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1. 发明申请

WO2011058521A4 PROCESS FOR THE PREPARATION OF CRYSTALLINE FORM I OF L-MALIC ACID SALT OF SUNITINIB 审中-公开
标题翻译：制备太尼丁L-肉豆蔻酸盐结晶形式I的方法
公开(公告)号：WO2011058521A4
公开(公告)日：2011-09-01
申请号：PCT/IB2010055150
申请日：2010-11-12
申请人： RANBAXY LAB LTD , SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to a process for the preparation of crystalline Form I of the L-malic acid salt of sunitinib.
摘要翻译：本发明涉及制备舒尼替尼的L-苹果酸盐的结晶形式I的方法。

2. 发明申请

WO2011058521A3 PROCESS FOR THE PREPARATION OF CRYSTALLINE FORM I OF L-MALIC ACID SALT OF SUNITINIB 审中-公开
标题翻译：制备硫酸铵的结晶形式I的方法
公开(公告)号：WO2011058521A3
公开(公告)日：2011-07-07
申请号：PCT/IB2010055150
申请日：2010-11-12
申请人： RANBAXY LAB LTD , SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to a process for the preparation of crystalline Form I of the L-malic acid salt of sunitinib.
摘要翻译：本发明涉及一种制备舒尼替尼的L-苹果酸盐的晶型I的方法。

3. 发明申请

WO2011033472A1 SALTS OF SUNITINIB 审中-公开
标题翻译： SUNITINIB的销售
公开(公告)号：WO2011033472A1
公开(公告)日：2011-03-24
申请号：PCT/IB2010054196
申请日：2010-09-16
申请人： RANBAXY LAB LTD , SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： SANWAL SUDHIR SINGH , KUMAR SARIDI MADHAVA DILEEP , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to salts of sunitinib and their preparation.
摘要翻译：本发明涉及舒尼替尼的盐及其制备方法。

4. 发明申请

WO02100323A2 METHYL ANALOGS OF SIMVASTATIN AS NOVEL HMG-CoA REDUCTASE INHIBITORS 审中-公开
标题翻译：辛伐他汀作为新型HMG-CoA还原酶抑制剂的甲基化学
公开(公告)号：WO02100323A2
公开(公告)日：2002-12-19
申请号：PCT/IB0202112
申请日：2002-06-10
申请人： RANBAXY LAB LTD , THAPER RAJESH KUMAR , KUMAR SARIDI MADHAVA DILEEP , KUMAR YATENDRA
发明人： THAPER RAJESH KUMAR , KUMAR SARIDI MADHAVA DILEEP
IPC分类号： A61K31/22 , A61K31/366 , A61P3/06 , A61P9/00 , C07C67/293 , C07C67/52 , C07C67/58 , C07C69/013 , C07C69/03 , C07C69/30 , C07D309/30 , A61K
CPC分类号： C07C69/30 , C07C2602/28 , C07D309/30
摘要： The present invention relates to a novel methyl analog of simvastatin, which has the ability to inhibit the synthesis of cholesterol. The compound of the present invention holds promise for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders. The invention also relates to a process for making the novel compound.
摘要翻译：本发明涉及辛伐他汀的新型甲基类似物，其具有抑制胆固醇合成的能力。本发明的化合物具有治疗和预防高胆固醇血症和各种心脏病的希望。本发明还涉及制备该新化合物的方法。

5. 发明申请

WO2011058525A3 PROCESSES FOR THE PREPARATION OF ERLOTINIB HYDROCHLORIDE FORM A AND ERLOTINIB HYDROCHLORIDE FORM B 审中-公开
标题翻译： ERLOTINIB氢氯酸盐形式A和ERLOTINIB氢氯化物形式B的制备方法
公开(公告)号：WO2011058525A3
公开(公告)日：2011-11-24
申请号：PCT/IB2010055155
申请日：2010-11-12
申请人： RANBAXY LAB LTD , MURUGESAN BALAGURU , VEMPALI ANANDAM , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： MURUGESAN BALAGURU , VEMPALI ANANDAM , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The present invention relates to processes for the preparation of erlotinib hydrochloride Form A and erlotinib hydrochloride Form B.(I).
摘要翻译：本发明涉及制备盐酸埃罗替尼形式A和盐酸埃洛替尼B型（I）的方法。

