发明名称 2-(MONO-OR DI-SUBSTITUTED 6,7-DIHYDRO-5H-PYRAZOLO(1,2-A)PYRAZOLIUM-6-YL)THIOCARBAPENEM DERIVATIVE
摘要 PURPOSE:To obtain the subject compound exhibiting powerful antibacterial activity, also having high resistance to kidney dehydropeptidase and beta-lactamase. CONSTITUTION:A compound of formula I[R<1> and R<2> are such that one of them is H, the other being a (OH-, lower alkoxy-, SH- or NH2-substituted) lower alkyl, carbamoyl, a mono- or di-lower alkyl-substituted amide, or halogen] and a pharmacologically permissible salt thereof, e.g. (1R, 5S, 6S)-2-[(6,7- dihydro-1,3-dimethyl-5H--pyrazolo[1,2-a]pyrazolium-6-yl)thio]-6-[(R)-1- hydroxyethyl]-1-methyl-carbapen-2-em-3-carboxylate. The compound of formula I can be obtained by reaction of a compound of formula II with a 2-substituted or a 1,3-disubstituted 6,7-dihydro-6-mercapto-5H-pyrazolo[1,2-a]pyrazolium salt of formula III to form a compound of formula IV, and then eliminating whose carboxyl protecting group R<3>.
申请公布号 JPH0770139(A) 申请公布日期 1995.03.14
申请号 JP19940170497 申请日期 1994.06.30
申请人 LEDERLE JAPAN LTD 发明人 TAMAI SEI;ISODA TAKETOSHI;MIHIRA ADO;KUMAGAI TOSHIO
分类号 A61K31/415;A61P31/04;C07D519/00 主分类号 A61K31/415
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