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1. 发明授权

US07629346B2 Pyrazinecarboxamide derivatives as CB1 antagonists 失效
标题翻译：吡嗪甲酰胺衍生物作为CB1拮抗剂
公开(公告)号：US07629346B2
公开(公告)日：2009-12-08
申请号：US11809047
申请日：2007-05-30
申请人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
IPC分类号： A61K31/4965 , A61K31/497
CPC分类号： C07D241/26 , C07D241/24 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及式I化合物：其中R 1至R 8如说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

2. 发明授权

US5804577A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5804577A
公开(公告)日：1998-09-08
申请号：US708161
申请日：1996-08-27
申请人： Paul Hebeisen , Ingrid Heinze-Krauss , Hans Richter , Valeri Runtz , Henri Stalder , Urs Weiss , George Petros Yiannikouros
发明人： Paul Hebeisen , Ingrid Heinze-Krauss , Hans Richter , Valeri Runtz , Henri Stalder , Urs Weiss , George Petros Yiannikouros
IPC分类号： C07D501/24 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/56 , C07D501/34
CPC分类号： C07D501/00
摘要： The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily hydroyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1是选自2-，3-和4-羟基苯基，3-硝基苯基和3-氟-4-羟基苯基的基团; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。

3. 发明授权

US4680408A Acyl derivatives 失效
标题翻译：酰基衍生物
公开(公告)号：US4680408A
公开(公告)日：1987-07-14
申请号：US872320
申请日：1986-06-09
申请人： Roland Reiner , Urs Weiss
发明人： Roland Reiner , Urs Weiss
IPC分类号： C07D293/06 , C07D501/20 , C07D505/00
CPC分类号： C07D293/06 , C07D505/00
摘要： There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
摘要翻译：呈现下式的化合物其中R 1是可用于头孢菌素化学的3-取代基之一，R 2是氢，低级烷基或COOR 3 - 低级烷基，其中R 3是氢，碱的阳离子或容易的可水解的酯基，X是硫，氧或-SO-和-SO2-基团之一，以及易水解的酯，这些化合物的易水解的醚和盐以及式I化合物或其酯的水合物，醚和盐也是用于制造这些化合物的方法以及用于其制造的化合物。

4. 发明申请

US20070293509A1 Pyrazinecarboxamide derivatives as CB1 antagonists 失效
标题翻译：吡嗪甲酰胺衍生物作为CB1拮抗剂
公开(公告)号：US20070293509A1
公开(公告)日：2007-12-20
申请号：US11809047
申请日：2007-05-30
申请人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
IPC分类号： A61K31/497 , A61K31/4965 , A61P1/00 , A61P3/04 , A61P3/10 , C07D241/10 , C07D419/02
CPC分类号： C07D241/26 , C07D241/24 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及式I化合物：其中R 1至R 8如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

5. 发明授权

US5935950A Cephalosporin pyridinium derivatives 失效
标题翻译：头孢菌素吡啶衍生物
公开(公告)号：US5935950A
公开(公告)日：1999-08-10
申请号：US924626
申请日：1997-09-05
申请人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Urs Weiss
发明人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Urs Weiss
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/16 , C07D501/24 , C07D501/56
CPC分类号： C07D501/00 , Y02P20/55
摘要： Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, cycloalkyl or acetyl;x is CH or N;n is 0, 1 or 2;m is 0 or 1;R.sup.2 is hydrogen, lower alkyl, .omega.-hydroxy alkyl, benzyl or lower alkyl-heterocyclyl, the benzyl and the heterocyclyl group being unsubstituted or substituted with at least one of the groups amino, cyano, carboxy, halogen, hydroxy, lower alkyl, lower alkoxy or --CONR.sub.2, where R is hydrogen or lower alkyl; or R.sup.2 is --CH.sub.2 CONR.sup.4 R.sup.5 ; whereinR.sup.4, R.sup.5 are each independently hydrogen, .omega.-hydroxy-alkyl, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl groups being unsubstituted or substituted with at least one of the groups optionally protected hydroxy, halogen, optionally substituted lower alkyl, optionally substituted lower alkoxy, .omega.-hydroxyalkyl or cyano; or R.sup.4 and R.sup.5 form together a group of formula ##STR2## with the proviso that when pyridinium ring A is pyridinium-4-yl, m is 1; as well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. These compounds are useful as parenteral antibiotics.
摘要翻译：其中R1是氢，低级烷基，环烷基或乙酰基的式Ⅰ化合物; x是CH或N; n为0,1或2; m为0或1; R2是氢，低级烷基，ω-羟基烷基，苄基或低级烷基 - 杂环基，苄基和杂环基是未取代的或被至少一个氨基，氰基，羧基，卤素，羟基，低级烷基，低级烷氧基或-CONR2，其中R是氢或低级烷基; 或R 2为-CH 2 CONR 4 R 5; 其中R 4，R 5各自独立地为氢，ω-羟基 - 烷基，苯基，苄基，萘基或杂环基，苯基，苄基，萘基或杂环基为未取代的或被至少一个选自羟基，卤素，取代的低级烷基，任选取代的低级烷氧基，ω-羟烷基或氰基; 或R 4和R 5一起形成式的基团，条件是当吡啶鎓环A为吡啶鎓-4-基时，m为1; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。这些化合物可用作胃肠外抗生素。

