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1. 发明专利

NZ705994A Process for preparing pemetrexed di potassium and its hydrates 未知
公开(公告)号：NZ705994A
公开(公告)日：2015-08-28
申请号：NZ70599413
申请日：2013-10-16
申请人： SHILPA MEDICARE LTD , SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , DR RAFIUDDIN , SINGH VINOD KUMAR , PIPAL BHAGAT RAJ , CHATURVEDI AKSHAY KANT
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
摘要： The present invention relates to Di potassium (S)-2-(4-(2-(2-amino-4-oxo4,7,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido) pentanedioate (I) and its hydrates useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer. The present invention also relates to a process for preparation thereof.

2. 发明专利

CA2888611A1 PROCESS FOR PREPARING PEMETREXED DI POTASSIUM AND ITS HYDRATES 未知
公开(公告)号：CA2888611A1
公开(公告)日：2014-04-24
申请号：CA2888611
申请日：2013-10-16
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR , PIPAL BHAGAT RAJ , CHATURVEDI AKSHAY KANT
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
摘要： The present invention relates to Di potassium (S)-2-(4-(2-(2-amino-4-oxo4,7,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido) pentanedioate (I) and its hydrates useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer. The present invention also relates to a process for preparation thereof.

3. 发明专利

NZ630289A Crystalline erlotinib hydrochloride process 未知
公开(公告)号：NZ630289A
公开(公告)日：2016-08-26
申请号：NZ63028913
申请日：2013-08-14
申请人： SHILPA MEDICARE LTD
发明人： PUROHIT PRASHANT , CHATURVEDI AKSHAYKANT , SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR
IPC分类号： C07D239/94
摘要： The disclosure relates to a process for preparation of Crystalline Erlotinib HCl (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride) Form-SE characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2&thetas;° 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 2&thetas;°, 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. The process for preparing Erlotinib hydrochloride crystalline Form-SE comprises the steps of: (a) Combining the Erlotinib free base or salt with a mixture of ketone and alcohol solvent both having water content up to less than 0.5% w/w; (b)raise the temperature up to about 40- 70°C; (c) stir the solution at same temperature up to a time between 15 to 60 minutes; (d) combine isopropanol and HC1 mixture; (e) optionally maintain the mixture for 10-60 minutes; (f) cooling the mixture up to about 10-40°C; and (g) isolating the crystalline material.

4. 发明专利

IN1248CH2013A AMORPHOUS 2-CHLORO-N-(4-CHLORO-3-(PYRIDIN-2-YL)PHENYL)-4-(METHYLSULFONYL)BENZAMIDE 未知
公开(公告)号：IN1248CH2013A
公开(公告)日：2015-08-21
申请号：IN1248CH2013
申请日：2013-03-22
申请人： SHILPA MEDICARE LTD
发明人： RAFIUDDIN , SINGH VINOD KUMAR , KOKARE NAGNNATH , CHATURVEDI AKSHAY KANT
IPC分类号： C07D20060101
摘要： The present invention relates to amorphous form of (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide (I) or its pharmaceutically active salts, and process for preparation thereof. The invention further relates to pharmaceutical compositions comprising amorphous form of (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide having anti-cancer activity.

5. 发明专利

AU2013346322B2 Crystalline Bortezomib process 未知
公开(公告)号：AU2013346322B2
公开(公告)日：2016-11-10
申请号：AU2013346322
申请日：2013-11-12
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR , CHATURVEDI AKSHAY KANT
IPC分类号： A61K31/517 , A61K31/60 , C07F5/02 , C07F5/04
摘要： The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB (Ia) and characterized by having water content ranging between 3.5 - 6.0 %

6. 发明专利

NZ630287A Crystalline bortezomib process 未知
公开(公告)号：NZ630287A
公开(公告)日：2016-07-29
申请号：NZ63028713
申请日：2013-11-12
申请人： SHILPA MEDICARE LTD
发明人： CHATURVEDI AKSHAYKANT , SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR
IPC分类号： A61K31/517 , A61K31/60
摘要： The disclosure relates to a process for the preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB (Ia) and characterized by having water content ranging between 3.5 - 6.0 % w/w; X-ray powder diffraction pattern comprising characteristic 2&thetas;° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5and 23.6 ± 0.20 2&thetas;°, wherein peaks at 9.8 and 11.39 ± 0.20 2&thetas;° are un-split and 100 % intensity peak is present at 5.6± 0.20 2&thetas;°, 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, 1201cm-1, 1150cm-1, 1020 cm-1, 747 cm-1and 702 cm-1and Raman absorption spectra having characteristic peaks approximately at 3066 cm-1, 1583 cm-1, 1528 cm-1,1281cm-1, 1213 cm-1, 1035 cm-1, 1022cm-1and 1004 cm-1, wherein the process comprises the steps of: (a) combining the Bortezomib with an aliphatic ester solvent or a mixture of aliphatic ester solvent and water; (b) raise the temperature upto about 40- 70°C; (c) stir the solution at same temperature up to a time between 15 to 60 minutes; (d) combine with aliphatic C6 to C7 hydrocarbon solvent; (e) optionally maintain the mixture for 10-60 minutes; (f) cooling the mixture upto about 10-40°C; and (g) isolating the crystalline material. Said crystalline Form-SB of Bortezomib is used as an active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.

