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1. 发明授权

US09593083B2 Crystalline erlotinib hydrochloride process 有权
标题翻译：结晶埃洛替尼盐酸盐工艺
公开(公告)号：US09593083B2
公开(公告)日：2017-03-14
申请号：US14418449
申请日：2013-08-14
申请人： Shilpa Medicare Limited
发明人： Vimal Kumar Shrawat , Prashant Purohit , Rafiuddin Dr. , Vinod Kumar Singh , Akshay Kant Chaturvedi
IPC分类号： C07D239/94
CPC分类号： C07D239/94 , C07B2200/13
摘要： The present invention provides process for preparation of Crystalline Erlotinib HCl (I) Form-SE characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2θ° peaks selected from the XRPD peak set of 5.60, 10.00, 11.40, 13.00, 13.50, 15.20, 18.40, 20.65, 21.86, 23.5, 31.80, 32.13, 32.80, 34.40±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 213 to 217° C. (Peak −1) and 225 to 235° C. (Peak −2) and IR absorption characteristic peaks at approximately 3278 cm−1, 1948 cm−1, 1871 cm−1, 1632 cm−1, 1164 cm−1, 1024 cm−1, 940 cm−1 and 742 cm−1 useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment cancer.
摘要翻译：本发明提供了制备结晶埃洛替尼（I）形式SE的方法，其特征在于X射线粉末衍射图，其包含至少5个特征2＆amp; tt;峰，其选自XRPD峰组5.60,10.00,11.40,13.00,13.50 ，15.20，18.40，20.65，21.86，23.5，31.80，32.13，32.80，34.40±0.20 2;该等温线包含213-217℃（峰-1）和225-235℃之间的吸热峰。（峰-2）和IR吸收特征峰在大约3278cm-1,1948cm -1，1871cm -1，1632cm -1，1164cm -1，1024cm -1，940cm -1和742cm -1， 1可用作用于治疗癌症的药物组合物中的活性药物成分。

2. 发明申请

US20150111929A1 PROCESS FOR PREPARING CRYSTALLINE SORAFENIB TOSYLATE 审中-公开
标题翻译：制备水溶性磺酰苯甲酸酯的方法
公开(公告)号：US20150111929A1
公开(公告)日：2015-04-23
申请号：US14381226
申请日：2012-12-31
申请人： SHILPA MEDICARE LIMITED
发明人： Prashant Purohit , Sriram Rampalli , Mohanrao Seshagiri Vijaya Murali , Lavkumar Upalla
IPC分类号： C07D213/81
CPC分类号： C07D213/81 , A61K31/44
摘要： The present invention provides an industrially suitable process for the preparation of substantially pure 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide or Sorafenib and its tosylate salt, with a suitable impurity profile and without requirement of any additional purification steps. The present invention also provides Sorafenib base (II) as stable crystalline Form-SSB.The present invention further relates to a process for the preparation of crystalline Sorafenib tosylate Form-I which is free from contamination of any other polymorphic form of Sorafenib tosylate, for e.g. Form II or Form III, and does not involve any seeding requirement for crystallization step.
摘要翻译：本发明提供工业上合适的制备基本上纯的4- {4 - [（{[4-氯-3-（三氟甲基） - 苯基]氨基}羰基）氨基]苯氧基} -N-甲基吡啶-2-甲酸的方法，甲酰胺或索拉非尼及其甲苯磺酸盐，具有合适的杂质分布，并且不需要任何额外的纯化步骤。本发明还提供了索拉非尼碱（II）作为稳定的晶型SSB。本发明还涉及一种制备结晶索拉非尼甲苯磺酸盐形式I的方法，其不含任何其它多晶型索拉非尼甲苯磺酸盐的污染物，例如， II型或III型，不涉及结晶步骤的任何接种要求。

3. 发明授权

US09403785B2 Process for preparing amorphous cabazitaxel 有权
标题翻译：制备无定形卡巴他赛的方法
公开(公告)号：US09403785B2
公开(公告)日：2016-08-02
申请号：US14349332
申请日：2012-12-26
申请人： SHILPA MEDICARE LIMITED
发明人： Vimal Kumar Shrawat , Prashant Purohit , Rafiuddin Dr , Vinod Kumar Singh , Akshay Kant Chaturvedi
IPC分类号： C07D305/14 , C07D413/12
CPC分类号： C07D305/14 , C07D413/12
摘要： The present invention provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), and process for preparation thereof. The present application also provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.
摘要翻译：本发明提供了非溶剂化的（2α，5β，7β，10β，13α）-4-乙酰氧基-13 - （{（2R，3S）-3 [（叔丁氧基羰基）氨基] -2- 羟基-3-苯基丙酰基}氧基）-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧塔纳-1-烯-2-基苯甲酸酯或卡巴他赛（I），及其制备方法。本申请还提供（2α，5β，7β，10β，13α）-4-乙酰氧基-13 - （{（2R，3S）-3 [（叔丁氧基羰基）氨基] -2 - 羟基-3-苯基丙酰基}氧基）-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧树脂-11-烯-2-基苯甲酸酯或具有XRPD图案的卡巴他赛（I）。 1和IR光谱如图1所示。并且可用作其包含其的药物组合物中的活性药物并具有抗癌活性。

