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31. 发明申请

WO2013057322A1 (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS 审中-公开
标题翻译：（HETERO）ARYL CYPOPRAMLAMINE COMPOUNDS AS LSD1 INHIBITORS
公开(公告)号：WO2013057322A1
公开(公告)日：2013-04-25
申请号：PCT/EP2012/070900
申请日：2012-10-22
申请人： ORYZON GENOMICS, S.A.
发明人： ORTEGA MUÑOZ, Alberto , FYFE, Mathew Colin Thor , MARTINELL PEDEMONTE, Marc , ESTIARTE MARTÍNEZ, María de los Ángeles , VALLS VIDAL, Nuria , KURZ, Guido , CASTRO PALOMINO LARIA, Julio Cesar
IPC分类号： C07D213/74 , C07C211/35 , A61K31/135 , A61P35/00 , A61P31/12 , A61P25/00
CPC分类号： C07C211/36 , C07B2200/07 , C07C209/28 , C07C211/37 , C07C211/38 , C07C211/40 , C07C213/00 , C07C215/46 , C07C215/64 , C07C217/54 , C07C217/74 , C07C269/00 , C07C271/24 , C07C273/00 , C07C273/18 , C07C275/26 , C07C311/08 , C07C311/21 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07D207/14 , C07D213/30 , C07D213/38 , C07D213/57 , C07D213/73 , C07D213/74 , C07D231/12 , C07D231/56 , C07D277/28 , C07D295/096 , C07D295/135 , C07D295/26 , C07D307/52 , C07D333/20
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
摘要翻译：本发明涉及（异）芳基环丙胺化合物，特别包括本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症，神经疾病或病症，或病毒感染。

32. 发明申请

WO2013011518A1 PROCESS FOR THE PREPARATION OF RETIGABINE OF THE FORMULA I AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制备公式I及其药学上可接受的药物的制备方法
公开(公告)号：WO2013011518A1
公开(公告)日：2013-01-24
申请号：PCT/IN2011/000639
申请日：2011-09-16
申请人： ARCH PHARMALABS LIMITED , MANDAL, Arun Kanti , RANBHAN, Kamlesh Jayantilal , SAXENA, Sudhanshu , GAIKWAD, Sanjay Ramrao , SARJEKAR, Pushpalata Balkrishna
发明人： MANDAL, Arun Kanti , RANBHAN, Kamlesh Jayantilal , SAXENA, Sudhanshu , GAIKWAD, Sanjay Ramrao , SARJEKAR, Pushpalata Balkrishna
IPC分类号： C07C209/28 , C07C209/36 , C07C209/52 , C07C249/02 , C07C269/04 , C07C269/06
CPC分类号： C07C269/04 , C07C209/28 , C07C209/36 , C07C209/52 , C07C249/02 , C07C269/06 , C07C211/50 , C07C211/51 , C07C251/24 , C07C271/28
摘要： The invention relates to process for the preparation of 2-amino-4-(4- fluorobenzylamino)-l-ethoxycarbonylaminobenzene generically known as Retigabine of the formula (I) and its pharmaceutically acceptable salts e.g. Formula IA, particularly to the modification over the prior art processes-I and II disclosed therein in US5384330. The modifications are depicted in the scheme I and scheme II respectively. Disclosed herein are also the novel processes for the preparation of intermediates of formulae M, N and O of the process-I and of formulae R, S, T of process-II, those are used for preparation of Retigabine of the formula I and its pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及制备通常称为式（I）的瑞替加滨的2-氨基-4-（4-氟苄基氨基）-1-乙氧基羰基氨基苯的方法及其药学上可接受的盐，例如，式IA，特别是关于在US5384330中公开的现有技术方法-I和II的改进。这些修改分别在方案I和方案II中描述。本文公开的方法也是制备方法I的式M，N和O的中间体和方法II的式R，S，T的中间体的新方法，其用于制备式I的瑞格列宾及其制备方法其药学上可接受的盐。

