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1. 发明申请

WO2009122429A2 CRYSTALLINE OXYBUTYNIN AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：结晶氧化丁烯及其制备方法
公开(公告)号：WO2009122429A2
公开(公告)日：2009-10-08
申请号：PCT/IN2009/000074
申请日：2009-02-04
申请人： MATRIX LABORATORIES LIMITED , RAY, Purna, Chandra , SETHI, Madhuresh , MAHAJAN, Sanjay , TYAGI, Om, Dutt
发明人： RAY, Purna, Chandra , SETHI, Madhuresh , MAHAJAN, Sanjay , TYAGI, Om, Dutt
IPC分类号： C07C219/20
CPC分类号： C07C219/20 , C07B2200/13 , C07C2601/14
摘要： The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.
摘要翻译：本发明涉及结晶奥昔布宁碱及其制备方法。此外，本发明公开了使用结晶奥昔布宁碱制备奥昔布宁的酸加成盐的方法。

2. 发明申请

WO2008155780A2 IMPROVED PROCESS FOR THE PREPARATION OF PURE RABEPRAZOLE 审中-公开
标题翻译：用于制备纯紫杉酚的改进方法
公开(公告)号：WO2008155780A2
公开(公告)日：2008-12-24
申请号：PCT/IN2008/000388
申请日：2008-06-19
申请人： MATRIX LABORATORIES LTD , TYAGI, Om, Dutt , RAY, Purna, Chandra , SETHI, Madhuresh, Kumar , CHAVHAN, Bhausaheb
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , SETHI, Madhuresh, Kumar , CHAVHAN, Bhausaheb
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a process for the preparation of pure Rabeprazole sulfoxide using the solvent mixture for the extraction steps and this invention further relates to the process for the preparation of amorphous Rabeprazole sodium using pure rabeprazole base in presence of aqueous NaOH and water miscible solvent and adding an anti-solvent.
摘要翻译：本发明涉及一种使用溶剂混合物制备纯拉贝拉唑亚砜的方法，本发明还涉及在NaOH水溶液和水混溶性溶剂存在下，使用纯雷贝拉唑碱制备无定形雷贝拉唑钠的方法并加入抗溶剂。

3. 发明申请

WO2009090544A3 PROCESS FOR PRODUCING AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
公开(公告)号：WO2009090544A3
公开(公告)日：2009-07-23
申请号：PCT/IB2009/000068
申请日：2009-01-15
申请人： MATRIX LABORATORIES LIMITED , RAO, P. V. Srinivas , CHAUHAN, Yogendra, Kumar , SRIVASTAVA, Tushar, Kumar , RAY, Purna, Chandra , TYAGI, Om, Dutt
发明人： RAO, P. V. Srinivas , CHAUHAN, Yogendra, Kumar , SRIVASTAVA, Tushar, Kumar , RAY, Purna, Chandra , TYAGI, Om, Dutt
IPC分类号： C07D207/34
摘要： Disclosed herein is an improved process for producing amorphous atorvastatin calcium and a method of packaging thereof.

4. 发明申请

WO2009072139A8 PROCESS FOR PRODUCING 2-[1-METHYL-5-(4-METHYLBENZOYL)- PYRROL-2- YL]ACETIC ACID OR SALT THEREOF 审中-公开
公开(公告)号：WO2009072139A8
公开(公告)日：2009-06-11
申请号：PCT/IN2008/000231
申请日：2008-04-08
申请人： MATRIX LABORATORIES LIMITED , KARUSALA, Nageswara, Rao , CHAVHAN, Bhausaheb , RATHINAPANDIAN, Jebaraj , VEERANKI, Muneendra, Kumar , RAY, Purna, Chandra , TYAGI, Om, Dutt
发明人： KARUSALA, Nageswara, Rao , CHAVHAN, Bhausaheb , RATHINAPANDIAN, Jebaraj , VEERANKI, Muneendra, Kumar , RAY, Purna, Chandra , TYAGI, Om, Dutt
IPC分类号： C07D207/337
摘要： The present invention relates to novel process for the preparation of tolmetin sodium, by employing easily available starting material and suitable reaction conditions. This invention is further related to novel crystalline forms of tolmetin methyl ester, tolmetin and tolmetin sodium and their process for the preparation.

5. 发明申请

WO2009125430A8 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
公开(公告)号：WO2009125430A8
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.

