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1. 发明公开

EP2513042A2 SOLID DAPOXETINE 审中-公开
标题翻译：达泊西汀以固体形式
公开(公告)号：EP2513042A2
公开(公告)日：2012-10-24
申请号：EP09851230.4
申请日：2009-11-13
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , JITHENDER, Aadepu
IPC分类号： C07C217/48
CPC分类号： C07C217/48 , C07B2200/07 , C07C213/10
摘要： The present invention relates to solid racemic dapoxetine, solid dapoxetine S(+)enantiomer, processes for their preparation and their use in the pharmaceutically active compound dapoxetine acid addition salt, and pharmaceutical compositions thereof.

2. 发明公开

EP2909166A1 PROCESSES FOR THE PREPARATION OF AGOMELATINE USING NOVEL INTERMEDIATES 审中-公开
标题翻译：流程，阿戈美拉汀的方法，用新型中间材料
公开(公告)号：EP2909166A1
公开(公告)日：2015-08-26
申请号：EP12887041.7
申请日：2012-10-22
申请人： Symed Labs Limited , Mohan Rao, Dodda , Anna Reddy, Ambati
发明人： MOHAN RAO, Dodda , ANNA REDDY, Ambati
IPC分类号： C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07C213/02 , C07C213/10 , C07C215/26 , C07C231/02 , C07C233/22 , C07C253/30 , C07C255/36
摘要： Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of Agomelatine or a salt thereof, in high yield and purity, using novel intermediates.

3. 发明公开

EP2545028A1 A NOVEL STEREOSPECIFIC SYNTHESIS OF (-) (2S,3S)-1-DIMETHYLAMINO-3-(3-METHOXYPHENYL)-2-METHYL PENTAN-3-OL 审中-公开
标题翻译：（ - ）（2S，3S）-1-二甲基氨基-3-（3-甲氧基苯基）-2-甲基戊-3-醇的新型立体异构合成
公开(公告)号：EP2545028A1
公开(公告)日：2013-01-16
申请号：EP11856935.9
申请日：2011-01-27
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , RAMCHANDRA REDDY, Pingili , HARITHA, KIrla , SRINIVAS, Kolluru
IPC分类号： C07C217/00
CPC分类号： C07C213/00 , C07B53/00 , C07B2200/07 , C07C213/08 , C07C221/00 , C07C217/72 , C07C215/54 , C07C225/06
摘要： The present invention relates to a novel stereospecific synthesis of (-) (2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol.
摘要翻译：（ - ）（2S）-3S）-1-二甲基氨基-3-（3-甲氧基苯基）-2-甲基戊-3-醇的新型立体定向合成中间体合成3 - [（1R ，2R）-3-（二甲基氨基）-1-乙基-2-甲基丙基]苯酚。

4. 发明公开

EP2167479A1 PROCESS FOR PREPARATION OF SUBSTANTIALLY OPTICALLY PURE LEVOROTATORY AND DEXTROROTATORY ENANTIOMERS OF CETIRIZINE USING NOVEL INTERMEDIATES 有权
标题翻译：用于生产的西替利嗪光学很大程度上清纯LEVOROTATORISCHEN DEXTROROTATORISCHEN对映体意味着新的中间体
公开(公告)号：EP2167479A1
公开(公告)日：2010-03-31
申请号：EP07805624.9
申请日：2007-06-15
申请人： Symed Labs Limited
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.

5. 发明公开

EP2844654A1 IMPROVED PROCESS FOR PREPARING RIVAROXABAN USING NOVEL INTERMEDIATES 有权
标题翻译：改进工艺用于生产使用利伐沙班的新中间体
公开(公告)号：EP2844654A1
公开(公告)日：2015-03-11
申请号：EP12876006.3
申请日：2012-05-02
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , VENKAT REDDY, Buthukuri
IPC分类号： C07D409/14
CPC分类号： C07D413/14 , C07D333/38
摘要： The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one or an acid addition salt thereof to produce rivaroxaban.

6. 发明公开

EP2705023A1 PROCESSES FOR THE PREPARATION OF N-[2-(7-METHOXY-1-NAPHTHYL)ETHYL]ACETAMIDE 审中-公开
标题翻译： PROCESS FOR制备N- [2-（7-甲氧基-1-萘基）乙基]乙酰胺
公开(公告)号：EP2705023A1
公开(公告)日：2014-03-12
申请号：EP11854945.0
申请日：2011-01-04
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , ANNA REDDY, Ambati
IPC分类号： C07C231/00
CPC分类号： C07C231/12 , C07B2200/13 , C07C213/02 , C07C231/02 , C07C233/18 , C07C253/30 , C07C255/37 , C07C217/60
摘要： The present invention relates to processes for the synthesis of N-[2-(7-methoxy-l - naphthethyl] acetamide, amorphous form of N-[2-(7-methoxy-l -naphthethyl] acetamide and pharmaceutical compositions thereof.

