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31. 发明申请

WO2013190559A1 IMPROVED PROCESSES FOR THE PREPARATION OF LINEZOLID CRYSTALLINE FORM III 审中-公开
标题翻译：线性晶体结构形式的改进方法III
公开(公告)号：WO2013190559A1
公开(公告)日：2013-12-27
申请号：PCT/IN2012/000434
申请日：2012-06-19
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda
发明人： MOHAN RAO, Dodda
IPC分类号： A61K31/5377
CPC分类号： A61K31/5377
摘要： We have surprisingly and unexpectedly found that linezolid crystalline Form III can be prepared in an improved, efficient and cost effective process, in high purity and with high yield, by reacting the solution of (S)-N-[[3-[3-fluoro-4-[4-morpholinyl] phenyl]-2-oxo-5-oxazolidinyl]methyl]amine in methylene chloride with acetic anhydride, optionally in the presence of an organic base, to produce a reaction mass containing linezolid, followed by layer separation and subsequent carbon treatment to the resulting organic layer to form a filtrate, adding water to the resulting filtrate, and subsequent removal of methylene chloride solvent by distillation, optionally seeding the reaction mass during the distillation process, to produce the crystalline Form III of linezolid.
摘要翻译：我们出人意料地意外地发现，利用（S）-N - [[3- [3-（3-甲氧基 - 苯基） - 哌啶-1-基]苯甲酸的溶液，可以以高纯度和高产率，以改进的，有效和成本有效的方法制备利奈唑胺晶形III 氟代-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]胺的二氯甲烷与乙酸酐，任选在有机碱存在下反应，生成含有利奈唑胺的反应物质，分离和随后的碳处理到所得有机层以形成滤液，向所得滤液中加入水，随后通过蒸馏除去二氯甲烷溶剂，任选地在蒸馏过程中接种反应物料，以产生利奈唑胺的晶型III 。

32. 发明申请

WO2013105100A1 PROCESSES FOR THE PREPARATION OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL)PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)-2-THIOPHENE-CARBOXAMIDE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备5-氯代-N - （{（5S）-2-氧代-3- [4-（3-氧代-4-吗啉基）苯基] -1,3-氧杂环己烯-5-基}甲基） -2-硫代羧酰胺及其中间体
公开(公告)号：WO2013105100A1
公开(公告)日：2013-07-18
申请号：PCT/IN2012/000025
申请日：2012-01-09
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , VENKAT REDDY, Buthukuri
发明人： MOHAN RAO, Dodda , VENKAT REDDY, Buthukuri
IPC分类号： C07D413/10
CPC分类号： C07D413/10 , C07D413/14
摘要： The present invention relates to processes for the preparation of oxazolidinone derivatives. More particularly the present invention provides processes for the preparation of 5-chloro-N-( {(5S)-2-oxo-3-[4-(3-oxo-4-moφholinyl)phenyl]-1,3-oxazolidin-5-yl methyl)-2-thiophene-carboxamide and intennediates thereof. Where L is a leaving group like halogen atom (F, CI, Br, I) or -OS02R where R = C'-4 alkyl straight chain or branched chain, sub or unsubstituted aryl, sub or unsub aryl alkyl; with a suitable reagent to provide the compound of formula (II). The reaction step is performed by reacting the compound of formula (IV) with amine source which may be dissolved in solvent like water or alcohol. For example ammonium hydroxide.
摘要翻译：本发明涉及制备恶唑烷酮衍生物的方法。更具体地说，本发明提供了制备5-氯-N（{（5S）-2-氧代-3- [4-（3-氧代-4-吗啉基）苯基] -1,3-恶唑烷-2-酮吡啶-5-基甲基）-2-噻吩 - 甲酰胺及其所得物。其中L为离去基团如卤原子（F，Cl，Br，I）或-OS02R，其中R = C'-4烷基直链或支链，亚或未取代的芳基，亚芳基或未烷基芳基烷基; 用合适的试剂提供式（II）化合物。反应步骤通过使式（IV）的化合物与可以溶解在溶剂中的胺源（如水或醇）反应来进行。例如氢氧化铵。

