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1. 发明申请

WO2006016203A1 AN IMPROVED PROCESS FOR THE PREPARATION OF IRINOTECAN HYDROCHLORIDE TRIHYDRATE 审中-公开
标题翻译：制备氯硝酸三氯化钛的改进方法
公开(公告)号：WO2006016203A1
公开(公告)日：2006-02-16
申请号：PCT/IB2004/002626
申请日：2004-08-09
申请人： SHILPA MEDICARE LIMITED , VISHNUKANT, B. , PUROHIT, Prashant , PAPARAO, K. , VEERESHAPA
发明人： VISHNUKANT, B. , PUROHIT, Prashant , PAPARAO, K. , VEERESHAPA
IPC分类号： C07D491/22
CPC分类号： C07D211/58
摘要： The invention relates to an improved process for the preparation of Irinotecan hydrochloride trihydrate of formula (4) of enhanced yield, purity by contacting 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride with 7-ethyl-10 hydroxy-camptothecin [IRT-3 (synthetic)] to obtain crude Irinotecan which is subsequently purified by solvent treatment, obtaining purified irinotecan which is converted into irinotecan hydrochloride trihydrate and the invention also relates to a report of the compound 1-chlorocorbonyl-4-iperidinopiperidine hydrochloride of formula (1) and its process for preparation.
摘要翻译：本发明涉及通过使1-氯羰基-4-哌啶基哌啶盐酸盐与7-乙基-10-羟基喜树碱[IRT-3（合成））接触来制备式（4）的盐酸伊立替康三水合物的改进方法，其具有提高的产率， ]以获得粗品伊立替康，其随后通过溶剂处理纯化，得到纯化的伊立替康，其转化为盐酸伊立替康三水合物，本发明还涉及式（1）的化合物1-氯羰基-4-哌啶哌啶盐酸盐及其方法准备。

2. 发明申请

WO2009078036A2 PROCESS AND INTERMEDIATE OF LETROZOLE 审中-公开
标题翻译： LETROZOLE的工艺和中间体
公开(公告)号：WO2009078036A2
公开(公告)日：2009-06-25
申请号：PCT/IN2008/000801
申请日：2008-12-01
申请人： SHILPA MEDICARE LTD. , VISHNUKANT, B.
发明人： VISHNUKANT, B.
IPC分类号： C07D249/08 , C07C257/06
CPC分类号： C07C257/06 , C07D249/08
摘要： The present invention relates to a process for the preparation of Letrozole involving the use of novel intermediate of Formula I.
摘要翻译：本发明涉及一种涉及使用式I的新型中间体的来曲唑的制备方法。

3. 发明申请

WO2007105231A1 IMPROVED PROCESS FOR HIGH PURITY ANASTROZOLE 审中-公开
标题翻译：改进高纯度阿诺方唑的方法
公开(公告)号：WO2007105231A1
公开(公告)日：2007-09-20
申请号：PCT/IN2007/000090
申请日：2007-03-08
申请人： SHILPA MEDICARE LTD. , VISHNUKANT, B. , PUROHIT, Prashant , PAPARAO, K. , VEERESHAPPA, Veereshappa
发明人： VISHNUKANT, B. , PUROHIT, Prashant , PAPARAO, K. , VEERESHAPPA, Veereshappa
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： The present invention relates to an improved process for the preparation of anastrozole having enhanced purity from crude anastrozole having isomeric impurity content up to less than 1 %. The invention also relates to a pocess comprising steps of converting (3- cyanomethyl-5-methylphenyl) acetonitrile to 2-[(3-cyanodimethylmethyl)-5-methyl phenyl]- meiliyl propiononitrile (I I) by C- alkylation, which is further converted into 2-[3-halomethyl- 5-cyanodimethyl methyl)phenyl] methyl propiononitrile (ill) by radical bromination and further to crude anastrozole by reacting (I II) with sodium salt of 1,2,4-triazole, purification of the crude anastrozole by preparing its acid addition salt, generating required final anaslrozole from the acid addition salt.
摘要翻译：本发明涉及一种制备具有高达小于1％的异构杂质含量的粗阿那曲唑具有增强的纯度的阿那曲唑的改进方法。本发明还涉及包含以下步骤的步骤：通过C-烷基化将（3-氰基甲基-5-甲基苯基）乙腈转化为2- [（3-氰基二甲基甲基）-5-甲基苯基] - 甲酰基丙腈（II），其进一步通过自由基溴化转化为2- [3-卤代甲基-5-氰基二甲基甲基）苯基]甲基丙腈（不合），再通过使（I II）与1,2,4-三唑的钠盐反应，将其纯化为阿那曲唑粗制阿那曲唑通过制备其酸加成盐，从酸加成盐产生所需的最终阿斯呋唑。

