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1. 发明授权

US08895772B2 Process for preparing bicalutamide 有权
标题翻译：制备比卡鲁胺的方法
公开(公告)号：US08895772B2
公开(公告)日：2014-11-25
申请号：US13634103
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Karri Papa Rao , Rafiuddin , Prashant Purohit
发明人： Vimal Kumar Shrawat , Karri Papa Rao , Rafiuddin , Prashant Purohit
IPC分类号： C07C381/00 , C07C255/50 , C07C253/30 , C07C315/02 , C07C253/34
CPC分类号： C07C253/30 , C07C253/34 , C07C315/02 , C07C317/46
摘要： The present invention provide processes for the preparation of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I).The present application also provides a method of purification of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I) using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D. The crystalline product of the process according to the present invention having an XRDP pattern as per FIG. 1, is useful as an active pharmaceutical and has anti-androgenic activity.
摘要翻译：本发明提供N- [4-氰基-3-（三氟甲基）苯基] -3 - [（4-氟苯基）磺酰基] -2-羟基-2-甲基丙酰胺（I）的制备方法。本申请还提供了使用乙酸乙酯的N- [4-氰基-3-（三氟甲基）苯基] -3 - [（4-氟苯基）磺酰基] -2-羟基-2-甲基丙酰胺（I）乙酸酯溶剂，产生产物，基本上不含工艺相关杂质A，B，C和D.根据本发明方法的结晶产物具有如图1所示的XRDP图案。 1可用作活性药物并具有抗雄激素活性。

2. 发明授权

US08829210B2 Process for preparing docetaxel and its hydrate 有权
标题翻译：多西紫杉醇及其水合物的制备方法
公开(公告)号：US08829210B2
公开(公告)日：2014-09-09
申请号：US13634612
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Rafiuddin , Veereshappa , Prashant Purohit
发明人： Vimal Kumar Shrawat , Rafiuddin , Veereshappa , Prashant Purohit
IPC分类号： C07D305/14 , A61K31/337
CPC分类号： C07D305/14 , A61K31/337
摘要： The present invention provide process of preparation of (2R,3S)—N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(β)-20-epoxy-1,2(α),4,7(β),10(β),13(α)-hexa hydroxy tax-11-en-9-one 4-acetate 2-benzoate or docetaxel and its trihydrate (I)
摘要翻译：本发明提供了制备（2R，3S）-N-羧基-3-苯基异丝氨酸，N-（叔丁基）-20-环氧-1,2（α）的N-叔丁酯，13-酯的方法， 4,7（＆bgr。），10（（bgr）），13（α） - 六羟基tax-11-烯-9-酮4-乙酸酯2-苯甲酸酯或多西紫杉醇及其三水合物（I）

3. 发明申请

US20140039209A1 PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE 有权
标题翻译：制备DOCETAXEL及其水合物的方法
公开(公告)号：US20140039209A1
公开(公告)日：2014-02-06
申请号：US13634612
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Rafiuddin , Prashant Purohit
发明人： Vimal Kumar Shrawat , Rafiuddin , Prashant Purohit
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , A61K31/337
摘要： The present invention provide process of preparation of (2R,3S)—N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(β)-20-epoxy-1,2(α),4,7(β),10(β),13(α)-hexa hydroxy tax-11-en-9-one 4-acetate 2-benzoate or docetaxel and its trihydrate (I)
摘要翻译：本发明提供了制备（2R，3S）-N-羧基-3-苯基异丝氨酸，N-叔丁酯，13-酯与5（β）-20-环氧-1,2（α），4 ，7（β），10（β），13（α） - 六羟基tax-11-烯-9-酮4-乙酸酯2-苯甲酸酯或多西他赛及其三水合物（I）

4. 发明申请

US20130217888A1 PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE 审中-公开
标题翻译：制备丁二酸二氢马来酸单氯化物的方法
公开(公告)号：US20130217888A1
公开(公告)日：2013-08-22
申请号：US13635097
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Seshachalam Unnam , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Seshachalam Unnam , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07D235/16
CPC分类号： C07D235/16 , A61K31/4184 , C07B2200/13 , C07C209/10
摘要： The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) The present application also provides a process of purification of Bendamustine hydrochloride or monohydrate to get substantially pure Bendamustine hydrochloride monohydrate crystalline Form-SM. The said Bendamustine hydrochloride monohydrate crystalline Form-SM is characterized by X-ray powder diffraction pattern comprising at least 5 characteristic peaks selected from the XRPD 2 theta degrees peaks at 7.42, 10.60, 11.17, 16.43, 17.94, 22.89, 26.33, 28.77, 30.28, 31.92, 40.89±0.1 2θ°.The present application also provides a process for the preparation of Bendamustine hydrochloride monohydrate crystalline Form-SM useful in making pharmaceutical composition for the treatment of cancer or similar proliferative disorders.
摘要翻译：本发明提供了制备式（I）的盐酸苯达莫司汀一水合物的方法。本申请还提供了盐酸苯达莫司汀或一水合物的纯化方法，以获得基本上纯的盐酸苯达莫司汀一水合物结晶形式-SM。所述盐酸苯达莫司汀一水合物结晶形式SM的特征在于X射线粉末衍射图，其包含从7.42,10.60,11.17,16.43,17.94,22.89,26.33,28.77,30.28处选择的XRPD2θ度峰中的至少5个特征峰，31.92，40.89±0.12θ。本申请还提供了制备用于制备用于治疗癌症或类似增殖性疾病的药物组合物的盐酸苯达莫司汀一水合物结晶形式-SM的方法。

