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公开(公告)号：US10258626B2
公开(公告)日：2019-04-16
申请号：US15428493
申请日：2017-02-09
发明人： Thierry Le Diguarher , Patrick Casara , Jérôme-Benoît Starck , Jean-Michel Henlin , James Edward Paul Davidson , James Brooke Murray , Christopher John Graham , I-Jen Chen , Olivier Geneste , John Hickman , Stéphane Depil , Arnaud Le Tiran , Mikl{dot over (o)}s Nyerges , Guillaume De Nanteuil
IPC分类号： A61K31/55 , A61K31/475 , A61K31/496 , A61K31/541 , A61K31/553 , A61K31/4725 , A61K31/5377 , A61K31/5383 , C07D491/052 , C07D401/02 , C07D401/12 , A61N5/10 , C07D471/00 , C07D471/04 , C07D487/04 , C07D207/30 , C07D211/06 , C07D211/80 , A61K45/06 , C07D498/04
摘要： Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
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![Synthesis process, and crystalline form of 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy} benzamide hydrochloride and pharmaceutical compositions containing it](/abs-image/US/2015/02/10/US08952179B2/abs.jpg.150x150.jpg)
2.发明授权Synthesis process, and crystalline form of 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy} benzamide hydrochloride and pharmaceutical compositions containing it 有权合成方法和4- {3- [顺式 - 六氢环戊并[c]吡咯-2（1H） - 基]丙氧基}苯甲酰胺盐酸盐和含有它的药物组合物的结晶形式公开(公告)号：US08952179B2
公开(公告)日：2015-02-10
申请号：US14103006
申请日：2013-12-11
发明人： Nicolas Robert , Jean-Michel Lerestif , Jean-Pierre Lecouve , Marina Gaillard , Loic Meunier , Philippe Letellier , Mathieu Boiret
IPC分类号： C07D209/52 , C07C309/63 , C07C235/46 , C07D317/22 , C07D319/06
CPC分类号： C07C309/63 , C07B2200/13 , C07C235/46 , C07D209/52 , C07D317/22 , C07D319/06
摘要： Industrial synthesis process for the compound of formula (I):
摘要翻译： 式（I）化合物的工业合成方法：
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![Process for the resolution of enantiomers of (3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-trien-7-yl)nitrile and application in the synthesis of ivabradine](/abs-image/US/2014/07/15/US08778930B2/abs.jpg.150x150.jpg)
3.发明授权Process for the resolution of enantiomers of (3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-trien-7-yl)nitrile and application in the synthesis of ivabradine 有权解决（3,4-二甲氧基 - 双环[4.2.0]八氢-1,3,5-三烯-7-基）腈的对映异构体的方法，并用于合成伊伐布雷定公开(公告)号：US08778930B2
公开(公告)日：2014-07-15
申请号：US13850514
申请日：2013-03-26
IPC分类号： A61K31/55 , C07D223/10 , C07D223/16 , C07C253/30 , C07C255/47 , C07C209/48
CPC分类号： C07C253/30 , C07C209/48 , C07C255/47 , C07D223/10 , C07D223/16
摘要： Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.
摘要翻译： 式（I）化合物的光学拆分方法：用手性色谱法。 应用于伊伐布雷定的合成，其与药学上可接受的酸及其水合物的加成盐。
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公开(公告)号：US08524949B2
公开(公告)日：2013-09-03
申请号：US13138511
申请日：2010-02-26
申请人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
发明人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
IPC分类号： C07C233/05
CPC分类号： C07C233/18
摘要： The present invention relates to a complex of agomelatine and to preparation thereof. The hydrogen halide complex of agomelatine obtained through the present method is more soluble, more stable, and of higher purity than agomelatine itself, making it more suitable to be used in pharmaceutical preparation. Using this method, product of high purity can be obtained through a simple process, without having to incur further complicated steps.
摘要翻译： 本发明涉及一种阿维菌素及其制备方法。 通过本发明方法获得的agomelatine的卤化氢配合物比agomelatine本身更可溶，更稳定和更高纯度，使其更适合用于制药。 使用这种方法，可以通过简单的工艺获得高纯度的产品，而不必进一步复杂的步骤。
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5.发明授权Indole compounds, a process for their preparation and pharmaceutical compositions containing them 失效吲哚化合物，其制备方法和含有它们的药物组合物公开(公告)号：US08003682B2
公开(公告)日：2011-08-23
申请号：US12311787
申请日：2007-10-17
申请人： Pascal Marchand , Vincent Babonneau , Sylvie Piessard , Muriel Duflos , Jean Albert Boutin , Valérie Audinot , Philippe Delagrange , Daniel-Henri Caignard
发明人： Pascal Marchand , Vincent Babonneau , Sylvie Piessard , Muriel Duflos , Jean Albert Boutin , Valérie Audinot , Philippe Delagrange , Daniel-Henri Caignard
IPC分类号： A61K31/4045 , C07D209/12
CPC分类号： C07D209/42
摘要： Compounds of formula (I): wherein: R1 represents an alkyl, cycloalkyl or cycloalkylalkyl group, R2 represents a linear or branched (C1-C6)alkyl group, and n represents from 1 to 6. Medicaments.
