Title:
CARBAPENEM DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/1993/000344
Kind Code:
A1
Abstract:
Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1-$g(b)-methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including $i(Pseudomonas aeruginosa) and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R?1¿ represents lower alkyl or optionally protected hydroxy lower alkyl; R?2¿, R?13¿ and R?14¿ represent each hydrogen or lower alkyl; R?3¿ represents optionally esterified carboxyl; R?4¿, R?9¿, R?10¿ and R?15¿ represent each an amino-protective group, hydrogen or lower alkyl; R?5¿, R?6¿, R?11¿ and R?12¿ represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R?5¿ and R?6¿ and/or R?11¿ and R?12¿ may combine together to form alkylene; R?7¿ represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR?71¿R?72¿; R?71¿ and R?72¿ represent each hydrogen or lower alkyl; R?8¿ represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R?8¿ may combine with R?7¿ to form alkylene; Z represents a single bond, oxygen, sulfur, -CR?11¿R?12¿-, -NR?13¿CO-, -CONR?14¿- or -NR?15¿-; and m and n represent each an integer of 0 to 6.
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Inventors:
NISHI TOSHIYUKI (JP)
KODA HIROKO (JP)
SUGITA KAZUYUKI (JP)
ISHIDA YOHHEI (JP)
TAKEMURA MAKOTO (JP)
KODA HIROKO (JP)
SUGITA KAZUYUKI (JP)
ISHIDA YOHHEI (JP)
TAKEMURA MAKOTO (JP)
Application Number:
PCT/JP1992/000790
Publication Date:
January 07, 1993
Filing Date:
June 19, 1992
Export Citation:
Assignee:
DAIICHI SEIYAKU CO (JP)
International Classes:
A61K31/40; A61K31/397; A61K31/4025; A61K31/496; A61P31/04; C07D477/00; C07D477/20; C07D; (IPC1-7): A61K31/40; C07D477/00
Foreign References:
| JPS60233076A | 1985-11-19 | |||
| JPS63179876A | 1988-07-23 | |||
| JPS6019787A | 1985-01-31 |
Other References:
See also references of EP 0641795A4
Attorney, Agent or Firm:
Hagino, Taira (14th Floor Toranomon-Mitsui Building, 8-1,
Kasumigaseki 3-chom, Chiyoda-ku Tokyo 100, JP)
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