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公开(公告)号:US5364768A
公开(公告)日:1994-11-15
申请号:US940784
申请日:1992-09-04
IPC分类号: C07D499/88 , C12P37/00
CPC分类号: C07D499/88
摘要: An in vitro process for preparing 6((1R)-hydroxyethyl) penem acids by hydrolyzing the carboxylic ester derivative thereof using an enzyme capable of selectively hydrolyzing the ester group at the 3-position of the carboxylic acid ester using an esterase, acylase or lipase enzyme, wherein the enzymatic hydrolysis is effected at a pH in the range of from 5 to 8 and at a temperature in the range of 20.degree. C. to 40.degree. C.
摘要翻译: 通过使用能够使用酯酶,酰基转移酶或脂肪酶选择性水解羧酸酯的3位的酯基的酶来水解其羧酸酯衍生物来制备6((1R) - 羟乙基)青霉烯酸的体外方法 酶,其中酶水解在5至8范围内的温度和20℃至40℃的温度下进行。
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公开(公告)号:US5362740A
公开(公告)日:1994-11-08
申请号:US983274
申请日:1992-11-30
申请人: Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Silvia De Bernardinis , Marcello Marchi , Mario Varasi
发明人: Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Silvia De Bernardinis , Marcello Marchi , Mario Varasi
IPC分类号: A61K31/435 , A61K31/4375 , A61K31/439 , A61K31/46 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P29/00 , A61P43/00 , C07D451/04 , C07D451/14 , C07D453/06 , C07D455/02 , C07D471/08 , C07D413/00 , A61K31/44
CPC分类号: C07D451/04 , C07D451/14 , C07D453/06 , C07D455/02 , C07D471/08
摘要: A compound of formula (I) ##STR1## wherein R' is hydrogen or methyl, m is zero or 1 and the symbol means that the azabicyclic rings may be in the .alpha. or the .beta. orientation, and the pharmaceutically acceptable salts thereof, are useful in treating CNS disorders, gut motility disorders, and/or emesis and/or pain in mammals, and/or migraine.
摘要翻译: 式(I)化合物其中R'为氢或甲基,m为0或1,符号表示氮杂双环可以是α或β取向,并且药学上 可接受的盐可用于治疗哺乳动物和/或偏头痛中的CNS紊乱,肠蠕动障碍和/或呕吐和/或疼痛。
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公开(公告)号:US5360904A
公开(公告)日:1994-11-01
申请号:US927511
申请日:1992-09-21
申请人: Angelo Bedeschi , Walter Cabri , Marcello Marchi , Ettore Perrone
发明人: Angelo Bedeschi , Walter Cabri , Marcello Marchi , Ettore Perrone
IPC分类号: C07C67/307 , C07C67/313 , C07D205/09 , C07D499/00 , C07D499/06 , C07D499/88 , C07D499/883 , C07D499/893 , C07D499/897 , C07F7/10
CPC分类号: C07D205/09 , C07C67/307 , C07C67/313 , C07D499/88 , Y02P20/55
摘要: A process for preparing penem esters by reacting ##STR1## wherein R.sub.1 is a hydroxy protecting group and X is a C.sub.1 -C.sub.10 alkyl or aryl group, with ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 -C.sub.6 alkyl group in the presence of an anhydrous organic solvent, condensing the product with ##STR3## wherein X is a halogen atom or a --OCOOR.sub.3 group and then cyclizing.
摘要翻译: PCT No.PCT / EP91 / 00522 Sec。 371日期:1992年9月21日 102(e)日期1992年9月21日PCT 1991年3月18日PCT公布。 WO91 / 14691 PCT出版物 (II)其中R 1是羟基保护基,X是C 1 -C 10烷基或芳基,其中R 2是(C 1 -C 10)烷基或芳基, 氢或C1-C6烷基,在无水有机溶剂的存在下,将产物与-OCOOR 3基团缩合,然后环化。
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