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1. 发明授权

US5719141A 2,9-diamino- and 2-amino-8-carbamoyl-4-hydroxy-alkanoic acid amide derivatives 失效
标题翻译： 2,9-二氨基 - 和2-氨基-8-氨基甲酰基-4-羟基 - 链烷酰胺衍生物
公开(公告)号：US5719141A
公开(公告)日：1998-02-17
申请号：US525254
申请日：1995-09-08
申请人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
发明人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5355 , A61K31/538 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61P9/12 , C07C237/04 , C07C237/06 , C07C237/22 , C07C271/20 , C07C271/22 , C07D207/00 , C07D209/00 , C07D209/08 , C07D209/42 , C07D211/00 , C07D211/34 , C07D211/60 , C07D213/40 , C07D213/75 , C07D213/89 , C07D215/00 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/04 , C07D235/06 , C07D235/08 , C07D239/70 , C07D239/74 , C07D241/00 , C07D241/36 , C07D241/44 , C07D265/28 , C07D265/34 , C07D265/36 , C07D279/12 , C07D279/14 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D411/02 , C07D413/02
CPC分类号： C07D213/40 , C07C237/06 , C07C237/22 , C07C271/20 , C07D209/08 , C07D209/42 , C07D211/34 , C07D213/89 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/06 , C07D239/74 , C07D241/44 , C07D265/36 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.
摘要翻译：其中R 1是芳基氨基，N-芳基-N-（低级烷氧基 - 低级烷基） - 氨基，N-芳基-N-芳基 - 低级烷基 - 氨基或杂环基的式I化合物（I）环碳原子，X是羰基或亚甲基，R2和R3彼此独立地是氢或低级烷基，或者与它们所键合的碳原子一起是亚环烷基，R4是氢，低级烷基，低级烷酰基或低级烷氧基羰基，R5是羟基，低级烷酰氧基或低级烷氧基羰基氧基，R6是氢，低级烷基，低级烯基，低级炔基，环烷基，环烷基 - 低级烷基，具有5-7个环原子的芳基 - 低级烷基或杂芳基 - 低级烷基在杂芳基环中，R 7为氢或低级烷基，或者R 6和R 7与它们所键合的碳原子一起为环亚烷基，R 8表示脂族，脂环族 - 脂族或杂芳基脂肪族基团，它们的盐可以是用作治疗药物的有效成分 t的高血压。

2. 发明授权

US10189813B2 Formylated N-heterocyclic derivatives as FGFR4 inhibitors 有权
公开(公告)号：US10189813B2
公开(公告)日：2019-01-29
申请号：US15561189
申请日：2016-03-23
申请人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Thomas Knoepfel , Catherine Leblanc , Robert Mah
发明人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Thomas Knoepfel , Catherine Leblanc , Robert Mah
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4427 , C07D213/75 , C07D405/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

3. 发明授权

US09802917B2 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide 有权
公开(公告)号：US09802917B2
公开(公告)日：2017-10-31
申请号：US15073766
申请日：2016-03-18
申请人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Bo Han , Thomas Knöpfel , Catherine Leblanc , Lv Liao , Robert Mah , Franck Mallet , Julie Martz , Can Wang , Jing Xiong , Xianglin Zhao
发明人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Bo Han , Thomas Knöpfel , Catherine Leblanc , Lv Liao , Robert Mah , Franck Mallet , Julie Martz , Can Wang , Jing Xiong , Xianglin Zhao
IPC分类号： A61K31/496 , C07D471/04 , C07D401/14 , C07C51/41 , C07C59/265
CPC分类号： C07D401/14 , C07B2200/13 , C07C51/412 , C07C59/265 , C07D471/04
摘要： The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.

4. 发明授权

US08324235B2 Heterocyclic spiro-compounds 失效
标题翻译：杂环螺环化合物
公开(公告)号：US08324235B2
公开(公告)日：2012-12-04
申请号：US12450521
申请日：2008-03-27
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Bibia Bennacer
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Bibia Bennacer
IPC分类号： A61K31/4188 , C07D401/14 , C07D235/02
CPC分类号： C07D491/20
摘要： The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中R，R 1，R 2，Q，T，n和p具有在说明书中更详细阐述的定义，涉及其制备方法和使用这些化合物作为药物，特别是作为醛固酮合成酶抑制剂。

