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31. 发明申请

US20130072519A1 2-PHENYL BENZOYLAMIDES 审中-公开
标题翻译： 2-苯基苯甲酰胺
公开(公告)号：US20130072519A1
公开(公告)日：2013-03-21
申请号：US13699230
申请日：2011-05-09
申请人： Edward Lee Conn , David Hepworth , Yingmei Qi , Benjamin Neil Rocke , Roger Benjamin Ruggeri , Yan Zhang
发明人： Edward Lee Conn , David Hepworth , Yingmei Qi , Benjamin Neil Rocke , Roger Benjamin Ruggeri , Yan Zhang
IPC分类号： C07D307/83 , A61K31/4035 , A61K31/435 , C07C235/84 , A61K31/216 , C07D221/04 , C07D209/44 , A61K31/343
CPC分类号： C07D307/83 , A61K31/216 , A61K31/343 , A61K31/4035 , A61K31/435 , C07C235/84 , C07D209/44 , C07D209/49 , C07D221/04 , C07D307/88 , C07D401/12 , C07D471/04
摘要： Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
摘要翻译：本文描述抑制微粒体甘油三酯转运蛋白（MTP）和/或载脂蛋白B（Apo B）分泌的式I化合物及其在治疗与动物相关疾病中的用途。

32. 发明授权

US08362073B2 Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的稠环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：US08362073B2
公开(公告)日：2013-01-29
申请号：US12939650
申请日：2010-11-04
申请人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
发明人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
IPC分类号： A61K31/166 , C07C231/02
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50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。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

33. 发明授权

US08133514B2 Carbon-substituted diketopiperazine delivery systems 失效
标题翻译：碳取代二酮哌嗪递送系统
公开(公告)号：US08133514B2
公开(公告)日：2012-03-13
申请号：US12473192
申请日：2009-05-27
申请人： Samuel J. Milstein
发明人： Samuel J. Milstein
IPC分类号： A61K9/14
CPC分类号： A61K9/5031 , A61K9/1617 , A61K31/35 , A61K31/70 , A61K38/16 , A61K38/21 , A61K38/28 , C07C229/42 , C07C233/55 , C07C233/63 , C07C233/87 , C07C235/38 , C07C235/64 , C07C235/84 , C07C237/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , Y10S977/906 , Y10S977/926
摘要： Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.
摘要翻译：提供了用于递送活性剂的组合物。这些递送组合物包括（a）活性剂; 和（b）至少一个单C取代或二-C取代的二酮哌嗪的载体。还提供了制备这些组合物并施用这些组合物的方法。

34. 发明申请

US20110152290A1 ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLAMINO-取代的氟化环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：US20110152290A1
公开(公告)日：2011-06-23
申请号：US12939650
申请日：2010-11-04
申请人： Matthias SCHAEFER , Josef PERNERSTORFER , Dieter KADEREIT , Hartmut STROBEL , Werngard CZECHTIZKY , L. Charlie CHEN , Alena SAFAROVA , Aleksandra WEICHSEL , Marcel PATEK
发明人： Matthias SCHAEFER , Josef PERNERSTORFER , Dieter KADEREIT , Hartmut STROBEL , Werngard CZECHTIZKY , L. Charlie CHEN , Alena SAFAROVA , Aleksandra WEICHSEL , Marcel PATEK
IPC分类号： A61K31/495 , C07C69/757 , A61K31/216 , C07C62/14 , A61K31/196 , C07D213/36 , A61K31/4409 , C07D209/12 , A61K31/405 , C07D307/12 , A61K31/341 , C07D211/22 , A61K31/445 , C07D261/04 , A61K31/42 , C07D451/02 , A61K31/46 , C07D241/04 , C07D235/12 , A61K31/4184 , C07D263/32 , A61K31/421 , C07D417/04 , A61K31/426 , C07D285/06 , A61K31/433 , A61P9/00 , A61P29/00 , A61P13/12 , A61P35/00 , A61P19/00 , A61P11/00 , A61P25/00 , A61P17/06
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50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。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