33. 发明申请

WO2011048612A3 PROCESS FOR PREPARATION OF PROPARGYLATED AMINOINDANS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制备丙氨酸氨基酸或其药学上可接受的盐的方法
公开(公告)号：WO2011048612A3
公开(公告)日：2011-08-11
申请号：PCT/IN2010000671
申请日：2010-10-08
申请人： GLENMARK GENERICS LTD , THANEDAR AMIT ANANT , DESHMUKH SHEKHAR ASHOK , ZOPE SUNIL SUDHAKAR , KELKAR LAXMIKANT MADHUKAR , KOILPILLAI JOSEPH PRABAHAR , GAJERA JITENDRA MAGANBHAI
发明人： THANEDAR AMIT ANANT , DESHMUKH SHEKHAR ASHOK , ZOPE SUNIL SUDHAKAR , KELKAR LAXMIKANT MADHUKAR , KOILPILLAI JOSEPH PRABAHAR , GAJERA JITENDRA MAGANBHAI
IPC分类号： C07C211/42 , A61K31/135 , A61P25/16 , C07C209/22 , C07C269/06 , C07C271/44
CPC分类号： C07C209/28 , C07C211/42 , C07C2602/08
摘要： A process for preparation of propargylated aminoindans or pharmaceutically acceptable salts thereof, comprises: a) reacting an indanone derivative or a salt thereof with propargyl amine or a salt thereof in the presence of a Lewis acid; b) subjecting the resultant reaction mixture to reduction.
摘要翻译：炔丙基化氨基茚满或其药学上可接受的盐的制备方法包括：a）在路易斯酸存在下，使茚酮衍生物或其盐与炔丙基胺或其盐反应; b）使得到的反应混合物进行还原。

34. 发明申请

WO2010059913A3 PREPARATION OF RASAGILINE AND SALTS THEREOF 审中-公开
标题翻译：制备RASAGILINE及其盐
公开(公告)号：WO2010059913A3
公开(公告)日：2010-09-16
申请号：PCT/US2009065279
申请日：2009-11-20
申请人： REDDYS LAB LTD DR , REDDYS LAB INC DR , CHERUKUPALLY PRAVEEN , VAJRALA VENKATA REDDY , ADLA VIJAYA KUMAR , RANGINENI SRINIVASULU , KANNIAH SUNDARALAKSHMI
发明人： CHERUKUPALLY PRAVEEN , VAJRALA VENKATA REDDY , ADLA VIJAYA KUMAR , RANGINENI SRINIVASULU , KANNIAH SUNDARALAKSHMI
IPC分类号： C07C209/28 , A61K31/135 , C07C211/42 , C07C249/02 , C07C251/20
CPC分类号： C07C211/42 , C07C209/28 , C07C249/02 , C07C2602/08 , Y10T428/2982 , C07C251/20
摘要： The present invention relates to processes for the preparation of rasagiline mesylate. Also provided is rasagiline mesylate having 90 volume percent of the particles (D90) with sizes less than about 6 µm and processes for the preparation thereof.
摘要翻译：本发明涉及制备甲磺酸雷沙吉兰的方法。还提供了具有90体积％的尺寸小于约6μm的颗粒（D90）的甲磺酸雷沙吉兰和其制备方法。

35. 发明申请

WO2010059913A2 PREPARATION OF RASAGILINE AND SALTS THEREOF 审中-公开
标题翻译：雷沙吉兰及其盐的制备
公开(公告)号：WO2010059913A2
公开(公告)日：2010-05-27
申请号：PCT/US2009/065279
申请日：2009-11-20
申请人： DR. REDDY'S LABORATORIES LTD. , DR. REDDY'S LABORATORIES, INC. , CHERUKUPALLY, Praveen , VAJRALA, Venkata Reddy , ADLA, Vijaya Kumar , RANGINENI, Srinivasulu , KANNIAH, Sundaralakshmi
发明人： CHERUKUPALLY, Praveen , VAJRALA, Venkata Reddy , ADLA, Vijaya Kumar , RANGINENI, Srinivasulu , KANNIAH, Sundaralakshmi
IPC分类号： C07C209/28 , C07C249/02 , C07C211/42 , C07C251/20 , A61K31/135
CPC分类号： C07C211/42 , C07C209/28 , C07C249/02 , C07C2602/08 , Y10T428/2982 , C07C251/20
摘要： The present invention relates to processes for the preparation of rasagiline mesylate. Also provided is rasagiline mesylate having 90 volume percent of the particles (D 90 ) with sizes less than about 6 μm and processes for the preparation thereof.
摘要翻译：本发明涉及制备甲磺酸雷沙吉兰的方法。还提供了甲磺酸雷沙吉兰具有90体积％的尺寸小于约6μm的颗粒（D 90）及其制备方法。