6. 发明授权

US4593093A Acyl derivatives 失效
公开(公告)号：US4593093A
公开(公告)日：1986-06-03
申请号：US600249
申请日：1984-04-16
申请人： Roland Reiner , Urs Weiss
发明人： Roland Reiner , Urs Weiss
IPC分类号： C07D293/06 , C07D501/20 , C07D501/24 , C07D505/00 , C07D421/14
CPC分类号： C07D505/00 , C07D293/06
摘要： There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --,and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.

7. 发明授权

US4458072A Acyl derivatives 失效
标题翻译：酰基衍生物
公开(公告)号：US4458072A
公开(公告)日：1984-07-03
申请号：US305870
申请日：1981-09-28
申请人： Roland Reiner , Urs Weiss
发明人： Roland Reiner , Urs Weiss
IPC分类号： C07D293/06 , C07D501/20 , C07D501/24 , C07D505/00 , C07D51/56 , A61K31/545
CPC分类号： C07D505/00 , C07D293/06
摘要： There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
摘要翻译：呈现下式的化合物其中R 1是可用于头孢菌素化学的3-取代基之一，R 2是氢，低级烷基或COOR 3 - 低级烷基，其中R 3是氢，碱的阳离子或容易的可水解的酯基，X是硫，氧或-SO-和-SO2-基团之一，以及易水解的酯，这些化合物的易水解的醚和盐以及式I化合物或其酯的水合物，醚和盐也是用于制造这些化合物的方法以及用于其制造的化合物。

8. 发明授权

US5359057A Acylation of amines 失效
标题翻译：胺的酰化
公开(公告)号：US5359057A
公开(公告)日：1994-10-25
申请号：US822173
申请日：1992-01-16
申请人： Andre Furlenmeier , Urs Weiss
发明人： Andre Furlenmeier , Urs Weiss
IPC分类号： C07D277/74 , C07D499/00 , C07D501/06 , C07D499/12
CPC分类号： C07D499/00 , C07D277/74
摘要： There is described a process for the manufacture of carboxylic acid amides by acylating amines with 2-benzothiazolyl thioesters of carboxylic acids, which process comprises reacting the amine in the form of an acid addition salt. This process is especially of great advantage when the amine is not particularly stable in the form of the free base, which is frequently the case especially with 7-aminocephalosporin derivatives. 7-Acylamino-cephalosporin derivatives can be manufactured in good yield and in high purity with the novel process.
摘要翻译：描述了通过用羧酸的2-苯并噻唑基硫酯将胺酰化而制备羧酸酰胺的方法，该方法包括以酸加成盐的形式使胺反应。当胺不是游离碱的形式不是特别稳定时，这个过程尤为重要，特别是7-氨基头孢菌素衍生物。 7-酰氨基 - 头孢菌素衍生物可通过新方法以良好的产率和高纯度制备。

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