7. 发明专利

AU2013333497A1 Process for preparing pemetrexed di potassium and its hydrates 未知
公开(公告)号：AU2013333497A1
公开(公告)日：2015-04-02
申请号：AU2013333497
申请日：2013-10-16
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR , PIPAL BHAGAT RAJ , CHATURVEDI AKSHAY KANT
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
摘要： The present invention relates to Di potassium (S)-2-(4-(2-(2-amino-4-oxo4,7,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido) pentanedioate (I) and its hydrates useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer. The present invention also relates to a process for preparation thereof.

8. 发明专利

CA2891822A1 CRYSTALLINE BORTEZOMIB PROCESS 未知
公开(公告)号：CA2891822A1
公开(公告)日：2014-05-22
申请号：CA2891822
申请日：2013-11-12
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR , CHATURVEDI AKSHAY KANT
IPC分类号： A61K31/517 , A61K31/60 , C07F5/02 , C07F5/04
摘要： The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB (Ia) and characterized by having water content ranging between 3.5 - 6.0 % w/w; X-ray powder diffraction pattern comprising characteristic 2?° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5and 23.6 ± 0.20 2?°, wherein peaks at 9.8 and 11.39 ± 0.20 2?° are un-split and 100 % intensity peak is present at 5.6± 0.20 2?°, 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, 1201cm-1, 1150cm-1, 1020 cm-1, 747 cm-1and 702 cm-1and Raman absorption spectra having characteristic peaks approximately at 3066 cm-1, 1583 cm-1, 1528 cm-1,1281cm-1, 1213 cm-1, 1035 cm-1, 1022cm-1and 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.

9. 发明专利

AU2013346322A1 Crystalline Bortezomib process 未知
公开(公告)号：AU2013346322A1
公开(公告)日：2015-05-28
申请号：AU2013346322
申请日：2013-11-12
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN , SINGH VINOD KUMAR , CHATURVEDI AKSHAY KANT
IPC分类号： A61K31/517 , A61K31/60 , C07F5/02 , C07F5/04
摘要： The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB (Ia) and characterized by having water content ranging between 3.5 - 6.0 %

10. 发明申请

WO2014167428A3 AMORPHOUS 4-(3-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXOIMIDAZOLIDIN-1-YL)-2-FLUORO-N-METHYLBENZAMIDE 审中-公开
标题翻译：异 - 4-（3-（4-氰基-3-（三氟甲基）苯基）-5,5-二甲基-4-氧代-2-硫代咪唑啉-1-基）-2-氟-N-甲基苯甲酰胺
公开(公告)号：WO2014167428A3
公开(公告)日：2015-02-19
申请号：PCT/IB2014059443
申请日：2014-03-05
申请人： SHILPA MEDICARE LTD
发明人： RAFIUDDIN DR , SINGH VINOD KUMAR , KOKARE NAGNNATH , HIRPARA SANJAY , ADDANKI ASHOK KUMAR , RAJU POTHURAJU , CHATURVEDI AKSHAYKANT
IPC分类号： A61K31/4166 , C07D233/02
CPC分类号： C07D233/86
摘要： The present invention relates to amorphous 4-(3-(4-cyano-3-(trifluoromethyl) phenyl)- 5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide (I) (I) and process for preparation thereof. The invention further relates to a solid dispersion of 4-(3-(4-cyano-3-(trifluoromethyl) phenyl)-5, 5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide and at least one pharmaceutically acceptable carrier. The amorphous 4-(3-(4-cyano-3-(trifluoromethyl) phenyl)-5,5-dimethyl-4-oxo-2- thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide (I) and/or its solid dispersion of the present invention can be useful in the treatment of cancer.
摘要翻译：本发明涉及无定形4-（3-（4-氰基-3-（三氟甲基）苯基）-5,5-二甲基-4-氧代-2-硫代咪唑烷-1-基）-2-氟-N-甲基苯甲酰胺（I）（I）及其制备方法。本发明还涉及4-（3-（4-氰基-3-（三氟甲基）苯基）-5,5-二甲基-4-氧代-2-硫代咪唑烷-1-基）-2-氟 - N-甲基苯甲酰胺和至少一种药学上可接受的载体。无定形4-（3-（4-氰基-3-（三氟甲基）苯基）-5,5-二甲基-4-氧代-2-硫代咪唑烷-1-基）-2-氟-N-甲基苯甲酰胺（I）和 /或其本发明的固体分散体可用于治疗癌症。

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