36. 发明申请

WO2008068625A9 PROCESSES FOR PREPARING CINACALCET HYDROCHLORIDE AND POLYMORPHIC FORMS THEREOF 审中-公开
标题翻译：制备CINACALCET HYDROCHLORIDE的方法及其多晶型
公开(公告)号：WO2008068625A9
公开(公告)日：2009-03-26
申请号：PCT/IB2007004309
申请日：2007-06-08
申请人： MEDICHEM SA , SZEKERES TIBOR , REPASI JOZSEF , SZABO ANDRAS , BENITO VELEZ MONICA , MANGION BERNARDINO
发明人： SZEKERES TIBOR , REPASI JOZSEF , SZABO ANDRAS , BENITO VELEZ MONICA , MANGION BERNARDINO
IPC分类号： C07C209/28 , C07C209/84 , C07C211/30
CPC分类号： C07C209/84 , C07B2200/13 , C07C209/28 , C07C211/30
摘要： The invention relates to cinacalcet hydrochloride, new polymorphic crystalline forms of cinacalcet hydrochloride, amorphous cinacalcet hydrochloride and synthetic processes for their preparation.
摘要翻译：本发明涉及盐酸西那卡塞，盐酸西那卡塞的新型多晶型物，盐酸非卡那西酯及其制备方法。

37. 发明申请

WO2003055844A1 PROCESS FOR PREPARING TERBINAFINE AND HCI SALT THEREOF 审中-公开
标题翻译：制备苦味碱和盐酸盐的方法
公开(公告)号：WO2003055844A1
公开(公告)日：2003-07-10
申请号：PCT/KR2002/002442
申请日：2002-12-26
申请人： YUHAN CORPORATION
发明人： LEE, Tai-Au , WANG, Kyu-Jung , KIM, Hong-Bae , KWON, Kyoung-Chan , KU, Chang-Hoe
IPC分类号： C07C209/24
CPC分类号： C07C209/28 , C07C211/30
摘要： Provided are a process for preparing terbinafine or its HCl salt, which comprises: (a) reacting a furan derivative with a base; (b) performing a reductive alkylation of the resulting compound obtained in the step (a) with N-methyl-1-naphthalenemethylamine or its HCl salt; and (c) purifying the resulting compound obtained in the step (b).
摘要翻译：提供了特比萘芬或其HCl盐的制备方法，其包括：（a）使呋喃衍生物与碱反应; （b）用N-甲基-1-萘甲胺或其HCl盐进行步骤（a）得到的化合物的还原烷基化; 和（c）纯化步骤（b）中得到的所得化合物。

38. 发明申请

WO0236540A2 PROCESS FOR PREPARATION OF beta -PHENETHYLAMINE DERIVATIVE 审中-公开
标题翻译：制备β-苯甲酰胺衍生物的方法
公开(公告)号：WO0236540A2
公开(公告)日：2002-05-10
申请号：PCT/IB0101996
申请日：2001-10-25
IPC分类号： C07C209/28 , C07C211/29
CPC分类号： C07C211/29 , C07C209/28 , C07C2601/04
摘要： A process for the production of Sibutramine i.e. N-1-[1-(4-chlorophenyl) cyclobutyl]-3-methylbutyl-N, N-dimethylamine of formula (I) comprising the steps of: (a) reacting a nitrile, 1-(4-chlorophenyl) cyclobutyl carbonitrile of formula (III) with a Grignard reagent, namely isobutyl magnesium bromide to produce the magnesium complex of formula (IV); (b) cleaving the magnesium complex of formula (IV) under basic conditions to form an imine of formula (VIII); (c) reducing the imine of formula (VIII) by a metal hydride to obtain an amine of the formula (VII), and (d) converting the amine (VII) first to its hydrochloride and then to Sibutramine of formula (I) by Eschweiler Clarke methylation.
摘要翻译：制备西布曲明的方法，即式（I）的N-1- [1-（4-氯苯基）环丁基] -3-甲基丁基-N，N-二甲胺的方法，包括以下步骤：（a）使腈，（III）的（4-氯苯基）环丁基腈与格氏试剂即异丁基溴化镁反应以制备式（IV）的镁络合物; （b）在碱性条件下裂解式（IV）的镁络合物以形成式（VIII）的亚胺; （c）用金属氢化物还原式（Ⅷ）的亚胺，得到式（Ⅶ）的胺，（d）首先将胺（Ⅶ）转化成盐酸盐，然后转化成式（I）的西布曲明，由 Eschweiler克拉克甲基化。