6. 发明申请

WO2008081475A2 NOVEL CRYSTALLINE FORMS OF ZOLMITRIPTAN 审中-公开
标题翻译： ZOLMITRIPTAN的新型结晶形式
公开(公告)号：WO2008081475A2
公开(公告)日：2008-07-10
申请号：PCT/IN2007/000620
申请日：2007-12-31
申请人： MATRIX LABORATORIES LTD , RAY, Purna, Chandra , ROHATGI, Amit , RAO, Jetti, Ramakoteswara , TYAGI, Om, Dutt
发明人： RAY, Purna, Chandra , ROHATGI, Amit , RAO, Jetti, Ramakoteswara , TYAGI, Om, Dutt
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention provides novel crystalline polymorphic forms of zolmitriptan characterized by.different solid state techniques. The novel processes for their preparation are also disclosed. Further, the present invention is also directed to novel processes for the preparation of zolmitriptan crystalline form A.
摘要翻译：本发明提供了以不同固态技术为特征的佐米曲普坦的新颖结晶多晶型形式。还公开了其制备的新方法。此外，本发明还涉及制备佐米曲坦晶型A的新方法。

7. 发明申请

WO2008035378A2 AN IMPROVED PROCESS FOR THE PREPARATION OF THALIDOMIDE 审中-公开
标题翻译：改进制备噻吗二胺的方法
公开(公告)号：WO2008035378A2
公开(公告)日：2008-03-27
申请号：PCT/IN2007/000413
申请日：2007-09-13
申请人： MATRIX LABORATORIES LTD , RAY, Purna, Chandra , TUMMANEPALLY, Jagan, Mohana, Chary , RATHINAPANDIAN, Jebaraj , TYAGI, Om, Dutt
发明人： RAY, Purna, Chandra , TUMMANEPALLY, Jagan, Mohana, Chary , RATHINAPANDIAN, Jebaraj , TYAGI, Om, Dutt
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： An improved process for the preparation of Thalidomide a TNF-alpha inhibitor by the conversion of N-phthaloyl L-glutamine in presence of an active ingredient of inorganic acid salts such as 1,1-Carbonyldi(1,2,4-triazole) as a condensing agent.
摘要翻译：在无机酸盐如1,1-羰基（1,2,4-三唑）的活性成分存在下，通过N-邻苯二甲酰基L-谷氨酰胺的转化制备沙利度胺TNF-α抑制剂的改进方法为缩合剂。

8. 发明申请

WO2009125430A3 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
公开(公告)号：WO2009125430A3
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.

9. 发明申请

WO2008142706A2 NOVEL PROCESS FOR THE SYNTHESIS OF PIOGLITAZONE AND ITS SALTS THEREOF 审中-公开
标题翻译：用于合成PIOGLITAZONE及其盐的新方法
公开(公告)号：WO2008142706A2
公开(公告)日：2008-11-27
申请号：PCT/IN2008/000315
申请日：2008-05-19
申请人： MATRIX LABORATORIES LTD , TYAGI, Om, Dutt , RAY, Purna, Chandra , RAO, Konudula, Babu , CHAUHAN, Yogendra, Kumar , NALLA, Raja, Mahendar, Reddy , PRASAD, Gadamsetty
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , RAO, Konudula, Babu , CHAUHAN, Yogendra, Kumar , NALLA, Raja, Mahendar, Reddy , PRASAD, Gadamsetty
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Present invention relates to an improved process for the preparation of thiazolidinedione derivatives. Further the invention provides the hydrogenation of acid addition salt of benzylidene compound with less reducing agent under low Hydrogen gas pressure to get substantially pure thiazolidinedione derivatives with improved yields.
摘要翻译：本发明涉及一种制备噻唑烷二酮衍生物的改进方法。此外，本发明提供了在低氢气压力下用较少还原剂氢化亚苄基化合物的酸加成盐，以获得基本上纯的噻唑烷二酮衍生物，其产率提高。

10. 发明申请

WO2009125430A2 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
标题翻译：改进生产DARIFENACIN的方法
公开(公告)号：WO2009125430A2
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.
摘要翻译：本发明公开了一种改进的达赖芬那克的制备方法，该方法包括使（2S，4R）-4-羟基-2-吡咯烷羧酸脱羧，然后进行原位甲苯磺酰化，得到1-甲苯磺酰基-3-（R） - （ - ）（R） - （ - ） - 羟基吡咯烷与甲基对甲苯磺酸酯反应，得到1-甲苯磺酰基-3-（S） - （ - ） - 甲氧基吡咯烷，使1-甲苯磺酰基-3- 在3-（S） - （+） - （1-氰基-1,1-二苯基甲基）-1-甲苯磺酰基吡咯烷存在下，将3-（S） - （ - ） - 甲氧基吡咯烷与二苯基乙腈反应，在酸性介质中在苯酚存在下保护3-（S） - （+） - （1-氰基-1,1-二苯基甲基）-1-甲苯磺酰基吡咯烷，得到3-（S） - （+） - （1-氰基 -1,1-二苯基甲基）吡咯烷，水解3-（S） - （+） - （1-氰基-1,1-二苯基甲基）吡咯烷，接着形成盐，得到3-（S） - （+） - - （+） - 酒石酸盐，将3-（S） - （+） - （1-氨基甲酰基-1,1-二苯基甲基）吡咯烷-L（+） - 酒石酸盐与 5-（2-溴乙基）-2,3--D 使用在溶剂中的碱的二氢苯并呋喃来给予达瑞那新。

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