公开(公告)号：US20110118229A1

公开(公告)日：2011-05-19

申请号：US12742966

申请日：2008-11-18

申请人： Young-Ro Choi ,  Bong-Jin Kim ,  Bok-Ju Song ,  Bum-Soo Lee ,  Dong-Woo Lee ,  Dong-Geun Seo ,  Young-Cheol Jeong ,  Si-Min Kim ,  Jee-Woong Kwon ,  Jae-Yang Kong ,  Heeyeong Cho

发明人： Young-Ro Choi ,  Bong-Jin Kim ,  Bok-Ju Song ,  Bum-Soo Lee ,  Dong-Woo Lee ,  Dong-Geun Seo ,  Young-Cheol Jeong ,  Si-Min Kim ,  Jee-Woong Kwon ,  Jae-Yang Kong ,  Heeyeong Cho

IPC分类号： A61K31/407 ,  C07D477/20 ,  C07D477/08 ,  C07D477/06 ,  A61P31/04

CPC分类号： C07D477/20

摘要： The present invention provides a 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives or their pharmaceutically acceptable salts show high oral absorption rate, and thus can be orally administered. The active metabolites thereof have a broad spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against methicillin-resistant Staphylococcus aurus (MRSA) and quinolone-resistant strains (QRS). In particular, the acid addition salts of the 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives are obtained in crystalline forms having excellent stability.

摘要翻译： 本发明提供2-芳基甲基氮杂环丁烷 - 碳青霉烯-3-羧酸酯衍生物或其药学上可接受的盐，其制备方法和包含其的药物组合物。 2-芳基甲基氮杂环丁烷 - 碳青霉烯-3-羧酸酯衍生物或其药学上可接受的盐显示出高的口服吸收率，因此可以口服给药。 其活性代谢物对革兰氏阳性和革兰氏阴性菌具有广谱的抗菌活性，对耐甲氧西林金黄色葡萄球菌（MRSA）和喹诺酮耐药菌株（QRS）具有优异的抗菌活性。 特别地，2-芳基甲基氮杂环丁烷 - 碳青霉烯-3-羧酸酯衍生物的酸加成盐以稳定性优异的结晶形式得到。

公开(公告)号：US20100274003A1

公开(公告)日：2010-10-28

申请号：US12733674

申请日：2008-09-17

申请人： Chang-Seob Kim ,  Dong-Woo Lee ,  Jae-Woo Lee ,  Mi-Ran Jung ,  Young-Cheol Jeong ,  Si-Min Kim ,  Young-Ro Choi ,  Dong-Geun Seo ,  Ju-Hee Lee ,  Phil-Sang Ahn

发明人： Chang-Seob Kim ,  Dong-Woo Lee ,  Jae-Woo Lee ,  Mi-Ran Jung ,  Young-Cheol Jeong ,  Si-Min Kim ,  Young-Ro Choi ,  Dong-Geun Seo ,  Ju-Hee Lee ,  Phil-Sang Ahn

IPC分类号： C07D487/04

CPC分类号： C07D477/20 ,  C07C213/04 ,  C07D205/04 ,  C07C215/08

摘要： The present invention provides a process for preparing an acid addition salt of a synthetic intermediate for carbapenem antibiotics and a novel acid addition salt of a synthetic intermediate for carbapenem antibiotics obtained from the process. The present invention also provides a process for preparing a carbapenem antibiotic using the acid addition salt. According to the process of the present invention, an acid addition salt of a synthetic intermediate for carbapenem antibiotics can be prepared in a high yield and high purity, without conducting column chromatography. Thus, the process of the present invention can be applied to mass production with an industrial scale. Furthermore, since the acid addition salts have solid forms, they are easy to handle and keep in a manufacturing site.

摘要翻译： 本发明提供了一种制备碳青霉烯类抗生素合成中间体的酸加成盐的方法和由该方法得到的碳青霉烯类抗生素合成中间体的新型酸加成盐。 本发明还提供了使用酸加成盐制备碳青霉烯类抗生素的方法。 根据本发明的方法，可以以高产率和高纯度制备碳青霉烯类抗生素合成中间体的酸加成盐，而不进行柱层析。 因此，本发明的方法可以应用于工业规模的批量生产。 此外，由于酸加成盐具有固体形式，因此易于处理并保持在制造现场。