33. 发明申请

WO2013046211A1 PROCESSES FOR THE PREPARATION OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL) PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)-2-THIOPHENE-CARBOXAMIDE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备5-氯代-N - （{（5S）-2-氧代-3- [4-（3-氧代-4-吗啉基）苯基] -1,3-氧杂环己烯-5-基}甲基） -2-硫代羧酰胺及其中间体
公开(公告)号：WO2013046211A1
公开(公告)日：2013-04-04
申请号：PCT/IN2011/000670
申请日：2011-09-27
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , VENKAT REDDY, Buthukuri
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , VENKAT REDDY, Buthukuri
IPC分类号： A61K31/425 , A61K31/535
CPC分类号： C07D265/32 , C07C215/08 , C07C219/06 , C07C219/16 , C07C233/18 , C07C247/04 , C07C251/24 , C07C271/20 , C07D203/12 , C07D333/38 , C07D409/12 , C07D413/10 , C07D413/14
摘要： TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
摘要翻译：本发明提供了制备5-氯-N - （{（5S）-2-氧代-3- [4-（3-氧代-4-吗啉基）苯基] -1,3-恶唑烷-5-酮的方法，吡啶-2-基}甲基）-2-噻吩 - 甲酰胺（I）及其中间体。还提供新的中间体及其在恶唑烷衍生物的合成中的应用。

34. 发明申请

WO2010128516A3 PROCESS FOR THE PREPARATION OF FLIBANSERIN INVOLVING NOVEL INTERMEDIATES 审中-公开
标题翻译：涉及新型中间体的白蛋白的制备方法
公开(公告)号：WO2010128516A3
公开(公告)日：2012-11-29
申请号：PCT/IN2009000267
申请日：2009-05-04
申请人： SYMED LABS LTD , MOHAN RAO DODDA , KRISHNA REDDY PINGILI , VENKAT REDDY BUTHUKURI
发明人： MOHAN RAO DODDA , KRISHNA REDDY PINGILI , VENKAT REDDY BUTHUKURI
IPC分类号： C07D235/26 , C07D403/06
CPC分类号： C07D235/26
摘要： The present invention related to process for the preparation of flibanserin involving novel intermediates. 1,3-dihydro-1-(2-bromoethyl)- 3-isopropenyl-2H-benzimidazol-2-one reacts with diethanolamine and converting the obtained dihydroxy compound to 1,3-dihydro- 1-[2-[N-[bis-(2-chloroethyl)amino]ethyl]-3-isopropenyl-2H-benzimidazol-2-one followed by depotection to obtain 1,3-dihydro- 1-[2-[N-bis-(2-chloroethyl)amino]ethyl]-1,2-H-benzimidazol-2-one. This on condensing with m-trifluoromethyl aniline gives flibanserin hydrochloride.
摘要翻译：本发明涉及涉及新型中间体的氟班色林的制备方法。 1,3-二氢-1-（2-溴乙基）-3-异丙烯基-2H-苯并咪唑-2-酮与二乙醇胺反应，并将所得二羟基化合物转化为1,3-二氢-1- [2- [N- [ （2-氯乙基）氨基]乙基] -3-异丙烯基-2H-苯并咪唑-2-酮，然后脱保护，得到1,3-二氢-1- [2- [N-双 - （2-氯乙基）氨基 ]乙基] -1,2-苯并咪唑-2-酮。在与三氟甲基苯胺缩合的情况下，可得到盐酸氟班色林。

35. 发明申请

WO2011161690A1 PROCESSES FOR THE PREPARATION OF (+)-N,N-DIMETHYL-2-[1-(NAPHTHALENYLOXY) ETHYL] BENZENE METHANAMINE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备（+） - N，N-二甲基-2- [1-（萘磺酰）乙基]苯甲酮甲胺及其中间体的方法
公开(公告)号：WO2011161690A1
公开(公告)日：2011-12-29
申请号：PCT/IN2011/000116
申请日：2011-02-25
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , JITHENDER, Aadepu , VENUGOPAL, Bingi
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , JITHENDER, Aadepu , VENUGOPAL, Bingi
IPC分类号： A01N37/00 , A61K31/20
CPC分类号： A61K31/137 , A61K31/138 , A61K31/235 , C07B2200/07 , C07C213/00 , C07C213/06 , C07C213/10 , C07C215/28 , C07C217/16
摘要： The present invention relates to processes for the preparation of S(+)-N,N-dimethyl-2-[1-(naphthalenyloxy)ethyl]benzene methanamine and intermediates thereof. More particularly the present invention relates to preparation of the compound 3(S)-(+)-N,N-dimethylamino-3-phenyl propanol useful as intermediate in the synthesis of pharmaceutically active compounds.
摘要翻译：本发明涉及制备S（+） - N，N-二甲基-2- [1-（萘氧基）乙基]苯甲胺的方法及其中间体。更具体地说，本发明涉及可用作合成药物活性化合物的中间体的化合物3（S） - （+） - N，N-二甲基氨基-3-苯基丙醇的制备。

