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1. 发明申请

WO2009133468A1 IMPROVED PROCESS FOR PREPARING QUINOLINE-3-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：制备喹啉-3-羧酰胺衍生物的改进方法
公开(公告)号：WO2009133468A1
公开(公告)日：2009-11-05
申请号：PCT/IB2009/005780
申请日：2009-04-27
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , SHARMA, Krishnadatt , SHEKHAWAT, Kundan, Singh , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , SHARMA, Krishnadatt , SHEKHAWAT, Kundan, Singh , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
IPC分类号： C07D215/22
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/22
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：本文公开了以高产率和纯度制备喹啉-3-甲酰胺衍生物如拉喹莫德或其药学上可接受的盐的改进的，商业上可行的和工业上有利的方法。

2. 发明申请

WO2010023561A1 PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制备VARENICLINE，VARENICLINE中间体及其药学上可接受的药物的方法
公开(公告)号：WO2010023561A1
公开(公告)日：2010-03-04
申请号：PCT/IB2009/007081
申请日：2009-08-31
申请人： ACTAVIS GROUP PTC EHF , SHEKHAWAT, Kundan, Singh , DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra
发明人： SHEKHAWAT, Kundan, Singh , DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D471/08
CPC分类号： C07D471/08
摘要： Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting l-(4,5-diamino-10-aza-tricyclo[6.3.1.0 2 7 ]dodeca-2(7),3,5-trien- 10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the pressence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of l-(4,5-diamino-10-aza-tricyclo[6.3.1.0 2 7 ]dodeca-2(7),3,5-trien-10-yl)-2,2,2- trifluoro-ethanone.
摘要翻译：本文提供了一种改进的，方便的，商业上可行的和环境友好的制备伐伦尼克林或其药学上可接受的盐的方法，其包括使1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二碳-2 （7），3,5-三烯-10-基）-2,2,2-三氟乙酮与氯乙醛在氧源的压力下反应。本文进一步提供了一种改进的和工业上有利的制备1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二-2（7），3,5-三烯-10-基）-2,2,2-三氟 - 乙酮。

3. 发明申请

WO2010001257A2 NOVEL SOLID STATE FORMS OF LAQUINIMOD AND ITS SODIUM SALT 审中-公开
标题翻译： LAQUINIMOD及其SODIUM盐的新型固体状态
公开(公告)号：WO2010001257A2
公开(公告)日：2010-01-07
申请号：PCT/IB2009/006560
申请日：2009-06-30
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
IPC分类号： C07D215/22 , A61K31/4704 , A61P37/02
CPC分类号： C07D215/56 , A61K31/4704
摘要： Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof.
摘要翻译：本文提供了一种新的结晶形式的拉喹莫德，其制备方法，药物组合物及其处理方法。本文还提供了新的无定形和多晶型的拉喹莫德钠，制备方法，药物组合物及其处理方法。

4. 发明申请

WO2010070449A2 HIGHLY PURE LAQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：高纯度液体或其药学上可接受的盐
公开(公告)号：WO2010070449A2
公开(公告)日：2010-06-24
申请号：PCT/IB2009/007946
申请日：2009-12-15
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra
发明人： DIXIT, Girish , SHARMA, Krishnadatt , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D215/56
CPC分类号： C07D215/56
摘要： Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1- methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity.
摘要翻译：本文提供了拉喹莫德，N-乙基-N-苯基-1,2-二氢-4-羟基-1-甲基-2-氧代喹啉-3-甲酰胺（脱氯罗喹莫德杂质）的杂质及其制备和分离方法。本文进一步提供了基本上不含脱氯洛喹莫德杂质的高纯度laquinimod或其药学上可接受的盐，其制备方法，以及包含高纯度laquinimod或其药学上可接受的盐基本上不含脱氯罗喹莫德杂质的药物组合物。