4. 发明申请

US20150057446A1 PROCESS FOR PREPARING DASATINIB MONOHYDRATE 审中-公开
标题翻译：用于制备单酯的方法
公开(公告)号：US20150057446A1
公开(公告)日：2015-02-26
申请号：US14382557
申请日：2013-04-16
申请人： SHILPA MEDICARE LIMITED
发明人： Prashant Purohit , Sriram Rampalli , Mohanrao Seshagiri Vijaya Murali , Lavkumar Upalla , Pradeep Pothana
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The present invention provides an improved process for preparing N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole carboxamide monohydrate or Dasatinib monohydrate (Formula A).
摘要翻译：本发明提供了制备N-（2-氯-6-甲基苯基）-2 - [[6- [4-（2-羟基乙基）-1-哌嗪基] -2-甲基-4-嘧啶基]氨基的改进方法 ] -5-噻唑甲酰胺一水合物或达沙替尼一水合物（式A）。

5. 发明申请

US20150175554A1 Highly pure bendamustine hydrochloride monohydrate 审中-公开
标题翻译：高纯度盐酸苯达莫司汀一水合物
公开(公告)号：US20150175554A1
公开(公告)日：2015-06-25
申请号：US14411399
申请日：2014-12-26
申请人： SHILPA MEDICARE LIMITED
发明人： Vimal Kumar Shrawat , Seshachalam Unnam , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07D235/16 , C07C209/10
CPC分类号： C07D235/16 , A61K31/4184 , C07B2200/13 , C07C209/10
摘要： The present invention provide processes for the preparation of highly pure Bendamustine hydrochloride monohydrate of formula (I) The present application relates to Bendamustine hydrochloride monohydrate crystalline Form-SM characterized by X-ray powder diffraction pattern as depicted in FIG. 1 consisting 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, and 40.89±0.1 2θ° having a purity of greater than 99.5% (by HPLC).The present application also provides a process for the preparation of highly pure 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）的高纯度盐酸苯达司汀一水合物的方法。本申请涉及如图1所示的以X射线粉末衍射图谱为特征的盐酸苯达莫司汀一水合物结晶形式SM。 1个选自XRPD2θ度峰的峰，其在7.42,10.60,11.17,16.43,17.94,22.89,26.33,27.77,30.28,31.92和40.89±0.1 2＆amp; t的峰上具有大于99.5％的纯度（通过HPLC ）。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高纯度盐酸苯达莫司汀一水合物结晶形式-SM的方法。

6. 发明授权

US09790185B2 Process for the preparation of regorafenib and its crystalline forms 有权
公开(公告)号：US09790185B2
公开(公告)日：2017-10-17
申请号：US15324683
申请日：2015-07-06
申请人： SHILPA MEDICARE LIMITED
发明人： Sriram Rampalli , Lav Kumar Upalla , Krishna Kumar Ramachandrula , Prashant Purohit , Chaturvedi Akshay Kant
IPC分类号： C07D213/81
CPC分类号： C07D213/81
摘要： The present invention relates to a process for the preparation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide or Regorafenib (I). The present invention further relates to a process for the purification of 4-[4-({[4-chloro-3-(trifluoromethyl) phenyl] carbamoyl} amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide or Regorafenib (I) to provide highly pure material.The present invention further relates to a process for the preparation stable crystalline material of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl pyridine-2-carboxamide or Regorafenib (I) useful in the preparation of pharmaceutical compositions for the treatment of cancer.