36. 发明申请

WO2010146595A2 NOVEL POLYMORPHS OF FLIBANSERIN HYDROCHLORIDE 审中-公开
标题翻译： FLIBANSERIN HYDROCHLORIDE的新型多聚体
公开(公告)号：WO2010146595A2
公开(公告)日：2010-12-23
申请号：PCT/IN2009/000347
申请日：2009-06-16
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , VENKAT REDDY, Buthukuri
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , VENKAT REDDY, Buthukuri
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention provides novel crystalline anhydrous form II, hemihydrate form III, anhydrous form IV, anhydrous form V, anhydrous form VI, hemihydrate form VII, hemihydrate form VIII, hemihydrate form IX and amorphous form of flibanserin hydrochloride, processes for its preparation and to pharmaceutical compositions containing them.
摘要翻译：本发明提供了新的无水形式II，半水合物形式III，无水形式IV，无水形式V，无水形式VI，半水合物形式VII，半水合物形式VIII，半水合物形式IX和无定形形式的氟班色林盐酸盐，其制备方法和含有它们的药物组合物。

37. 发明申请

WO2008152650A1 PROCESS FOR PREPARATION OF SUBSTANTIALLY OPTICALLY PURE LEVOROTATORY AND DEXTROROTATORY ENANTIOMERS OF CETIRIZINE USING NOVEL INTERMEDIATES 审中-公开
标题翻译：使用新型中间体制备基质的光学纯度和光催化降解能力的方法
公开(公告)号：WO2008152650A1
公开(公告)日：2008-12-18
申请号：PCT/IN2007/000239
申请日：2007-06-15
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , SATYANARAYANA RAO, Bitra
发明人： MOHAN RAO, Dodda , SATYANARAYANA RAO, Bitra
IPC分类号： C07D295/073
CPC分类号： C07D295/073
摘要： The present invention relates to a novel and commercially viable process for substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine intermediate, 1-[(4-chlorophenyl)phenylmethyl]piperazine, thereby producing substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine and their pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates.
摘要翻译：本发明涉及一种用于西替立嗪中间体，1 - [（4-氯苯基）苯基甲基]哌嗪的基本上光学纯的左旋和右旋对映异构体的新型和商业上可行的方法，由此制备西替利嗪及其药学上可接受的基本上光学纯的左旋和右旋对映异构体使用新型中间体，其高纯度和高产率的其酸加成盐。

38. 发明申请

WO2005099353A2 A NOVEL PROCESS FOR THE PREPARATION OF LINEZOLID AND RELATED COMPOUNDS 审中-公开
标题翻译：制备线性和相关化合物的新方法
公开(公告)号：WO2005099353A2
公开(公告)日：2005-10-27
申请号：PCT/IN2004000105
申请日：2004-04-19
申请人： SYMED LABS LTD , MOHAN RAO DODDA , KRISHNA REDDY PINGILI
发明人： MOHAN RAO DODDA , KRISHNA REDDY PINGILI
IPC分类号： C07D295/135 , C07D413/10 , C07D417/10
CPC分类号： C07D413/10 , C07D263/20 , C07D295/135 , C07D417/10
摘要： The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; b) subjecting N-[3-Chloro-2-(R)-hydroxypropyl]-3-fluoro-4-morpholinyl aniline produced above to carbonylation; c) reacting (5R)-5-(chloromethyl)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxazolidinone produced above with potassium phthalimide; d) reacting (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]phthalimide produced above with hydrazine hydrate; and e) reacting S-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]amine produced above with acetic anhydride to produce linezolid.
摘要翻译：本发明提供了一种制备5-氨基甲基取代的恶唑烷酮的新方法，包括利奈唑胺的恶唑烷酮抗菌剂的关键中间体。因此，利奈唑胺通过以下方法制备：a）使3-氟-4-吗啉基苯胺与R-表氯醇反应; b）使上面制备的N- [3-氯-2-（R） - 羟丙基] -3-氟-4-吗啉基苯胺进行羰基化; c）使上述制备的（5R）-5-（氯甲基）-3- [3-氟-4-（4-吗啉基）苯基] -2-恶唑烷酮与邻苯二甲酰亚胺钾反应; d）使上述制备的（S）-N - [[3- [3-氟-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]邻苯二甲酰亚胺与水合肼反应; 和e）使上述制备的S-N - [[3- [3-氟-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]胺与乙酸酐反应，生成利奈唑胺。