5. 发明申请

WO2008107797A2 LERCANIDIPINE HYDROCHLORIDE POLYMORPHS AND AN IMPROVED PROCESS FOR PREPARATION OF 1,1,N-TRIMETHYL-N-(3,3-DIPHENYLPROPYL)-2-AMINOETHYL ACETOACETATE 审中-公开
标题翻译： LERCANIDIPINE HYDROCHLORIDE POLYMORPHS和改进的1,1,1-三甲基-N-（3,3-二苯基丙基）-2-氨基乙酸乙酯的制备方法
公开(公告)号：WO2008107797A2
公开(公告)日：2008-09-12
申请号：PCT/IB2008/000903
申请日：2008-03-05
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , SHARMA, Krishnadatt, Baldevprasad , PRADHAN, Nitin Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , SHARMA, Krishnadatt, Baldevprasad , PRADHAN, Nitin Sharadchandra , VALGEIRSSON, Jon
IPC分类号： C07C213/06 , C07C219/06 , C07D211/86 , A61K31/4422
CPC分类号： C07C219/06 , C07C213/06 , C07D213/803
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N- trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride.
摘要翻译：本文公开了改进的，商业上可行的和工业上有利的方法，用于制备基本上纯的勒卡西地平中间体1,1,1-三甲基-N-（3,3-二苯基丙基）-2-氨乙基乙酰乙酸酯。该中间体可用于以高产率和纯度制备乐卡尼地平或其药学上可接受的盐。本发明还提供了一种新的盐酸乐卡尼平的结晶形式及其制备方法。本发明还提供了制备盐酸乐卡地平的无定形形式的方法。

6. 发明申请

WO2011030224A3 PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES 审中-公开
标题翻译：帕利哌酮或药物可接受的盐，大部分不含杂质
公开(公告)号：WO2011030224A3
公开(公告)日：2011-03-17
申请号：PCT/IB2010/002568
申请日：2010-09-10
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , KHILE, Anil, Shahaji , PATEL, Jayesh, Laljibhai , PRADHAN, Nitin, Sharadchandra
发明人： DIXIT, Girish , KHILE, Anil, Shahaji , PATEL, Jayesh, Laljibhai , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D471/04 , A61K31/519 , A61P25/00
摘要： Provided herein are impurities of paliperidone, 3-[2-[4-[l-(4-fruoro-2-hydroxyphenyl) methanoyl]piperidinyl-l-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[l,2-a]pyrimidin-4- one (methanoyl impurity), 3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-l,2- benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[l,2-a]pyrimidin- 4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9- keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates.
摘要翻译：本文提供了帕潘立酮，3- [2- [4- [1-（4-呋喃-2-羟基苯基）甲酰基]哌啶基-1-基]乙基] -2-甲基 - 6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮（甲酰基杂质），3- [2- [4-（6-氟-1,2-苯并异恶唑-3 - 基）-1-哌啶基]乙基] -2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮（脱羟基杂质）和3- [2- [4-（6-氟-1,2-二氢 - 2-苯并异恶唑-3-基）-1-哌啶基]乙基] -2-甲基-7,8-二氢-6H-吡啶并[1,2-a]嘧啶-4,9-二酮（9-酮杂质），以及其制备和分离方法。本文进一步提供基本上不含甲醛酰基，脱羟基和9-酮杂质的高纯度帕潘立酮或其药学上可接受的盐，其制备方法，以及包含基本上不含甲亚酰基的高纯度帕潘立酮或其药学上可接受的盐的药物组合物，脱羟基和9-酮杂质。本文还提供了用于制备帕潘立酮中间体的改进且有效的方法。

7. 发明申请

WO2010128355A3 IMPROVED PROCESSES FOR PREPARING SUBSTANTIALLY PURE ARFORMOTEROL AND ITS INTERMEDIATES 审中-公开
标题翻译：改进的制备大量纯的ARFORMOTEROL及其中间体的方法
公开(公告)号：WO2010128355A3
公开(公告)日：2010-11-11
申请号：PCT/IB2009/008097
申请日：2009-12-28
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , GAIKWAD, Nandkumar , PRADHAN, Nitin, Sharadchandra
发明人： DIXIT, Girish , GAIKWAD, Nandkumar , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07C201/12 , C07C205/36 , C07C213/02 , C07C213/10 , C07C217/60 , C07C217/80 , C07C231/02 , C07C231/12 , C07C233/43
摘要： Provided herein are improved, convenient and industrially advantageous processes for the preparation of N-[2-hydroxy-5-[(1R)-l-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1- methylethyl] amino]ethyl]phenyl]formamide (Arformoterol) or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided further herein is an improved and industrially advantageous process for the preparation of a substantially enantiomerically pure arformoterol intermediate, (R)-4-methoxy-α-methyl-N-(phenylmethyl)benzeneethanamine.
摘要翻译：本文提供了用于制备N- [2-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2- （4-甲氧基苯基）-1-甲基乙基]氨基]乙基]苯基]甲酰胺（阿福特罗尔）或其药学上可接受的盐。本文进一步提供了用于制备基本上对映体纯的阿福特罗中间体（R）-4-甲氧基-α-甲基-N-（苯基甲基）苯乙胺的改进的和工业上有利的方法。

