Sulfur-containing compounds method for their use and prodction

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United States of America Patent

PATENT NO 5783703
SERIAL NO

08795428

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Abstract

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A first embodiment of the invention relates to novel carbapenem compounds, (1R, 5S, 6S)-2-?1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-?(R)-1-hydroxy-ethyl!-1-methylcarbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a ?1-(1,3-thia-zolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, --COO.sup..crclbar. or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections. The second embodiment of the invention relates to 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine represented by the following formula and its acid addition salts ##STR2## and to the production process therefor. The above compounds are useful as intermediates for preparing carbapenem compounds, which have strong antibacterial activity, with convenience and high yield.

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PFIZER JAPAN INC3-22-7 YOYOGI SHIBUYA-KU TOKYO

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Abe, Takao Sakado, JP 178 2310
Hayashi, Kazuhiko Saitama-ken, JP 176 2164
Isoda, Takeshi Sayama, JP 87 885
Kumagai, Toshio Kawagoe, JP 163 2292
Mihira, Ado Asaka, JP 8 28
Sato, Chisato Kamifukuoka, JP 7 28
Tamai, Satoshi Kawasaki, JP 42 234

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