39. 发明申请

WO00041992A1 REDUCTIVE ALKYLATION OF SECONDARY AMINES WITH HYDROSILANE 审中-公开
标题翻译：二级胺与水解的还原性烷基化
公开(公告)号：WO00041992A1
公开(公告)日：2000-07-20
申请号：PCT/US1999/030299
申请日：1999-12-20
IPC分类号： A61K31/5513 , A61P35/00 , A61P43/00 , C07C209/28 , C07D243/14 , C07D403/06 , C07D409/12 , C07D409/14 , C07D233/34 , C07D333/64
CPC分类号： C07D403/06 , C07C209/28 , C07D243/14 , C07D409/12 , C07D409/14
摘要： A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has application in the preparationof imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.
摘要翻译：公开了通过使用氢硅烷和路易斯酸通过第二胺的还原烷基化生产叔胺的新方法。该新方法可用于制备含咪唑的苯并二氮杂，法呢基蛋白转移酶的抑制剂。

40. 发明申请

WO9958475A3 PREPARATION OF COMPOUNDS USING POLYMER SUPPORTED REAGENTS 审中-公开
标题翻译：使用聚合物支持的试剂制备化合物
公开(公告)号：WO9958475A3
公开(公告)日：2000-06-15
申请号：PCT/GB9901251
申请日：1999-05-11
申请人： CAMBRIDGE COMBINATORIAL LTD , LEY STEVEN , BOLLI MARTIN , HINZEN BERTHOLD , GERVOIS ANNE GERALDINE , HALL BEVERLEY , HABERMANN JORG , SCOTT JAMES , HAUNERT FRANK
发明人： LEY STEVEN , BOLLI MARTIN , HINZEN BERTHOLD , GERVOIS ANNE-GERALDINE , HALL BEVERLEY , HABERMANN JORG , SCOTT JAMES , HAUNERT FRANK
IPC分类号： C07B61/00
CPC分类号： C07C45/511 , C07B61/00 , C07B2200/11 , C07C1/34 , C07C45/28 , C07C209/28 , C07C213/02 , C07C213/08 , C07C2601/08 , C07D207/16 , C07D211/62 , C07D213/30 , C07D213/89 , C07D231/06 , C07D303/04 , C07D307/44 , C07D409/12 , C40B40/04 , C40B50/14 , C40B99/00 , C07C15/44 , C07C15/52 , C07C15/50 , C07C47/55 , C07C47/54 , C07C47/575 , C07C47/542 , C07C49/255 , C07C49/217 , C07C49/753 , C07C49/235 , C07C49/683 , C07C211/52 , C07C217/58 , C07C217/84
摘要： There is described a process for the preparation of a compound which process includes a first reaction and a second reaction, wherein the process uses a first solid supported reagent in said first reaction and a second solid supported reagent in said second reaction. The process may be used to effect multi-step organic synthesis for potential applications in combinatorial chemistry and/or the preparation of chemical libraries.
摘要翻译：描述了一种制备化合物的方法，该方法包括第一反应和第二反应，其中所述方法在所述第一反应中使用第一固体支持的试剂，在所述第二反应中使用第二固体负载的试剂。该方法可用于在组合化学和/或化学文库的制备中用于潜在应用的多步有机合成。

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