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1. 发明授权

US09217001B2 Crystalline bortezomib process 有权
标题翻译：结晶硼替佐米方法
公开(公告)号：US09217001B2
公开(公告)日：2015-12-22
申请号：US14434105
申请日：2013-11-12
申请人： Vimal Kumar Shrawat , Rafiuddin , Vinod Kumar Singh , Akshay Kant Chaturvedi
发明人： Vimal Kumar Shrawat , Rafiuddin , Vinod Kumar Singh , Akshay Kant Chaturvedi
IPC分类号： C07D241/12 , C07F5/02 , C07F5/04
CPC分类号： C07F5/025 , C07B2200/13 , C07D241/12
摘要： The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2θ° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±0.20 2θ°, wherein peaks at 9.8 and 11.39±0.20 2θ° are un-split and 100% intensity peak is present at 5.6±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 45 to 60° C. (Peak-1) and 175 to 185° C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm−1, 3304 cm−1, 2953 cm−1, 2927 cm−1, 2868 cm−1, 1627 cm−1, 1455 cm−1, 1400 cm−1, 1201 cm−1, 1150 cm−1, 1020 cm−1, 747 cm−1 and 702 cm−1 and Raman absorption spectra having characteristic peaks approximately at 3066 cm−1, 1583 cm−1, 1528 cm−1, 1281 cm−1, 1213 cm−1, 1035 cm−1, 1022 cm−1 and 1004 cm−1. The invention also provides the use of said crystalline Form-SB as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.
摘要翻译：本发明提供制备作为其一水合物的结晶硼替佐米（Ia）的方法，其被称为结晶形式-SB，其特征在于含水量在3.5-6.0％w / w之间; X射线粉末衍射图包含特征2＆amp; t s;峰值选自5.6,7.5,9.8,10.2,11.3,15.1,18.0,20.5,21.5和23.6±0.20 2的色度;°，其中9.8和11.39的峰 ±0.20 2＆amp; thetas;°是未分裂的，并且在5.6±0.20 2时存在100％强度峰值;°，DSC等温线包含在45至60℃（峰-1）和175至185℃之间的吸热峰。（峰-2）和IR吸收特征峰值大约在3387cm -1，3304cm -1，2953cm -1，2927cm -1，2868cm -1，1627cm -1，1455cm -1，1400cm -1，具有大约在3066cm-1,1583cm-1,1528cm -1的特征峰的拉曼吸收光谱的1,1201cm -1，1150cm -1，1020cm -1，747cm -1和702cm -1， 1281cm-1,1213cm-1,1035cm -1，1022cm -1和1004cm -1。本发明还提供所述结晶形式-SB作为药物组合物中的活性药物成分用于治疗癌症的用途。

2. 发明授权

US09278932B1 Process for preparation of 2-chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide solid forms 有权
标题翻译：制备2-氯-N-（4-氯-3-吡啶-2-基苯基）-4-甲基磺酰基苯甲酰胺固体形式的方法
公开(公告)号：US09278932B1
公开(公告)日：2016-03-08
申请号：US14773322
申请日：2014-03-05
申请人： Rafiuddin Dr , Vinod Kumar Singh , Nagnnath Kokare , Akshaykant Chaturvedi
发明人： Rafiuddin Dr , Vinod Kumar Singh , Nagnnath Kokare , Akshaykant Chaturvedi
IPC分类号： C07D213/38 , C07D213/40 , C07F5/04
CPC分类号： C07D213/40 , C07D213/38 , C07F5/04
摘要： The present invention relates to crystalline 2-Chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide (I) designated as Form-SV and process for preparation thereof. The invention further relates to pharmaceutical compositions comprising crystalline Form-SV or non-crystalline form of (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide, useful in the treatment of cancer.
摘要翻译：本发明涉及名为Form-SV的结晶2-氯-N-（4-氯-3-吡啶-2-基苯基）-4-甲基磺酰基苯甲酰胺（I）及其制备方法。本发明还涉及包含结晶形式SV或非结晶形式的（2-氯-N-（4-氯-3-（吡啶-2-基）苯基）-4-（甲基磺酰基）苯甲酰胺的药用组合物，其可用在治疗癌症。

3. 发明申请

WO2012042532A1 PROCESS FOR PREPARING BICALUTAMIDE 审中-公开
标题翻译：制备贝伐菌胺的方法
公开(公告)号：WO2012042532A1
公开(公告)日：2012-04-05
申请号：PCT/IN2011000584
申请日：2011-08-29
申请人： SHILPA MEDICARE LTD , SHRAWAT VIMAL KUMAR , PUROHIT PRASHANT , RAFIUDDIN , RAO KARRI PAPA
发明人： SHRAWAT VIMAL KUMAR , PUROHIT PRASHANT , RAFIUDDIN , RAO KARRI PAPA
IPC分类号： C07C317/32 , C07C315/02
CPC分类号： C07C253/30 , C07C253/34 , C07C315/02 , C07C317/46
摘要： Processes for the preparation of N-[4-cyano-3-(trifluoro methyl) phenyl]-3-[(4-fluorophenyl) sulphonyl]-2-hydroxy-2- methyl propanamide or Bicalutamide are provided. A method for purifying the Bicalutamide using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D, and the crystalline form of Bicalutamide are also disclosed.
摘要翻译：提供了制备N- [4-氰基-3-（三氟甲基）苯基] -3 - [（4-氟苯基）磺酰基] -2-羟基-2-甲基丙酰胺或比卡鲁胺的方法。还公开了使用乙酸乙酯溶剂纯化比卡鲁胺的方法，其产生产物，基本上不含工艺相关杂质A，B，C和D，以及比卡鲁胺的结晶形式。