7. 发明公开

EP2496595A2 PROCESS FOR THE PREPARATION OF IRON (III) CARBOXYMALTOSE COMPLEX 审中-公开
标题翻译：制备铁（III）羧基羧酸络合物的方法
公开(公告)号：EP2496595A2
公开(公告)日：2012-09-12
申请号：EP09851061.3
申请日：2009-11-04
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili , VENKAT REDDY, Buthukuri
IPC分类号： C07H23/00
CPC分类号： C07H23/00
摘要： The present invention related to novel processes for the preparation of iron (III) carboxymaltose complex. Thus, for example, heating a mixture of one or more maltodextrins, ferric hydroxide and water, oxidizing the iron maltodextrin complex obtained using an aqueous sodium hypochlorite solution and maintaining at 25°C to 125°C to obtain iron (III) carboxymaltose complex.
摘要翻译：本发明涉及用于制备铁（III）羧基麦芽糖络合物的新方法。因此，例如，加热一种或多种麦芽糖糊精，氢氧化铁和水的混合物，氧化使用次氯酸钠水溶液获得的铁麦芽糖糊精配合物，并保持在25℃至125℃以获得羧基麦芽糖铁络合物。

8. 发明授权

EP1737850B1 A NOVEL PROCESS FOR THE PREPARATION OF LINEZOLID AND RELATED COMPOUNDS 有权
标题翻译： HERSTLELUNG利奈唑胺和相关链接的新方法
公开(公告)号：EP1737850B1
公开(公告)日：2007-10-03
申请号：EP04728229.8
申请日：2004-04-19
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili
IPC分类号： C07D413/10 , C07D263/20
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.

9. 发明公开

EP1737850A2 A NOVEL PROCESS FOR THE PREPARATION OF LINEZOLID AND RELATED COMPOUNDS 有权
标题翻译：一种用于制备LINEZOLID和相关化合物的新方法
公开(公告)号：EP1737850A2
公开(公告)日：2007-01-03
申请号：EP04728229.8
申请日：2004-04-19
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , KRISHNA REDDY, Pingili
IPC分类号： C07D413/10 , C07D263/20
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：本发明提供了制备5-氨基甲基取代的恶唑烷酮的新方法，恶唑烷酮抗菌剂包括利奈唑胺的关键中间体。因此，利奈唑胺通过以下步骤制备：a）使3-氟-4-吗啉基苯胺与R-表氯醇反应; b）使上述制得的N- [3-氯-2-（R） - 羟丙基] -3-氟-4-吗啉基苯胺羰基化; 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）将上面制得的（S）-N - [[3- [3-氟-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]邻苯二甲酰亚胺与肼水合物反应; 和e）将上面制得的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。

10. 发明公开

EP2989097A1 IMPROVED PROCESSES FOR THE PREPARATION OF LINEZOLID USING NOVEL INTERMEDIATES 审中-公开
标题翻译： VERBESSERTE VERFAHREN ZUR HERSTELLUNG VON LINEZOLID MITTELS NEUARTIGER ZWISCHENPRODUKTE
公开(公告)号：EP2989097A1
公开(公告)日：2016-03-02
申请号：EP13883336.3
申请日：2013-04-25
申请人： Symed Labs Limited
发明人： MOHAN RAO, Dodda , VENKAT REDDY, Buthukuri
IPC分类号： C07D413/12
CPC分类号： C07D263/24 , C07D209/48 , C07D263/20 , C07D295/135
摘要： Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of Linezolid, in high yield and purity, using novel intermediates. In one aspect, provided herein are efficient, industrially advantageous and environmentally friendly processes for the preparation of linezolid, in high yield and with high purity, using novel intermediates. The processes disclosed herein avoid the tedious and cumbersome procedures of the prior processes, thereby resolving the problems associated with the processes described in the prior art, which is more convenient to operate at lab scale and in commercial scale operations.
摘要翻译：本文提供了使用新型中间体以高产率和纯度制备利奈唑胺的商业可行和工业上有利的方法。在一个方面，本文提供了使用新型中间体以高产率和高纯度制备利奈唑胺的有效，工业上有利且环境友好的方法。本文公开的方法避免了先前方法的繁琐而繁琐的过程，从而解决了与现有技术中描述的方法相关的问题，这在实验室规模和商业规模操作中更方便。

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