35. 发明授权

US07910621B2 Small molecule antagonists of XIAP family proteins 失效
标题翻译： XIAP家族蛋白的小分子拮抗剂
公开(公告)号：US07910621B2
公开(公告)日：2011-03-22
申请号：US10594200
申请日：2005-03-22
申请人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
发明人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
IPC分类号： A61K31/352 , C07D311/30
CPC分类号： C07C235/84 , C07C50/28 , C07C50/30 , C07D311/30
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
摘要翻译：本发明涉及XIAP家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了塞林和其他XIAP抑制剂以及使用这些化合物作为XIAP家族蛋白的抗凋亡作用的拮抗剂的方法。本发明还提供了治疗疾病和病理（例如肿瘤性疾病）的方法。

36. 发明申请

US20110009638A1 METHOD FOR PREPARING 3-TRIFLUOROMETHYL CHALCONES 有权
标题翻译：制备3-三氟甲基吡咯烷酮的方法
公开(公告)号：US20110009638A1
公开(公告)日：2011-01-13
申请号：US12933493
申请日：2009-04-08
申请人： Gary David Annis
发明人： Gary David Annis
IPC分类号： C07D213/56 , C07D249/08 , C07D231/14 , C07D231/12 , C07D261/04 , C07C51/347 , C07C231/12 , C07D277/30 , C07C67/327 , C07C45/74 , C07C303/30 , C07C209/68 , C07C253/30 , C07C45/68 , C07C49/80 , C07C25/13
CPC分类号： C07D261/04 , C07C17/35 , C07C25/13 , C07C45/455 , C07C45/70 , C07C49/80 , C07C49/813 , C07C67/343 , C07C205/45 , C07C209/74 , C07C231/12 , C07C231/14 , C07C235/84 , C07D213/40 , C07D231/12 , C07D231/14 , C07D231/16 , C07D249/08 , C07D249/10 , C07D277/28 , C07C69/94 , C07C69/76 , C07C211/56
摘要： Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.
摘要翻译：公开了一种制备式1化合物的方法，其中Q和Z如本公开中所定义，包括从包含式2化合物，式3化合物，包含至少一种选自由式4的碱土金属氢氧化物组成的组，其中M是Ca，Sr或Ba，式4a的碱金属碳酸盐，其中M1是Li，Na或K，1,5-二氮杂双环[4.3.0]壬-5-烯和 1,8-二氮杂双环[5.4.0]十一碳-7-烯，以及能够与水形成低沸点共沸物的非质子传递溶剂。还公开了制备式2化合物的方法，其包括（1）形成反应混合物，该反应混合物包含衍生自在存在下使式5的化合物（其中X为Cl，Br或I）与镁金属或烷基卤化镁接触的格利雅试剂的醚溶剂，然后（2）使反应混合物与式6化合物（其中Y是OR 11或NR 12 R 13）和R 11，R 12和R 13如本公开所定义。进一步公开的是制备式7化合物的方法，其中Q和Z如本公开所定义，使用式1的化合物，其特征在于通过上述方法制备式1化合物或使用制备的式1化合物通过上述方法。

37. 发明申请

US20100261760A1 EP2 Receptor Agonists 审中-公开
标题翻译： EP2受体激动剂
公开(公告)号：US20100261760A1
公开(公告)日：2010-10-14
申请号：US12820752
申请日：2010-06-22
申请人： Alexander William Oxford , Richard John Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
发明人： Alexander William Oxford , Richard John Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
IPC分类号： A61K31/4439 , A61K31/4418 , A61K31/381 , A61K31/36 , A61K31/341 , C07D401/12 , C07D213/81 , C07D333/38 , C07D407/10 , C07D307/54 , A61P13/12 , A61P15/00 , A61P27/06 , A61P19/10 , A61P11/06 , A61P37/00
CPC分类号： C07D213/81 , C07C233/75 , C07C233/81 , C07C235/84 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要： The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.
摘要翻译：本公开提供EP2受体激动剂化合物和使用该化合物治疗可通过EP2受体激动作用缓解的病症的方法。