6. 发明申请

WO2011092663A3 SORAFENIB DIMETHYL SULPHOXIDE SOLVATE 审中-公开
标题翻译： SORAFENIB二甲基硫醚溶剂
公开(公告)号：WO2011092663A3
公开(公告)日：2011-12-29
申请号：PCT/IB2011050396
申请日：2011-01-28
申请人： RANBAXY LAB LTD , JARYAL JAGDEV SINGH , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN , ZADE SACHIN DEORAO , SINGH AJAY SHANKAR
发明人： JARYAL JAGDEV SINGH , SATHYANARAYANA SWARGAM , THAPER RAJESH KUMAR , PRASAD MOHAN , ZADE SACHIN DEORAO , SINGH AJAY SHANKAR
IPC分类号： C07D213/81 , A61K31/4412
CPC分类号： C07D213/81 , G01N30/02
摘要： The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro- 3-(trifluoromethyl)phenyl]ureido }phenoxy)-N2 -methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.
摘要翻译：本发明提供4-（4- {3- [4-氯-3-（三氟甲基）苯基]脲基}苯氧基）-N2-甲基吡啶-2-甲酰胺的二甲基亚砜溶剂合物，其制备方法，包含它的药物组合物并用于治疗癌症。本发明还提供了用于鉴定，定量和分离索拉非尼相关物质的新型HPLC方法。

7. 发明申请

WO2011058524A3 CRYSTALLINE FORMS OF BOSENTAN SALTS AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译： BOSENTAN销售的结晶形式及其制备方法
公开(公告)号：WO2011058524A3
公开(公告)日：2011-08-11
申请号：PCT/IB2010055153
申请日：2010-11-12
申请人： RANBAXY LAB LTD , SINGH RAKESH , MITTAL ANU , BISHT GOPAL SINGH , KHANNA MAHAVIR SINGH , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： SINGH RAKESH , MITTAL ANU , BISHT GOPAL SINGH , KHANNA MAHAVIR SINGH , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D403/04
CPC分类号： C07D239/69 , C07D403/04
摘要： The present invention relates to crystalline forms of bosentan salts and processes for their preparation.(FORMULA)
摘要翻译：本发明涉及波生坦盐的结晶形式及其制备方法（公式）

8. 发明申请

WO2011016016A1 PROCESSES FOR THE PREPARATION OF VARDENAFIL 审中-公开
标题翻译：植物的制备方法
公开(公告)号：WO2011016016A1
公开(公告)日：2011-02-10
申请号：PCT/IB2010053594
申请日：2010-08-09
申请人： RANBAXY LAB LTD , MITTAL ANU , KHANNA MAHAVIR SINGH , THAPER RAJESH KUMAR , PRASAD MOHAN
发明人： MITTAL ANU , KHANNA MAHAVIR SINGH , THAPER RAJESH KUMAR , PRASAD MOHAN
IPC分类号： C07D249/12 , C07D295/26 , C07D487/04
CPC分类号： C07D487/04 , C07D249/12 , C07D295/26
摘要： The present invention provides processes for the preparation of vardenafil, its pharmaceutically acceptable salts, hydrates and intermediates.
摘要翻译：本发明提供了伐地那非，其药学上可接受的盐，水合物和中间体的制备方法。