8. 发明申请

WO2009112954A3 PROCESSES FOR THE PREPARATION OF BOSENTAN AND RELATED COMPOUNDS 审中-公开
公开(公告)号：WO2009112954A3
公开(公告)日：2009-09-17
申请号：PCT/IB2009/005454
申请日：2009-03-12
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , GAIKWAD, Nandkumar , NAIDU, Hima, Prasad , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , GAIKWAD, Nandkumar , NAIDU, Hima, Prasad , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
IPC分类号： C07D403/04 , A61K31/606 , A61K31/513 , A61P9/00 , A61P11/00
摘要： Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of substantially pure ethylene glycol sulfonamide compounds such as bosentan.

9. 发明申请

WO2009093127A2 SUBSTANTIALLY PURE AND A STABLE CRYSTALLINE FORM OF BOSENTAN 审中-公开
标题翻译： BOSENTAN的大量纯度和稳定的结晶形式
公开(公告)号：WO2009093127A2
公开(公告)日：2009-07-30
申请号：PCT/IB2009/000108
申请日：2009-01-22
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , GAIKWAD, Nandkumar , NAIDU, Hima, Prasad , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , GAIKWAD, Nandkumar , NAIDU, Hima, Prasad , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
CPC分类号： C07D403/04
摘要： Described is a highly stable crystalline form of bosentan having a water content in the range of about 3 - 4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A 5 . Provided also herein is a bosentan impurity, p-tert-butyl-N-[6-hydroxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl] benzenesulfonamide (deshydroxyethyl bosentan impurity), and process for preparing and isolating thereof. Further provided are highly pure bosentan or a pharmaceutically acceptable salt thereof substantially free of deshydroxyethyl bosentan and bosentan dimer impurities, process for the preparation thereof, and pharmaceutical compositions comprising solid particles of highly pure bosentan or a pharmaceutically acceptable salt thereof, wherein 90 volume-percent of the particles (D 90 ) have a size of less than about 300 microns.
摘要翻译：描述了基于波生坦总重量（波生坦结晶形式A5），其制备方法和药物组合物的水含量在约3-4重量％范围内的高度稳定的结晶形式的波生坦包括波生坦晶体A5。本文还提供了一种波生坦杂质，对叔丁基-N- [6-羟基-5-（2-甲氧基苯氧基）-2-（2-嘧啶基）-4-嘧啶基]苯磺酰胺（脱羟乙基波生坦杂质）和方法用于制备和分离它们。还提供了高纯度的波生坦或其药学上可接受的盐，其基本上不含脱羟基乙基波生坦和波生坦二聚体杂质，其制备方法以及包含高纯度波生坦固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％的颗粒（D90）具有小于约300微米的尺寸。

10. 发明申请

WO2010136895A1 SOLID STATE FORMS OF PALIPERIDONE SALTS AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： PALIPERIDONE SALTS的固体状态及其制备方法
公开(公告)号：WO2010136895A1
公开(公告)日：2010-12-02
申请号：PCT/IB2010/001375
申请日：2010-05-25
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , KHILE, Anil, Shahaji , NAIR, Vignesh , PRADHAN, Nitin, Sharadchandra
发明人： DIXIT, Girish , KHILE, Anil, Shahaji , NAIR, Vignesh , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D471/04 , A61K31/517
CPC分类号： C07D471/04
摘要： Provided herein are solid state forms of paliperidone salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. Paliperidone is represented by the following structural formula (I) : More particularly, provided are solid state forms of paliperidone acid addition salts, wherein the acid counter ion is provided by an acid selected from the group consisting of L- (+) -tartaric acid, p- toluenesulfonic acid, maleic acid, oxalic acid, fumaric acid, acetic acid and malic acid. Provided also herein is a process for preparing substantially pure paliperidone free base using the solid state forms of paliperidone salts.
摘要翻译：本文提供的是利培酮盐的固态形式，制备方法，药物组合物及其处理方法。哌啶酮由以下结构式（I）表示：更具体地说，提供了帕培酮酸加成盐的固态形式，其中酸抗衡离子由选自下列的酸提供：L-（+） - 酒石酸，对甲苯磺酸，马来酸，草酸，富马酸，乙酸和苹果酸。本文还提供了使用固体形式的利培培酮盐制备基本上纯的利培酮游离碱的方法。

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