38. 发明申请

US20100144876A1 MODULATOR 有权
标题翻译：调制器
公开(公告)号：US20100144876A1
公开(公告)日：2010-06-10
申请号：US12707812
申请日：2010-02-18
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： A61K31/221 , A61K31/192 , A61K31/166 , A61K31/194 , A61P25/28 , A61P21/02 , A61P13/10
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO2，CN，COR3，COOR3，NR3R4，CONR3R4，SO3H，SO2-R3，SO2NR3R4和CF3的极性官能团，其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，X-Y不是间位-C≡-C-（CH 2）2 CO 2 H，间-C≡C-（CH 2）（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位-C≡C-（CH 2）4 OH。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

39. 发明申请

US20100137612A1 METHOD FOR PRODUCTION OF 3-HYDROXYPROPAN-1-ONE COMPOUND FOR PRODUCTION OF 2- PROPEN-1-ONE COMPOUND AND METHOD FOR PRODUCTION OF ISOXAZLINE COMPOUND 有权
标题翻译：用于生产2-丙烯-1-酮化合物的3-羟基丙-1-酮化合物的生产方法和生产ISOXAZLINE化合物的方法
公开(公告)号：US20100137612A1
公开(公告)日：2010-06-03
申请号：US12452347
申请日：2008-06-27
申请人： Manabu Yaosaka , Tomohisa Utsunomiya , Yuji Moriyama , Tomohiro Matsumoto , Kazutaka Matoba
发明人： Manabu Yaosaka , Tomohisa Utsunomiya , Yuji Moriyama , Tomohiro Matsumoto , Kazutaka Matoba
IPC分类号： C07D261/04 , C07C63/06 , C07C45/61
CPC分类号： C07C45/72 , C07C45/66 , C07C45/74 , C07C49/83 , C07C49/835 , C07C51/353 , C07C51/367 , C07C51/377 , C07C65/40 , C07C67/327 , C07C67/343 , C07C67/347 , C07C69/65 , C07C231/12 , C07C253/30 , C07C319/20 , C07D213/30 , C07D213/50 , C07D213/61 , C07D233/14 , C07D249/08 , C07D261/04 , C07D401/04 , C07C323/22 , C07C235/84 , C07C255/56 , C07C69/76 , C07C49/813 , C07C65/38
摘要： There is provided a novel intermediate for producing pesticides. A method for producing 1,3-bis(substituted phenyl)-3-substituted-3-hydroxypropan-1-one compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method for producing 1,3-bis(substituted phenyl)-3-substituted-2-propen-2-one compound of Formula (2) comprises dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
摘要翻译：提供了一种生产农药的新型中间体。制备式（3）的1,3-双（取代的苯基）-3-取代-3-羟基丙-1-酮化合物的方法包括使式（4）的芳族酮化合物与式（4）的取代的苯乙酮化合物 5）作为起始原料在有机溶剂或水中，在存在或不存在添加剂的情况下，在悬浮状态的碱存在下进行。制备式（2）的1,3-双（取代的苯基）-3-取代-2-丙烯-2-酮化合物的方法包括使式（3）的化合物脱水。一步法制备化合物（2）的方法包括使化合物（4）和化合物（5）反应得到化合物（3）。此外，制备式（1）的异恶唑啉化合物的方法包括使任选被卤素原子取代的脂族或芳族烃溶剂中的化合物（2）与羟胺反应，加入选自相转移催化剂，C1-C6醇和非质子极性溶剂在碱和水的存在下反应。

40. 发明授权

US07713963B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US07713963B2
公开(公告)日：2010-05-11
申请号：US11548501
申请日：2006-10-11
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

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