7. 发明申请

US20150299141A1 Crystalline Erlotinib Hydrochloride Process 审中-公开
标题翻译：结晶埃罗替尼盐酸盐工艺
公开(公告)号：US20150299141A1
公开(公告)日：2015-10-22
申请号：US14418449
申请日：2013-08-14
申请人： Shilpa Medicare Limited
发明人： Vimal Kumar Shrawat , Prashant Purohit , Rafiuddin Dr. , Vinod Kumar Singh , Akshay Kant Chaturvedi
IPC分类号： C07D239/94
CPC分类号： C07D239/94 , C07B2200/13
摘要： The present invention provides process for preparation of Crystalline Erlotinib HCl (I) Form-SE characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2θ° peaks selected from the XRPD peak set of 5.60, 10.00, 11.40, 13.00, 13.50, 15.20, 18.40, 20.65, 21.86, 23.5, 31.80, 32.13, 32.80, 34.40±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 213 to 217° C. (Peak -1) and 225 to 235° C. (Peak -2) and IR absorption characteristic peaks at approximately 3278 cm−1, 1948 cm−1, 1871 cm−1, 1632 cm−1, 1164 cm−1, 1024 cm−1, 940 cm−1 and 742 cm−1 useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment cancer.
摘要翻译：本发明提供了制备结晶埃洛替尼（I）形式SE的方法，其特征在于X射线粉末衍射图，其包含至少5个特征2＆amp; tt;峰，其选自XRPD峰组5.60,10.00,11.40,13.00,13.50 ，15.20，18.40，20.65，21.86，23.5，31.80，32.13，32.80，34.40±0.20 2;该等温线包含213-217℃（峰-1）和225-235℃之间的吸热峰。（峰-2）和IR吸收特征峰在大约3278cm-1,1948cm -1，1871cm -1，1632cm -1，1164cm -1，1024cm -1，940cm -1和742cm -1， 1可用作用于治疗癌症的药物组合物中的活性药物成分。

8. 发明授权

US09145406B2 Process for preparing dasatinib monohydrate 有权
标题翻译：制备达沙替尼一水合物的方法
公开(公告)号：US09145406B2
公开(公告)日：2015-09-29
申请号：US14382557
申请日：2013-04-16
申请人： SHILPA MEDICARE LIMITED
发明人： Prashant Purohit , Sriram Rampalli , Mohanrao Seshagiri Vijaya Murali , Lavkumar Upalla , Pradeep Pothana
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The present invention relates to an improved process for preparation of Dasatinib monohydrate Formula A, comprising the steps of: a) reacting the compound of Formula I with 1-(2-Hydroxyethyl)piperazine (Formula II) in the presence of acetonitrile solvent, an organic base and a phase transfer catalyst; b) heating the reaction mixture at 50-80° C.; c) adding water to the reaction mass obtained in step b); d) cooling the reaction mixture to a temperature below 35° C.; e) filtering and drying the material obtained in step d); f) optionally purifying the product obtained from step e); g) isolating the crystalline Dasatinib monohydrate.
摘要翻译：本发明涉及一种制备达沙替尼一水合物式A的改进方法，其包括以下步骤：a）在乙腈溶剂存在下使式I化合物与1-（2-羟乙基）哌嗪（式II）反应，有机碱和相转移催化剂; b）在50-80℃加热反应混合物; c）向步骤b）中获得的反应物质中加入水; d）将反应混合物冷却至低于35℃的温度; e）过滤并干燥步骤d）中获得的材料; f）任选地纯化从步骤e）获得的产物; g）分离结晶达沙替尼一水合物。

9. 发明申请

US20140336246A1 PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL 有权
标题翻译：制备无定形卡宾的方法
公开(公告)号：US20140336246A1
公开(公告)日：2014-11-13
申请号：US14349332
申请日：2012-12-26
申请人： SHILPA MEDICARE LIMITED
发明人： Vimal Kumar Shrawat , Prashant Purohit , Rafiuddin Dr , Vinod Kumar Singh , Akshaykant Chaturvedi
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , C07D413/12
摘要： The present invention provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), and process for preparation thereof.The present application also provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.
摘要翻译：本发明提供一种非溶剂化无定形形式的（2α，5α，b，10α，17α）-4-乙酸基 - 13 - （{（2R，3S）-3 [（叔丁氧基羰基）氨基] -2-羟基-3-苯基丙酰基}氧基）-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧基十二烷-1-烯-2-基苯甲酸酯或卡巴他赛（I），以及制备方法其中。本申请还提供非溶剂化无定形形式的（2α，5β，7α，b，10α，13α）-4-乙酸基 - 13 - （{（2R，3S）-3 [（叔丁氧基羰基）氨基 ] -2-羟基-3-苯基丙酰基}氧基）-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧塔塔-1-烯-2-基苯甲酸酯或具有XRPD图案的卡巴他赛（I）根据图 1和IR光谱如图1所示。并且可用作其包含其的药物组合物中的活性药物并具有抗癌活性。

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