4. 发明申请

WO2012042532A4 PROCESS FOR PREPARING BICALUTAMIDE 审中-公开
公开(公告)号：WO2012042532A4
公开(公告)日：2012-04-05
申请号：PCT/IN2011/000584
申请日：2011-08-29
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal, Kumar , PUROHIT, Prashant , RAFIUDDIN , RAO, Karri, Papa
发明人： SHRAWAT, Vimal, Kumar , PUROHIT, Prashant , RAFIUDDIN , RAO, Karri, Papa
IPC分类号： C07C317/32 , C07C315/02
摘要： Processes for the preparation of N-[4-cyano-3-(trifluoro methyl) phenyl]-3-[(4-fluorophenyl) sulphonyl]-2-hydroxy-2- methyl propanamide or Bicalutamide are provided. A method for purifying the Bicalutamide using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D, and the crystalline form of Bicalutamide are also disclosed.

5. 发明专利

IN3103MU2015A PREPARATION AND CHARACTERIZATION OF QUERCETIN DERIVATIVES QUERCETIN THIOSEMICARBAZONES HAVING HIGH SUNSCREEN PROTECTION AND ANTICANCER ACTIVITY 未知
公开(公告)号：IN3103MU2015A
公开(公告)日：2015-10-16
申请号：IN3103MU2015
申请日：2015-08-16
申请人： ABDUL WAJID ABDUL RAFIQUE , DEVIDAS TOTARAM MAHAJAN , QUAZI SYED AZHARUDDIN QUAZI SYED RAFIUDDIN
发明人： ABDUL WAJID ABDUL RAFIQUE , DEVIDAS TOTARAM MAHAJAN , QUAZI SYED AZHARUDDIN QUAZI SYED RAFIUDDIN
IPC分类号： A61K31/00 , A61K8/00
摘要： The present invention relates to a process for the preparation and characterization of new Quercetin derivatives Quercetinthiosem carbazones based sunscreen cream having high sunscreen protection and anticancer activity. Following invention is described in detail with the help of Figure 1 of sheet 1 shows the diagram for a Thin Layer Chromatography results where the mobile phase used are Toluene: Ethyl acetate: Formic Acid 6:2:0.8 (v/v/v), Figure 2 of sheet 1 shows the diagram for FTIR graph for the Quercetin, Figure 3 of sheet 2 shows the diagram for FTIR graph for the Quercetin and Figure 4 of the sheet 2 shows the diagram for FTIR graph for the Quercetin Thiosemicarbazone derivative.

6. 发明申请

US20220127231A1 PROCESS FOR THE PREPARTION OF AMIFAMPRIDINE PHOSPHATE 有权
公开(公告)号：US20220127231A1
公开(公告)日：2022-04-28
申请号：US17474087
申请日：2021-09-14
申请人： RAFIUDDIN Dr , YUVATEJA BOYINA
发明人： RAFIUDDIN Dr , YUVATEJA BOYINA
IPC分类号： C07D213/73
摘要： The present invention relates to an improved process for the preparation of substantially pure Amifampridine phosphate The present invention further relates to a substantially pure Amifampridine Phosphate, useful for the preparation of pharmaceutical composition thereof.

7. 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。

8. 发明专利

IN1692DE2015A A PRESSURE COOKER BASED GENERATION OF ELECTRICAL ENERGY 未知
公开(公告)号：IN1692DE2015A
公开(公告)日：2015-07-17
申请号：IN1692DE2015
申请日：2015-06-08
申请人： NIDAL RAFIUDDIN
发明人： NIDAL RAFIUDDIN
IPC分类号： H02N11/00
摘要： The present invention relates to the generation of electrical energy on small scale using a pressure cooker. The pressure cooker is used as a boiler to produce steam. This steam evacuated through vent tube with an orifice when expanded through turbine coupled with one or many dc generators produces electrical energy which is used to supply load or charge batteries.

9. 发明申请

WO2013111157A1 PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL 审中-公开
标题翻译：制备无定形卡宾的方法
公开(公告)号：WO2013111157A1
公开(公告)日：2013-08-01
申请号：PCT/IN2012/000855
申请日：2012-12-26
申请人： SHILPA MEDICARE LIMITED , SHRAWAT, Vimal Kumar , PUROHIT, Prashant , RAFIUDDIN, . , SINGH, Vinod Kumar , CHATURVEDI, Akshay Kant
发明人： SHRAWAT, Vimal Kumar , PUROHIT, Prashant , RAFIUDDIN, . , SINGH, Vinod Kumar , CHATURVEDI, Akshay Kant
IPC分类号： C07D305/14 , A61K31/337
CPC分类号： C07D305/14 , C07D413/12
摘要： The present invention provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-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), (I) and process for preparation thereof. The present application also provides a non-solvated amorphous form of (2?,5?,7?,10?,13?)-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，7α，10β，13β）-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-环氧塔纳-1-烯-2-基苯甲酸酯或卡巴他赛（I），（I ）及其制备方法。本申请还提供了非溶剂化的（2α，5α，7α，10β，13β）-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），其具有根据图1的XRPD图案和根据图3的IR光谱，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。

10. 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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