5. 发明申请

US20080182990A1 Process for the Preparation of Irinotecan Hydrochloride Trihydrate 审中-公开
标题翻译：盐酸伊立替康三水合物的制备方法
公开(公告)号：US20080182990A1
公开(公告)日：2008-07-31
申请号：US11573397
申请日：2004-08-09
申请人： B. Vishnukant , Prashant Purohit , K. Paparao , Veereshapa
发明人： B. Vishnukant , Prashant Purohit , K. Paparao , Veereshapa
IPC分类号： C07D471/22
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-piperidinopiperidine 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（合成的））接触来制备式（4）的伊立替康盐酸三水合物的改进方法，其具有提高的产率，）]以获得随后通过溶剂处理纯化的粗制伊立替康，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-哌啶基哌啶盐酸盐及其准备过程

6. 发明申请

US20090286989A1 Process for High Purity Anastrozole 审中-公开
标题翻译：高纯度阿那曲唑的方法
公开(公告)号：US20090286989A1
公开(公告)日：2009-11-19
申请号：US12224965
申请日：2007-03-08
申请人： B. Vishnukant , Prashant Purohit , K. Paparao , Veereshappa Veereshappa
发明人： B. Vishnukant , Prashant Purohit , K. Paparao , 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 process 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。本发明还涉及一种包括以下步骤的方法：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）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（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呋唑。

7. 发明申请

US20130281739A1 FINGOLIMOD POLYMORPHS AND THEIR PROCESSES 有权
标题翻译： FINGOLIMOD POLYMORPHS及其方法
公开(公告)号：US20130281739A1
公开(公告)日：2013-10-24
申请号：US13635207
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Veereshappa N/A , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Veereshappa N/A , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07C215/28 , C07C213/10
CPC分类号： C07C213/10 , C07B2200/13 , C07C215/28
摘要： The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof.The application provides processes for preparation of crystalline polymorphic forms-α, β and μ substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which 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：本发明提供了芬戈莫德HCl（I）的结晶多晶型物及其制备方法。该应用提供了制备基本上不含工艺相关杂质的结晶多晶型α，β和μ的方法。通过根据本发明的方法获得的具有根据图1和2的XRDP图案的芬戈莫德HCl（I）的结晶多晶型物。 1,3和5，其可用作用于治疗或预防包括多发性硬化的自身免疫相关病症的药物组合物中的活性药物成分。

8. 发明申请

US20130274501A1 PROCESS FOR PREPARING BICALUTAMIDE 有权
标题翻译：制备贝伐菌胺的方法
公开(公告)号：US20130274501A1
公开(公告)日：2013-10-17
申请号：US13634103
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Karri Papa Rao , N/A Rafiuddin , Prashant Purohit
发明人： Vimal Kumar Shrawat , Karri Papa Rao , N/A Rafiuddin , Prashant Purohit
IPC分类号： C07C253/30 , C07C253/34
CPC分类号： C07C253/30 , C07C253/34 , C07C315/02 , C07C317/46
摘要： The present invention provide processes for the preparation of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I).The present application also provides a method of purification of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I) using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D. The crystalline product of the process according to the present invention having an XRDP pattern as per FIG. 1, is useful as an active pharmaceutical and has anti-androgenic activity.
摘要翻译：本发明提供N- [4-氰基-3-（三氟甲基）苯基] -3 - [（4-氟苯基）磺酰基] -2-羟基-2-甲基丙酰胺（I）的制备方法。本申请还提供了使用乙酸乙酯的N- [4-氰基-3-（三氟甲基）苯基] -3 - [（4-氟苯基）磺酰基] -2-羟基-2-甲基丙酰胺（I）乙酸酯溶剂，产生产物，基本上不含工艺相关杂质A，B，C和D.根据本发明方法的结晶产物具有如图1所示的XRDP图案。 1可用作活性药物并具有抗雄激素活性。

9. 发明授权

US09266816B2 Fingolimod polymorphs and their processes 有权
标题翻译：芬戈莫德多晶型物及其工艺
公开(公告)号：US09266816B2
公开(公告)日：2016-02-23
申请号：US13635207
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Veereshappa , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Veereshappa , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07C213/10 , C07C215/10 , C07C215/28
CPC分类号： C07C213/10 , C07B2200/13 , C07C215/28
摘要： The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof.The application provides processes for preparation of crystalline polymorphic forms-α, β and μ substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which 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：本发明提供了芬戈莫德HCl（I）的结晶多晶型物及其制备方法。该应用提供了制备结晶多晶型α-bgr的方法。并且μ基本上不含与工艺相关的杂质。通过根据本发明的方法获得的具有根据图1和2的XRDP图案的芬戈莫德HCl（I）的结晶多晶型物。 1,3和5，其可用作用于治疗或预防包括多发性硬化的自身免疫相关病症的药物组合物中的活性药物成分。

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