thereof. - 77 -

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