39. 发明申请

WO2017178966A1 TOPICAL SPRAY FORMULATION OF GLYCOPYRROLATE 审中-公开
标题翻译：丙二醇的局部喷雾配方
公开(公告)号：WO2017178966A1
公开(公告)日：2017-10-19
申请号：PCT/IB2017/052078
申请日：2017-04-11
申请人： SUVEN LIFE SCIENCES LIMITED , MANAM, Mohan Rao , VALLABHANENI, Murali Krishna Prasad , JASTI, Venkateswarlu
发明人： MANAM, Mohan Rao , VALLABHANENI, Murali Krishna Prasad , JASTI, Venkateswarlu
IPC分类号： A61K8/49
CPC分类号： A61K8/4913 , A61K8/046 , A61K8/345 , A61K8/35 , A61K8/731 , A61K8/8152 , A61K8/8176 , A61K8/8182 , A61K8/86 , A61K9/0014 , A61K9/7015 , A61K31/40 , A61K2800/87 , A61Q15/00
摘要： The present invention relates to topical spray compositions and methods for the preparation of the same. The topical spray composition comprising Glycopyrrolate or its salts with specific class of excipients may be used to reduce various secretions in human body, specifically to control hyperhydrosis.
摘要翻译：本发明涉及局部喷雾组合物及其制备方法。包含格隆溴铵或其盐与特定类型的赋形剂的局部喷雾组合物可用于减少人体中的各种分泌物，特别是用于控制hyperhydrosis。

40. 发明申请

WO2016046833A3 IMPROVED PROCESSES FOR THE PREPARATION OF AGOMELATINE USING NOVEL INTERMEDIATES 审中-公开
标题翻译：采用新型中间体改进氨甲喋呤的制备工艺
公开(公告)号：WO2016046833A3
公开(公告)日：2016-03-31
申请号：PCT/IN2014/000618
申请日：2014-09-24
申请人： SYMED LABS LIMITED , MOHAN RAO, Dodda , MALLA REDDY, Vanga
发明人： MOHAN RAO, Dodda , MALLA REDDY, Vanga
IPC分类号： A61K31/165
摘要： Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of agomelatine, in high yield and purity, using novel intermediates. The process includes: a) reacting N-[2-(7-hydroxy-3,4-dihydro-1-naphthalenyl)ethyl] acetamide with a suitable activating agent; b) subjecting the acylated compound to aromatization by reacting with a suitable aromatizing agent; c) deprotecting the aromatized compound with a suitable deprotecting agent to produce the N-[2-(7-hydroxy-1-naphthalenyl)ethyl] acetamide; d) reacting the deprotected compound with a methylating agent to produce agomeltaine.
摘要翻译：本文提供了使用新型中间体以高收率和纯度制备阿戈美拉汀的改进的，商业上可行的和工业上有利的方法。该方法包括：a）使N- [2-（7-羟基-3,4-二氢-1-萘基）乙基]乙酰胺与合适的活化剂反应; b）通过与合适的芳香剂反应使酰化的化合物芳构化; c）用合适的脱保护剂使芳构化的化合物去保护，生成N- [2-（7-羟基-1-萘基）乙基]乙酰胺; d）使脱保护的化合物与甲基化试剂反应以产生阿戈美拉汀。

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