摘要翻译： 式（I）化合物：其中：R1表示烷基，环烷基或环烷基烷基，R2表示直链或支链（C1-C6）烷基，n表示1-6。药物。
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6.发明授权Peptides which interact with anti-apoptotic members of the Bcl-2 protein family, and uses 失效与Bcl-2蛋白家族的抗凋亡成员相互作用的肽和用途公开(公告)号：US07927813B2
公开(公告)日：2011-04-19
申请号：US11883400
申请日：2006-01-31
CPC分类号： C07K14/4747
摘要： The invention relates to a method of screening and identifying modulators of the protein interaction between new peptides and anti-apoptotic members of the Bcl-2 protein family. The modulators identified on the basis of this method are administered to patients with cancer in order to bring about apoptotic-type and/or autophagic-type programmed cell death in those patients.
摘要翻译： 本发明涉及筛选和鉴定Bcl-2蛋白家族的新肽和抗凋亡成员之间的蛋白质相互作用的调节剂的方法。 基于该方法鉴定的调节剂被施用于患有癌症的患者，以便在那些患者中引起凋亡型和/或自噬型程序性细胞死亡。
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7.发明授权Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and its application in the synthesis of agomelatine 有权合成（7-甲氧基-1-萘基）乙腈的方法及其在合成agomelatine中的应用公开(公告)号：US07470806B2
公开(公告)日：2008-12-30
申请号：US11051868
申请日：2005-02-04
IPC分类号： C07C255/03
CPC分类号： C07C253/30 , C07C2602/10 , C07C255/37
摘要： A process for the industrial synthesis of the compound of formula (I) Application in the synthesis of agomelatine.
摘要翻译： 用于工业合成式（I）化合物的方法在合成agomelatine中的应用。
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公开(公告)号：US07459434B2
公开(公告)日：2008-12-02
申请号：US10566668
申请日：2004-08-04
CPC分类号： C07K14/4747 , C07K14/4702
摘要： The invention relates to the identification of a new peptide interacting with the anti-apoptotic proteins Bcl-2, Bcl-W and/or Bcl-XL, and also to screening methods allowing identification of modifiers of those interactions.
摘要翻译： 本发明涉及鉴定与抗凋亡蛋白Bcl-2，Bcl-W和/或Bcl-XL相互作用的新肽，以及鉴定这些相互作用的改性剂的筛选方法。
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9.发明授权Amino acid derivatives, method for production thereof and pharmaceutical compositions comprising said derivative 失效氨基酸衍生物，其生产方法和包含所述衍生物的药物组合物公开(公告)号：US07265220B2
公开(公告)日：2007-09-04
申请号：US10505005
申请日：2003-02-17
IPC分类号： C07C257/18 , C07C311/13 , C07C311/19 , C07C259/18 , A61K31/196 , A61P7/04 , C07D213/34 , C07D295/22 , C07D261/20
CPC分类号： C07D295/26 , A61K38/00 , C07C257/18 , C07C259/18 , C07C311/10 , C07C311/13 , C07C311/19 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2603/14 , C07C2603/28 , C07D213/34 , C07D261/20 , C07K5/06034 , C07K5/06078
摘要： Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.
摘要翻译： 式（I）的化合物：其中：R 1表示任选取代的芳基，杂芳基或烷基，或式 - （CO）-CR 6 R' 其中R 6，R 7，R 3，R 3，R 7， 8和R 9如在说明书中所定义，R 2表示氢或烷基，R 3表示氢或任选取代的 烷基，R 4表示饱和或不饱和的，7至15元双环体系或任选取代的烷基，或R 3和R 4， 与携带它们的碳原子一起形成任选含有一个或多个选自O，S和N的杂原子的任选被取代的饱和或不饱和的3至18元单，双，三环体系， n表示1或2，Ar表示芳基或杂芳基，R 5表示任选取代的氨基，胍基，氰基或脒基，其旋光异构体，以及其中的加成盐 与药学上可接受的酸。 含有相同功能的药物，可用于涉及活化蛋白C的病理状况。
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公开(公告)号：US20050143440A1
公开(公告)日：2005-06-30
申请号：US11069094
申请日：2005-03-01
申请人： Sylvain Rault , Marina Kopp , Jean-Charles Lancelot , Stephane Lemaitre , Daniel-Henri Caignard , Jean-Guy Bizot-Espiard , Pierre Renard
发明人： Sylvain Rault , Marina Kopp , Jean-Charles Lancelot , Stephane Lemaitre , Daniel-Henri Caignard , Jean-Guy Bizot-Espiard , Pierre Renard
IPC分类号： A61K31/381 , A61K31/402 , A61K31/417 , A61K31/4178 , A61K31/44 , A61K31/4439 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , C07D401/06 , C07D403/06 , C07D409/06 , A61K31/4164
CPC分类号： C07D401/06 , C07D403/06 , C07D409/06
摘要： Compounds of formula (I): wherein: R1 represents an optionally substituted heteroaryl group, R2 represents an optionally substituted cycloalkyl group, R3 represents a hydrogen atom or an alkyl group, and R4 and R5 are as defined in the description, and Medicinal products containing the same are useful in the treatment of non-insulin-dependent type II diabetes, obesity, type I diabetes, hyperlipidaemia, hypercholesterolaemia and cardiovascular complications thereof.
摘要翻译： 式（I）化合物：其中：R 1表示任选取代的杂芳基，R 2表示任选取代的环烷基，R 3， 表示氢原子或烷基，R 4和R 5和R 5如说明书中所定义，并且含有它们的药用产品可用于治疗非 - 胰岛素依赖型II型糖尿病，肥胖症，I型糖尿病，高脂血症，高胆固醇血症及其心血管并发症。
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