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1. 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

2. 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。

3. 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

4. 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。

5. 发明申请

WO2012160568A1 PROCESS FOR PREPARING DOCETAXEL TRIHYDRATE POLYMORPH 审中-公开
标题翻译：制备三氯乙烯聚合物的方法
公开(公告)号：WO2012160568A1
公开(公告)日：2012-11-29
申请号：PCT/IN2011/000587
申请日：2011-08-29
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
发明人： SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
IPC分类号： C07D305/14 , A61K31/335 , A61K31/337 , A61P35/00
CPC分类号： A61K31/337
摘要： A crystalline form of docetaxel trihydrate designated as Form-VK and process for preparation thereof are provided. A substantially pure trihydrate crystalline product obtained by the process is also provided. The crystalline product of the process which has an XRPD pattern as per Fig-1 is useful as an active pharmaceutical in pharmaceutical composition and has anti-cancer activity.
摘要翻译：提供了称为Form-VK的多西他赛三水合物的结晶形式及其制备方法。还提供通过该方法获得的基本上纯的三水合物结晶产物。具有根据图1的XRPD图案的方法的结晶产物可用作药物组合物中的活性药物并具有抗癌活性。

6. 发明申请

WO2012143932A1 CRYSTALLINE STRONTIUM RANELATE FORM-S 审中-公开
标题翻译：晶体结构形式
公开(公告)号：WO2012143932A1
公开(公告)日：2012-10-26
申请号：PCT/IN2011/000590
申请日：2011-08-29
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
发明人： SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
IPC分类号： A61K31/381
CPC分类号： C07D333/38 , C07D333/40
摘要： Crystalline strontium ranelate form-S and process for preparation thereof are provided. Also provided is a substantially pure crystalline product obtained by the process having characteristic XRPD peak set of 7.70, 15.33, 16.46, 19.55, 20.11, 22.08, 27.90, 29.47±0.10 20° and water content in the range of 20.5 to 23.0% w/w, which is therapeutically used for the treatment of bone diseases like osteoporosis.
摘要翻译：提供了雷奈酸锶晶型-S及其制备方法。还提供了通过该方法获得的基本上纯的结晶产物，其具有7.70,15.33,16.46,19.55,20.11,22.08,27.90,29.47±0.10 20°的特征XRPD峰值，水含量在20.5至23.0％w / w，其被治疗用于治疗诸如骨质疏松症之类的骨疾病。

7. 发明申请

WO2012070059A1 FINGOLIMOD POLYMORPHS AND THEIR PROCESSES 审中-公开
标题翻译： FINGOLIMOD POLYMORPHS及其方法
公开(公告)号：WO2012070059A1
公开(公告)日：2012-05-31
申请号：PCT/IN2011/000586
申请日：2011-08-29
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
发明人： SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , SINGH, Vinod Kumar
IPC分类号： C07C215/28 , C07C213/00 , A61K31/137 , A61P37/02
CPC分类号： C07C213/10 , C07B2200/13 , C07C215/28
摘要： Crystalline polymorphic forms of fingolimod hydrochloride, their XRPD patterns and preparation are provided. Processes for preparing crystalline polymorphic forms-α, β and μ substantially free from processes related impurities are also provided. The crystalline polymorphic forms of fingolimod hydrochloride are useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment or prevention of autoimmune related disorder including multiple sclerosis.
摘要翻译：提供盐酸芬戈莫德的结晶多晶型物质，其XRPD图谱及其制备方法。还提供了用于制备基本上不含工艺相关杂质的结晶多晶型-a，β和μ的方法。盐酸芬戈莫德的结晶多晶型可用作用于治疗或预防包括多发性硬化的自身免疫相关疾病的药物组合物中的活性药物成分。

8. 发明申请

WO2012131698A1 PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE 审中-公开
标题翻译：制备DOCETAXEL及其水合物的方法
公开(公告)号：WO2012131698A1
公开(公告)日：2012-10-04
申请号：PCT/IN2011/000588
申请日：2011-08-29
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , RAFIUDDIN, .
发明人： SHRAWAT, Vimal Kumar , ., Veereshappa , PUROHIT, Prashant , RAFIUDDIN, .
IPC分类号： C07D305/14 , A61K31/337 , A61P35/00
CPC分类号： C07D305/14 , A61K31/337
摘要： Disclosed is a process of preparation of (2R,3S)-N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(P)-20-epoxy-l,2(a), 4,7(P), 10(β), 13(a)-hexa hydroxyl tax-l l-en-9-one 4-acetate 2-benzoate (docetaxel) and its trihydrate (I).
摘要翻译：公开了制备（2R，3S）-N-羧基-3-苯基异丝氨酸，N-叔丁酯，13-酯与5（P）-20-环氧-1,2（a），4， 7（P），10（ß），13（a） - 六羟基tax-11-烯-9-酮4-乙酸酯2-苯甲酸酯（多西紫杉醇）及其三水合物（I）。

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