5. 发明授权

US08071774B2 Heterocyclic spiro-compounds as aldosterone synthase inhibitors 失效
标题翻译：杂环螺环化合物作为醛固酮合成酶抑制剂
公开(公告)号：US08071774B2
公开(公告)日：2011-12-06
申请号：US11921311
申请日：2006-05-30
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Nathalie Jotterand , Christoph Schumacher , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Nathalie Jotterand , Christoph Schumacher , Michael Quirmbach
IPC分类号： C07D491/20 , A61K31/438
CPC分类号： C07D471/04 , C07D471/10 , C07D491/10
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R1, R2, U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中A，R，R 1，R 2，U，V，W，X，Y，Z，n和p具有在描述中更详细阐述的定义，其制备方法和使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

6. 发明授权

US08071773B2 Heterocyclic spiro-compounds as aldosterone synthase inhibitors 失效
标题翻译：杂环螺环化合物作为醛固酮合成酶抑制剂
公开(公告)号：US08071773B2
公开(公告)日：2011-12-06
申请号：US11921312
申请日：2006-05-30
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Nathalie Jotterand , Christoph Schumacher , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Nathalie Jotterand , Christoph Schumacher , Michael Quirmbach
IPC分类号： C07D471/20 , A61K31/438 , A61K31/437
CPC分类号： C07D471/20
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中R，R 1，R 2，W，X，Y，Z和n具有在说明书中更详细阐述的定义，及其制备方法使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

7. 发明授权

US08022068B2 Substituted piperidines as renin inhibitors 失效
公开(公告)号：US08022068B2
公开(公告)日：2011-09-20
申请号：US12865930
申请日：2009-02-06
申请人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Robert Mah , Vincenzo Tschinke
发明人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Robert Mah , Vincenzo Tschinke
IPC分类号： C07D413/12 , C07D413/14 , A61K31/445
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.

8. 发明申请

US20110212950A1 4,4-DISUBSTITUTED PIPERIDINES 审中-公开
标题翻译： 4,4-取代的哌啶
公开(公告)号：US20110212950A1
公开(公告)日：2011-09-01
申请号：US12734321
申请日：2008-10-24
申请人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
发明人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
IPC分类号： A61K31/538 , C07D413/12 , C07D413/14 , A61P9/00
CPC分类号： C07D413/12 , C07D413/14
摘要： The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R2, has the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式（I）的4,4-二取代哌啶及其盐，优选其药学上可接受的盐，其中R2具有说明书中所述的含义，其制备方法和这些化合物的用途作为药物，特别是作为肾素抑制剂。

9. 发明申请

US20110144197A1 ALCANOIC ACID AMIDES SUBSTITUTED BY SATURATED O-HETEROCYCLES 审中-公开
标题翻译：饱和脂肪酸取代的氨基酸
公开(公告)号：US20110144197A1
公开(公告)日：2011-06-16
申请号：US13030419
申请日：2011-02-18
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
IPC分类号： A61K31/341 , C07D307/14 , C07D309/06 , A61K31/351 , C07D307/00 , A61K31/343 , C07D307/93 , A61P9/00 , A61P27/06 , A61P9/12 , A61P9/10 , A61P13/12
CPC分类号： A61K31/335
摘要： Compounds of the general formula (formula I) in which the meanings of the substituents R1 and R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：取代基R 1和R 6的含义如权利要求1所示的通式（式I）的化合物具有肾素抑制性质，可用作药物。

10. 发明申请

US20100311714A1 1H-IMIDAZO[4,5-c]QUINOLINONE COMPOUNDS 审中-公开
标题翻译： 1H-咪唑并[4,5-c]喹啉酮化合物
公开(公告)号：US20100311714A1
公开(公告)日：2010-12-09
申请号：US12792187
申请日：2010-06-02
申请人： Pascal Furet , Patricia Imbach , Robert Mah , Frédéric Stauffer
发明人： Pascal Furet , Patricia Imbach , Robert Mah , Frédéric Stauffer
IPC分类号： A61K31/437 , C07D471/04 , A61K31/506 , A61K31/497 , A61P35/04
CPC分类号： C07D471/04 , C07D471/14
摘要： The invention relates to the use of 1H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone compounds.
摘要翻译：本发明涉及1H-咪唑并[4,5-c]喹啉酮化合物及其盐在治疗蛋白质和/或脂质激酶依赖性疾病中的用途以及用于制备用于治疗所述疾病的药物制剂; 用于治疗蛋白质和/或脂质激酶依赖性疾病的1H-咪唑并[4,5-c]喹啉酮化合物; 一种治疗所述疾病的方法，包括将1H-咪唑并[4,5-c]喹啉酮化合物给予温血动物，特别是人; 包括1H-咪唑并[4,5-c]喹啉酮化合物的药物制剂，特别是用于治疗蛋白质和/或脂质激酶依赖性疾病; 新的1H-咪唑并[4,5-c]喹啉酮化合物; 以及制备新型1H-咪唑并[4,5-c]喹啉酮化合物的方法。

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