4. 发明申请

WO2008035377A3 NOVEL INTERMEDIATES FOR THE PREPARATION OF CAMPTOTHECIN ANALOGUES 审中-公开
标题翻译：制备CAMPTOTHECIN类似物的新型中间体
公开(公告)号：WO2008035377A3
公开(公告)日：2009-01-08
申请号：PCT/IN2007000381
申请日：2007-08-31
申请人： SHILPA MEDICARE LTD , VISHNUKANT B
发明人： VISHNUKANT B
IPC分类号： C07D401/04 , C07D491/22
CPC分类号： C07D491/22 , C07D211/58 , Y02P20/55
摘要： The present invention relates to novel intermediate compounds of formula (Ia) and its salts thereof, wherein R is an amino protecting group, R1 is selected from the group consisting of hydrogen, an alkyl, araalkyl, hydroxymethyl, carboxymethyl, acyloxymethyl, trialkylsilyl or an N-substituted alkyl amine where nitrogen forms the linking atom. The invention also relates to the use of these novel intermediate compounds of formula (Ia) for the preparation of camptothecin analogues and its salts, more particularly the anti-cancer drug irinotecan and its pharmaceutically accepted salts.
摘要翻译：本发明涉及式（Ia）的新型中间体化合物及其盐，其中R是氨基保护基，R 1选自氢，烷基，芳烷基，羟甲基，羧甲基，酰氧基甲基，三烷基甲硅烷基或其中氮形成连接原子的N-取代的烷基胺。本发明还涉及式（Ia）的这些新型中间体化合物在制备喜树碱类似物及其盐中的用途，更具体地说是抗癌药物伊立替康及其药学上可接受的盐。

5. 发明申请

WO2008035377A2 NOVEL INTERMEDIATES FOR THE PREPARATION OF CAMPTOTHECIN ANALOGUES 审中-公开
标题翻译：制备CAMPTOTHECIN类似物的新型中间体
公开(公告)号：WO2008035377A2
公开(公告)日：2008-03-27
申请号：PCT/IN2007/000381
申请日：2007-08-31
申请人： SHILPA MEDICARE LTD. , VISHNUKANT, B.
发明人： VISHNUKANT, B.
IPC分类号： C07D401/04 , C07D491/22
CPC分类号： C07D491/22 , C07D211/58 , Y02P20/55
摘要： The present invention relates to novel intermediate compounds of formula (Ia) and its salts thereof, wherein R is an amino protecting group, R 1 is selected from the group consisting of hydrogen, an alkyl, araalkyl, hydroxymethyl, carboxymethyl, acyloxymethyl, trialkylsilyl or an N-substituted alkyl amine where nitrogen forms the linking atom. The invention also relates to the use of these novel intermediate compounds of formula (I a ) for the preparation of camptothecin analogues and its salts, more particularly the anti-cancer drug irinotecan and its pharmaceutically accepted salts.
摘要翻译：本发明涉及式（Ia）的新型中间体化合物及其盐，其中R是氨基保护基，R 1选自氢，烷基，芳烷基，羟甲基羧甲基，酰氧基甲基，三烷基甲硅烷基或N-取代的烷基胺，其中氮形成连接原子。本发明还涉及这些用于制备喜树碱类似物及其盐的这些新型中间体式化合物（更优选抗癌药物伊立替康及其药学上可接受的盐）的用途。

6. 发明申请

WO2008026222A2 PROCESS AND INTERMEDIATES OF 2,2' DIFLUORONUCLEOSIDES 审中-公开
标题翻译： 2,2'二异氰尿嘧啶的工艺和中间体
公开(公告)号：WO2008026222A2
公开(公告)日：2008-03-06
申请号：PCT/IN2007/000354
申请日：2007-08-20
申请人： SHILPA MEDICARE LTD , VISHNUKANT, B , PUROHIT, Prashant , PAPARAO, K , VEERESHAPPA, Veereshappa
发明人： VISHNUKANT, B , PUROHIT, Prashant , PAPARAO, K , VEERESHAPPA, Veereshappa
IPC分类号： C07H5/02
CPC分类号： C07H5/02
摘要： The present invention provides novel 1-trihaloacetimido-2-deoxy-2,2'-difluoro-3,5-di-O-protected ribose intermediates. The compounds are useful in the preparation of 2'-deoxy-2,2'-difluoro-beta nucleosides and more particularly 2'-deoxy-2,2'-difluoro-beta cytidine and other beta anomer nucleosides and its salts having antiviral and anticancer activity
摘要翻译：本发明提供新的1-三卤乙酰亚氨基-2-脱氧-2,2'-二氟-3,5-二-O-保护的核糖中间体。该化合物可用于制备2'-脱氧-2,2'-二氟-β核苷，更具体地可用于2'-脱氧-2,2'-二氟-β胞苷和其它β-异头核苷及其具有抗病毒和/ 抗癌活性

