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1. 发明申请

WO2012059935A9 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：WO2012059935A9
公开(公告)日：2012-06-14
申请号：PCT/IN2011000585
申请日：2011-08-29
申请人： SHILPA MEDICARE LTD , SHRAWAT VIMAL KUMAR , PUROHIT PRASHANT , SINGH VINOD KUMAR , UNNAM SESHACHALAM
发明人： SHRAWAT VIMAL KUMAR , PUROHIT PRASHANT , SINGH VINOD KUMAR , UNNAM SESHACHALAM
IPC分类号： C07D235/16 , A61K31/4184 , A61P35/00
CPC分类号： C07D235/16 , A61K31/4184 , C07B2200/13 , C07C209/10
摘要： A process for preparing Bendamustine hydrochloride monohydrate is provided. A process for purifying said monohydrate to get substantially purne Bendamustine hydrochloride monohydrate crystalline form is also provided.
摘要翻译：提供了一种制备盐酸苯达莫司汀一水合物的方法。还提供了一种用于纯化所述一水合物以获得基本上沸腾的盐酸苯达司汀一水合物结晶形式的方法。

2. 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。

3. 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.

4. 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.

5. 发明专利

NZ630290A Process for preparation of fingolimod and its salts 未知
公开(公告)号：NZ630290A
公开(公告)日：2016-09-30
申请号：NZ63029014
申请日：2014-01-11
申请人： SHILPA MEDICARE LTD
发明人： SHRAWAT VIMAL KUMAR , RAFIUDDIN DR , CHATURVEDI AKSHAYKANT
IPC分类号： C07C209/50 , C07C211/17 , C07C215/28
摘要： Disclosed is a process for the preparation of Fingolimod hydrochloride (I) comprising: a) reacting 2-acetamido-1,3-diacetoxy-2-(2-phenylethyl)propane with octanoyl chloride in presence of a Friedel-Craft’s catalyst (such a lewis acid selected from FeCl3, AlCl3, TiCl4, ZnCl2 or BF3) and a halohydrocarbon organic solvent (such as dichloromethane, dichloroethane or chloroform) under inert atmosphere at room temperature to form 2-acetamido-2-(4-octanoylphenethyl)propane-1,3-diyl diacetate; b) hydrogenating 2-acetamido-2-(4-octanoylphenethyl)propane-1,3-diyl diacetate with 10% Pd/C at temperature ranging between 20 and -35°C in presence of ethanol and acetic acid, wherein the ratio of ethanol to acetic acid is in the ratio of 8:2 to get 2-acetamido-2-(4-octylphenethyl)propane-1,3-diyl diacetate; c) optionally recrystallizing the product obtained in step b) with a hydrocarbon solvent (such as n-hexane, n-heptane) or an alcoholic solvent (such as methanol and/or ethanol) or both, to get purified 2-acetamido-2-(4-octyl phenethyl)propane-1,3-diyl diacetate; d) treating 2-acetamido-2-(4-octylphenethyl)propane-1,3-diyl diacetate in the presence of organic solvents selected from C1-C4 alcohol (such as methanol, ethanol or isopropanol) and a base (such as an alkali metal hydroxide selected from LiOH, NaOH or KOH) to get Fingolimod free base; and e) converting Fingolimod free base into Fingolimod hydrochloride (I) in an organic solvent and 5 to 15% w/w IPA- HCl solution at pH ranging between 1.00 to 3.00, wherein Fingolimod hydrochloride may be further provided in crystalline form ß being characterized by X-ray powder diffraction pattern having, characteristic 2&thetas;° peaks in XRPD peak set of 3.54, 7.10, 10.67, 15.36, 17.83, 20.53, 21.49, 23.29, 25.12, 26.68 and 29.22 ± 0.1 2&thetas;°.

6. 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.

7. 发明公开

EP3166931A4 AN IMPROVED PROCESS FOR THE PREPARATION OF ENZALUTAMIDE 审中-公开
公开(公告)号：EP3166931A4
公开(公告)日：2018-05-09
申请号：EP15819144
申请日：2015-07-06
申请人： SHILPA MEDICARE LTD
发明人： HIRPARA SANJAY , SHRAWAT VIMAL KUMAR , POTHURAJU RAJU , TRIPATHI CHANDRESH KUMAR , AKSHAYKANT CHATURVEDI
IPC分类号： C07D233/86
CPC分类号： C07D233/86 , C07B2200/13
摘要： The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.

8. 发明公开

EP2697211A4 PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE 审中-公开
标题翻译：于制备多烯紫杉醇及其水合物中
公开(公告)号：EP2697211A4
公开(公告)日：2014-08-13
申请号：EP11862252
申请日：2011-08-29
申请人： SHILPA MEDICARE LTD
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

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 %

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