9. 发明申请

WO2009101634A3 A NOVEL PROCESS FOR THE PREPARATION OF ESZOPICLONE 审中-公开
标题翻译：一种制备ESZOPICLONE的新工艺
公开(公告)号：WO2009101634A3
公开(公告)日：2014-10-16
申请号：PCT/IN2009000097
申请日：2009-02-11
申请人： LUPIN LTD , THAPER RAJESH KUMAR , PRABHAVAT MANO J DEVILALJI , RALHAN SUMAN , SINGARE DNYANESHWAR TUKARAM , BHOSALE SMITE SHIVAJI , BHATNAGAR AKSHAT KUMAR
发明人： THAPER RAJESH KUMAR , PRABHAVAT MANO J DEVILALJI , RALHAN SUMAN , SINGARE DNYANESHWAR TUKARAM , BHOSALE SMITE SHIVAJI , BHATNAGAR AKSHAT KUMAR
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is related to a novel process for the preparation of eszopiclone (II), that comprises the following steps: (a) preparation of zopiclone (I) by reaction of 6-(5-chloropyridin-2-yl)-5-hydroxy-7-oxo- 5,6-dihydropyrrolo[3,4-b]pyrazine-5-one (5-OH-Py) (III) with chloro-carbonyl-4- methyl-piperazine (CMP) free base (IV) or its acid addition salt in the presence of diazabicylo [5.4.0]undec-7-ene (DBU) or a mixture of DBU and other bases; (b) resolution of racemic zopiclone with dibenzoyl-D-tartaric acid in suitable solvent wherein dibenzoyl-D-tartaric acid addition salt of eszopiclone is separated by the addition of a nitrile solvent; (c) optional purification of dibenzoyl-D-tartaric acid addition salt of eszopiclone by dissolution in solvent selected from alcohols, ketones or mixture thereof followed by the precipitation by adding a nitrile solvent; (d) conversion of the dibenzoyl-D-tartaric acid addition salt of eszopiclone to obtain the eszopiclone free base (II) by treating with an alkaline solution; (e) purification of eszopiclone by dissolving in nitrile solvent followed by addition of ketonic solvent. The eszopiclone (II) obtained by the process of the present invention has chiral purity greater than 99.9% and less amounts of organic volatile impurities. The present invention further provides novel crystalline form B of eszopiclone- Dibenzoyl-D-tartarate salt (V) and its preparation.
摘要翻译：本发明涉及一种制备右佐佐酮（II）的新方法，其包括以下步骤：（a）通过6-（5-氯吡啶-2-基）-5- 羟基-7-氧代-5,6-二氢吡咯并[3,4-b]吡嗪-5-酮（5-OH-Py）（III）与氯 - 羰基-4-甲基 - 哌嗪（CMP）游离碱）或其酸加成盐在二氮杂双环[5.4.0]十一碳-7-烯（DBU）或DBU和其他碱的混合物存在下反应; （b）在合适的溶剂中用二苯甲酰基-D-酒石酸拆分外消旋佐匹克隆，其中通过加入腈溶剂将依佐溴隆的二苯甲酰基-D-酒石酸加成盐分离; （c）通过溶解在选自醇，酮或其混合物的溶剂中，随后通过加入腈溶剂沉淀来任选地纯化依佐溴隆的二苯甲酰基-D-酒石酸加成盐; （d）通过用碱性溶液处理转化依佐来普酮的二苯甲酰基-D-酒石酸加成盐以获得依曲普西酮游离碱（II）; （e）通过溶解在腈溶剂中，然后加入酮溶剂来纯化佐佐匹克。通过本发明方法获得的佐佐匹克（II）具有大于99.9％的手性纯度和较少量的有机挥发性杂质。本发明还提供了佐佐匹克 - 二苯甲酰基-D-酒石酸盐（V）的新型结晶形式B及其制备方法。

10. 发明申请

WO2005076749A3 A NOVEL PROCESS FOR THE PREPARATION OF 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE 审中-公开
标题翻译：制备1-苄基-4 - [（5,6-二甲氧基-1-吲哚-2-基）甲基]哌嗪的新工艺
公开(公告)号：WO2005076749A3
公开(公告)日：2006-06-08
申请号：PCT/IN2005000044
申请日：2005-02-11
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
发明人： DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
IPC分类号： C07D211/02 , C07D211/32 , C07D211/70
CPC分类号： C07D211/02 , C07D211/32 , C07D211/70
摘要： Disclosed herein is the novel process for producing 1-benzyl-4-(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (donepezil) of formula [I] by treating novel starting compound 1,2,3,6-tetrahydropyridine derivative of formula [V] with 5,6-dimethoxy-1-indanone of formula [IV] to obtain an intermediate 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]-1,2,3,6-tetrahydro pyridine of formula [II] and reducing the same to produce 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine of formula [I]. The invention further comprising the process for preparation of the novel compound of formula [V].
摘要翻译：本文公开了通过处理新的起始化合物1,2,3（1）的新型制备式[I]的1-苄基-4-（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶（多奈哌齐）式[Ⅴ]的6-四氢吡啶衍生物与式[Ⅳ]的5,6-二甲氧基-1-二氢茚酮得到中间体1-苄基-4 - [（5,6-二甲氧基-1-茚满酮基）甲基 ] -1,2,3,6-四氢吡啶并将其还原，得到式（I）的1-苄基-4 - [（5,6-二甲氧基-1-茚满-2-基）甲基]哌啶 [一世]。本发明还包括制备式[Ⅴ]新化合物的方法。

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