7. 发明申请

WO2009078036A3 PROCESS AND INTERMEDIATE OF LETROZOLE 审中-公开
标题翻译：氯吡格雷的方法和中间体
公开(公告)号：WO2009078036A3
公开(公告)日：2009-10-22
申请号：PCT/IN2008000801
申请日：2008-12-01
申请人： SHILPA MEDICARE LTD , VISHNUKANT B
发明人： VISHNUKANT B
IPC分类号： C07D249/08 , C07C257/06
CPC分类号： C07C257/06 , C07D249/08
摘要： The present invention relates to a process for the preparation of Letrozole involving the use of novel intermediate of Formula I.
摘要翻译：本发明涉及一种涉及使用式I的新型中间体的来曲唑的制备方法。

8. 发明申请

WO2008026222A3 PROCESS AND INTERMEDIATES OF 2,2' DIFLUORONUCLEOSIDES 审中-公开
标题翻译： 2,2'二异氰尿嘧啶的工艺和中间体
公开(公告)号：WO2008026222A3
公开(公告)日：2009-06-18
申请号：PCT/IN2007000354
申请日：2007-08-20
申请人： SHILPA MEDICARE LTD , VISHNUKANT B , PUROHIT PRASHANT , PAPARAO K , VEERESHAPPA VEERESHAPPA
发明人： VISHNUKANT B , PUROHIT PRASHANT , PAPARAO K , VEERESHAPPA VEERESHAPPA
IPC分类号： C07H5/02
CPC分类号： C07H5/02
摘要： The present invention provides novel 1-trihaloacetimido-2-deoxy-2,2'-difluoro-3,5-di-O-protected ribose intermediates. The compounds are useful in the preparation of 2'-deoxy-2,2'-difluoro-beta nucleosides and more particularly 2'-deoxy-2,2'-difluoro-beta cytidine and other beta anomer nucleosides and its salts having antiviral and anticancer activity
摘要翻译：本发明提供新的1-三卤乙酰亚氨基-2-脱氧-2,2'-二氟-3,5-二-O-保护的核糖中间体。该化合物可用于制备2'-脱氧-2,2'-二氟-β核苷，更具体地可用于2'-脱氧-2,2'-二氟-β胞苷和其它β-异头核苷及其具有抗病毒和/ 抗癌活性

9. 发明申请

WO2007105231B1 IMPROVED PROCESS FOR HIGH PURITY ANASTROZOLE 审中-公开
标题翻译：改进高纯度溶胶的方法
公开(公告)号：WO2007105231B1
公开(公告)日：2007-11-22
申请号：PCT/IN2007000090
申请日：2007-03-08
申请人： SHILPA MEDICARE LTD , VISHNUKANT B , PUROHIT PRASHANT , PAPARAO K , VEERESHAPPA VEERESHAPPA
发明人： VISHNUKANT B , PUROHIT PRASHANT , PAPARAO K , VEERESHAPPA VEERESHAPPA
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： The present invention relates to an improved process for the preparation of anastrozole having enhanced purity from crude anastrozole having isomeric impurity content up to less than 1 %. The invention also relates to a pocess comprising steps of converting (3- cyanomethyl-5-methylphenyl) acetonitrile to 2-[(3-cyanodimethylmethyl)-5-methyl phenyl]- meiliyl propiononitrile (II) by C- alkylation, which is further converted into 2-[3-halomethyl- 5-cyanodimethyl methyl)phenyl] methyl propiononitrile (Ill) by radical bromination and further to crude anastrozole by reacting (III) with sodium salt of 1,2,4-triazole, purification of the crude anastrozole by preparing its acid addition salt, generating required final anaslrozole from the acid addition salt.
摘要翻译：本发明涉及一种用于制备具有高达小于1％的异构杂质含量的粗制阿拉曲唑具有增强的纯度的阿那曲唑的改进方法。本发明还涉及包含以下步骤的步骤：通过C-烷基化将（3-氰基甲基-5-甲基苯基）乙腈转化为2- [（3-氰基二甲基甲基）-5-甲基苯基] - 丙烯酰基丙腈（II），其进一步通过自由基溴化转化为2- [3-卤代甲基-5-氰基二甲基甲基）苯基]甲基丙腈（III），再通过（III）与1,2,4-三唑的钠盐反应，粗制的阿那曲唑，阿那曲唑通过制备其酸加成盐，从酸加成盐产生所需的最终阿斯苯唑。

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