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1. 发明授权

US08415336B2 Cyclic (aza)indolizinecarboxamides, their preparation and their use as pharmaceuticals 有权
标题翻译：环状（氮杂）中氮茚甲酰胺，它们的制备及其作为药物的用途
公开(公告)号：US08415336B2
公开(公告)日：2013-04-09
申请号：US13353889
申请日：2012-01-19
申请人： Henning Steinhagen , Bodo Scheiper , Hans Matter , Gary McCort , Guillaume Begis , Pascale Goberville , Berangere Thiers
发明人： Henning Steinhagen , Bodo Scheiper , Hans Matter , Gary McCort , Guillaume Begis , Pascale Goberville , Berangere Thiers
IPC分类号： A61K31/496 , A61K31/5025 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, Ra, R10, R20, R30, R40, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式Ⅰa和Ⅰb的环吲哚嗪甲酰胺和氮杂吲哚烷甲酰胺，其中R，Ra，R10，R20，R30，R40，Y，n，p和q具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体地说，它们抑制酶肾素并调节肾素 - 血管紧张素系统的活性，并且可用于治疗例如高血压等疾病。本发明还涉及制备式Ia和Ib化合物的方法，其用途和包含它们的药物组合物。

2. 发明授权

US5371227A Quinoline derivatives, process for their preparation, and their therapeutic applications 失效
标题翻译：喹啉衍生物，其制备方法及其治疗应用
公开(公告)号：US5371227A
公开(公告)日：1994-12-06
申请号：US39828
申请日：1993-03-30
申请人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
发明人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
IPC分类号： C07D215/12 , C07D401/14
CPC分类号： C07D401/14 , C07D215/12
摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy --(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.
摘要翻译：本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示，氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基 - （C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

3. 发明申请

US20130131034A1 DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译：氨基酸衍生物，其制备及其在治疗中的应用
公开(公告)号：US20130131034A1
公开(公告)日：2013-05-23
申请号：US13582171
申请日：2011-03-01
申请人： Markus Follmann , Pascale Goberville , Stéphanie Hachtel , Gerhard Hessler , Heinz-Werner Kleemann , Thomas Maier , Gary MC Cort , Carsten Struebing , Bérangère Thiers , Li-Hsing Wang
发明人： Markus Follmann , Pascale Goberville , Stéphanie Hachtel , Gerhard Hessler , Heinz-Werner Kleemann , Thomas Maier , Gary MC Cort , Carsten Struebing , Bérangère Thiers , Li-Hsing Wang
IPC分类号： C07D487/08 , C07D295/096 , C07D205/04 , C07D243/08 , C07D411/12 , C07D211/56 , C07D401/12
CPC分类号： C07D487/08 , C07D205/04 , C07D207/08 , C07D211/56 , C07D211/58 , C07D243/08 , C07D295/08 , C07D295/096 , C07D401/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D411/12 , C07D413/12
摘要： The instant invention relates to derivatives of formula (I) and their application in therapeutics.
摘要翻译：本发明涉及式（I）的衍生物及其在治疗中的应用。

4. 发明授权

US5432283A Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US5432283A
公开(公告)日：1995-07-11
申请号：US295469
申请日：1994-08-25
申请人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
发明人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
IPC分类号： C07D215/12 , C07D401/14 , C07D403/10 , C07D215/16
CPC分类号： C07D401/14 , C07D215/12
摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.
摘要翻译：本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示，氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基（C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

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