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1. 发明申请

WO2009013633A4 AMORPHOUS COPRECIPITATES OF ATORVASTATIN PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
公开(公告)号：WO2009013633A4
公开(公告)日：2009-01-29
申请号：PCT/IB2008/002808
申请日：2008-07-21
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
IPC分类号： A61K9/14 , A61K9/16 , A61K31/40 , A61P3/06
摘要： The present invention relates to stable amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts with pharmaceutically acceptable excipients, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts of the present invention have improved physiochemical characteristics that assist in the effective bioavailability

2. 发明申请

WO2009007856A2 NOVEL POLYMORPH OF ATORVASTATIN CALCIUM AND USE THEREOF FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译：阿托伐他汀钙的新型多晶型及其用于制备非晶态阿托伐他汀钙的应用
公开(公告)号：WO2009007856A2
公开(公告)日：2009-01-15
申请号：PCT/IB2008/002624
申请日：2008-07-11
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
CPC分类号： C07D207/34
摘要： The present invention provides a novel polymorphic form of atorvastatin calcium, designated as form Al, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a process for the preparation of highly pure amorphous atorvastatin calcium using the novel atorvastatin calcium form Al. The present invention also relates to novel amorphous form of atorvastatin tert-butyl ester, chemically known as [R-(R*,R*)]-2-(4-fluorophenyl)- [β],[δ]-dihydroxy-5-(l-methylethyl)-3-phenyl-4-(phenylcarbamoyl)-lH-pyrrole-l- heptanoicacid tert-butyl ester, process for the preparation, and its application for preparing highly pure atorvastatin and its pharmaceutically acceptable salts thereof. The present invention also relates to use of the novel amorphous atorvastatin tert-butyl ester and novel atorvastatin calcium form al for preparing amorphous atorvastatin calcium.
摘要翻译：本发明提供了阿托伐他汀钙的新型多晶型形式，称为形式A1，制备方法，药物组合物及其治疗方法。本发明进一步提供了使用新的阿托伐他汀钙形式Al制备高纯度无定形阿托伐他汀钙的方法。本发明还涉及化学上已知为[R-（R *，R *）] - 2-（4-氟苯基） - [β]，[δ] - 二羟基-5 - （1-甲基乙基）-3-苯基-4-（苯基氨基甲酰基）-1H-吡咯-1-庚酸叔丁酯，其制备方法及其制备高纯度阿托伐他汀及其药学上可接受的盐的应用。本发明还涉及新型无定形阿托伐他汀叔丁酯和新型阿托伐他汀钙形式的用于制备无定形阿托伐他汀钙的用途。

3. 发明申请

WO2009004480A2 QUETIAPINE SALTS AND THEIR POLYMORPHS 审中-公开
标题翻译： QUETIAPINE SALTS及其POLYMORPHS
公开(公告)号：WO2009004480A2
公开(公告)日：2009-01-08
申请号：PCT/IB2008/002341
申请日：2008-05-07
申请人： ACTAVIS GROUP PTC EHF , DIXIT, Girish , KHILE, Anil, Shahaji , PATEL, Jayesh, Laljibhai , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： DIXIT, Girish , KHILE, Anil, Shahaji , PATEL, Jayesh, Laljibhai , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
CPC分类号： C07D281/14
摘要： The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate.
摘要翻译：本发明涉及喹硫平的新颖稳定的盐形式，制备方法，药物组合物及其处理方法。更具体地说，本发明提供了喹硫平的新型酸加成盐，其中酸抗衡离子由选自苯磺酸，二苯甲酰基-L-（+） - 酒石酸和二对甲苯酰基 - L - （+） - 酒石酸。本发明还提供了选自喹硫平氢溴酸盐，硫酸喹硫平，硝酸喹硫平和柠檬酸喹硫平的新型多晶型盐酸喹硫平盐。

4. 发明申请

WO2009024863A2 PROCESS FOR THE PREPARATION OF MODAFINIL ENANTIOMERS 审中-公开
标题翻译：制备莫达非尼对映体的方法
公开(公告)号：WO2009024863A2
公开(公告)日：2009-02-26
申请号：PCT/IB2008/002634
申请日：2008-06-26
申请人： ACTAVIS GROUP PTC EHF , GIRISH, Dixit , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
发明人： GIRISH, Dixit , KHILE, Anil, Shahaji , PRADHAN, Nitin, Sharadchandra , VALGEIRSSON, Jon
IPC分类号： C07C315/02 , C07C315/04 , C07C317/44
CPC分类号： C07C315/02 , C07B2200/07 , C07C315/04 , C07C317/44
摘要： Disclosed herein is a convenient, commercially viable and environmentally friendly process for the preparation of Armodafinil. The present invention also provides an improved, commercially viable and industrially advantageous process for the preparation of pure 2-[(diphenylmethyl) sulfinyl] acetic acid (also known as modafinic acid) substantially free of sulfone impurity i.e., 2-[(diphenylmethyl)sulfonyl] acetic acid. The intermediate is useful for preparing Modafmil and its enantiomers, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：这里公开的是用于制备阿莫达非尼的方便的，商业上可行的和环境友好的方法。本发明还提供了用于制备基本上不含砜杂质的纯2 - [（二苯基甲基）亚磺酰基]乙酸（也称作莫达芬尼酸）的改进的，商业上可行的和工业上有利的方法，即2 - [（二苯基甲基）磺酰基 ]乙酸。该中间体可用于高产率和高纯度地制备莫达非尔及其对映异构体或其药学上可接受的盐。

5. 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。

6. 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。

7. 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.

8. 发明申请

WO2009047637A1 NOVEL POLYMORPHS OF BOSENTAN 审中-公开
标题翻译：博斯坦的新概念
公开(公告)号：WO2009047637A1
公开(公告)日：2009-04-16
申请号：PCT/IB2008/003262
申请日：2008-10-13
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 , A61P9/00 , A61K31/506
CPC分类号： C07D403/04
摘要： Disclosed herein are novel polymorphic forms of bosentan, processes for preparation, pharmaceutical compositions, and method of treating thereof.
摘要翻译：本文公开了波生坦的新型多晶型物，制备方法，药物组合物及其治疗方法。

9. 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。

10. 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。

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