PHARMACEUTICAL PREPARATION CONTAINING 1-METHYLCARBAPENEM DERIVATIVE

• Main Authors: OYA SATORU, UTSUI YUKIO, ISHIKAWA KATSUYA, SHIMOJI YASUO, YASUDA HIROSHI, KAWAMOTO ISAO, KOJIMA KATSUHIKO
• Format: Patent
• Language: English
• Published: 16.11.1999
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To obtain a pharmaceutical preparation having excellent antibacterial activity and useful for the prevention or treatment of infectious diseases by including a methylcarbapenem derivative as an active component. SOLUTION: A compound of formula I R is H or a 1-4C alkyl; R is H or the like; A is a group of formula II [(n) is 0-2; (p) is 0-2; R is H or a 1-4C alkyl; R is a group of formula III (B is phenylene, phenylenealkyl or the like; R is H or a 1-4C alkyl; R is a group of the formula: C (=NH) R (R is H or the like))] or the like} such as 2- 2-[3-(2-guanidinoacetylamino)pyrrolidin-1- ylcarbonyl]pyrrolidin-4-ylthio}-6-(1-hydroxyethyl)-1-methyl-1-carbapen -2-em-3- carboxylic acid is used as an active component of the objective preparation. The compound of formula I is stable to dehydropeptidase I and β-lactamase and has high recovery ratio to urine and low renal toxicity.