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11. 发明申请

WO2009093127A3 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：WO2009093127A3
公开(公告)日：2010-07-22
申请号：PCT/IB2009000108
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
IPC分类号： C07D403/04 , A61K31/506 , A61P11/00
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 A5. 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 (D90) 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。

12. 发明申请

WO2009004485A3 REPAGLINIDE SUBSTANTIALLY FREE OF DIMER IMPURITY 审中-公开
标题翻译： REPAGLINIDE基本上不含二聚氰胺
公开(公告)号：WO2009004485A3
公开(公告)日：2009-03-19
申请号：PCT/IB2008002548
申请日：2008-06-05
申请人： ACTAVIS GROUP PTC EHF , SEBASTIAN SONNY , BALLA SASIDHAR VENKATA , KATIKAREDDY RAMAMURTHY , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： SEBASTIAN SONNY , BALLA SASIDHAR VENKATA , KATIKAREDDY RAMAMURTHY , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2- ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1- piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume- percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2- piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.
摘要翻译：本发明提供了基本上不含二聚体杂质的高纯度瑞格列奈及其制备方法。本发明还涉及2-乙氧基-N - [（1S）-3-甲基-1- [2-（1-哌啶基）苯基]丁基] -4- [2 - [[（1S）-3-甲基 -1- [2-（1-哌啶基）苯基]丁基]氨基] -2-氧代乙基]苯甲酰胺，瑞格列奈的杂质及其制备和分离方法。本发明还涉及包含基本上不含二聚体杂质的纯瑞格列奈的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400微米的尺寸。本发明还提供外消旋3-甲基-1-（2-哌啶子基 - 苯基）-1-丁胺的光学拆分方法及其在制备瑞格列奈中的应用。

13. 发明申请

WO2009130604A3 SOLID STATE FORMS OF DEFERASIROX SALTS AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： DEFERASIROX SALTS的固体状态及其制备方法
公开(公告)号：WO2009130604A3
公开(公告)日：2009-12-30
申请号：PCT/IB2009005783
申请日：2009-04-20
申请人： ACTAVIS GROUP PTC EHF , NEELA PRAVEEN KUMAR , CHARUGUNDLA KISHORE , PATIL RAJENDRA SURYABHAN , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： NEELA PRAVEEN KUMAR , CHARUGUNDLA KISHORE , PATIL RAJENDRA SURYABHAN , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07D249/08 , A61K31/4196 , A61P39/04
CPC分类号： C07D249/08
摘要： Provided herein are novel solid state forms of deferasirox salts, process for the preparation, pharmaceutical compositions, and method of treating thereof. The solid state forms of deferasirox salts are useful for preparing deferasirox (I) in high purity.
摘要翻译：本文提供了新型固体形式的去伏他西酮盐，制备方法，药物组合物及其治疗方法。去伏他西酮盐的固态形式可用于制备高纯度的去甲草酮（I）。

14. 发明申请

WO2009053840A3 SOLID FORMS OF (±)-O-DESMETHYLVENLAFAXINE SALTS 审中-公开
标题翻译：（±）-O-DESMETHYLVENLAFAXINE盐的固体形式
公开(公告)号：WO2009053840A3
公开(公告)日：2009-06-25
申请号：PCT/IB2008003308
申请日：2008-10-21
申请人： ACTAVIS GROUP PTC EHF , SEBASTIAN SONNY , PATTABHI RAMAN BUDDHAVARAPU , CHALLA KRISHNA , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： SEBASTIAN SONNY , PATTABHI RAMAN BUDDHAVARAPU , CHALLA KRISHNA , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07C215/64 , A61K31/137
CPC分类号： C07C215/64 , C07B2200/13 , C07C55/07 , C07C59/08 , C07C63/08 , C07C215/66 , C07C2601/14
摘要： The present invention relates to solid forms of (±)-O-desmethylvenlafaxine salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides solid forms of acid addition salts of (±)- O-desmethylvenlafaxine wherein the acid counter ion is provided by an acid selected from the group consisting of oxalic acid, benzoic acid and lactic acid.
摘要翻译：本发明涉及（±）-O-去甲基文拉法辛盐的固体形式，制备方法，药物组合物及其治疗方法。更具体地说，本发明提供了（±）-O-去甲基文拉法辛的酸加成盐的固体形式，其中酸抗衡离子由选自草酸，苯甲酸和乳酸的酸提供。

15. 发明申请

WO2009077858A3 HEMIOXALATE SALT OF ELETRIPTAN 审中-公开
标题翻译：乙酸盐盐酸盐
公开(公告)号：WO2009077858A3
公开(公告)日：2011-03-31
申请号：PCT/IB2008003721
申请日：2008-12-17
申请人： ACTAVIS GROUP PTC EHF , KUSUMBA VIJAYA GOPAL , SANKINENI SAMPATH KUMAR , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： KUSUMBA VIJAYA GOPAL , SANKINENI SAMPATH KUMAR , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07D403/06 , A61K31/404 , A61P25/00
CPC分类号： C07D403/06
摘要： The present invention relates to novel hemioxalate salt of eletriptan, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention relates to solid forms of eletriptan hemioxalate, processes for preparation, pharmaceutical compositions, and method of treating thereof. The solid form of eletriptan hemioxalate is useful for preparing eletriptan free base or a pharmaceutically acceptable salt thereof, particularly eletriptan hydrobromide, in high purity. The present invention also provides a process for preparing substantially pure eletriptan hydrobromide using eletriptan hemioxalate.
摘要翻译：本发明涉及新型的替比曲坦半盐酸盐，制备方法，药物组合物及其治疗方法。本发明涉及依托曲坦半胱氨酸盐的固体形式，制备方法，药物组合物及其处理方法。依托曲坦半胱氨酸盐的固体形式可用于以高纯度制备伊曲坦游离碱或其药学上可接受的盐，特别是依托曲坦氢溴酸盐。本发明还提供了使用依他曲坦半胱氨酸盐制备基本上纯的依托曲坦氢溴酸盐的方法。

16. 发明申请

WO2008152518A2 PROCESS FOR THE PREPARATION OF RISEDRONATE SODIUM 审中-公开
标题翻译：制备雷公藤酸钠的方法
公开(公告)号：WO2008152518A2
公开(公告)日：2008-12-18
申请号：PCT/IB2008002391
申请日：2008-05-16
申请人： ACTAVIS GROUP PTC EHF , KUMAR NEELA PRAVEEN , SINGARE DNYANESHWAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： KUMAR NEELA PRAVEEN , SINGARE DNYANESHWAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
CPC分类号： C07F9/582
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of risedronic acid or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：本文公开了一种用于以高产率和纯度制备利塞膦酸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。

17. 发明申请

WO2009122301A3 RASAGILINE MESYLATE PARTICLES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： RASAGILINE MESYLATE颗粒及其制备方法
公开(公告)号：WO2009122301A3
公开(公告)日：2009-11-26
申请号：PCT/IB2009005643
申请日：2009-03-31
申请人： ACTAVIS GROUP PTC EHF , PATIL NILESH SUDHIR , PAGIRE HAUSHABHAU SHIVAJI , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： PATIL NILESH SUDHIR , PAGIRE HAUSHABHAU SHIVAJI , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07C211/42 , A61K9/14 , A61K31/205 , A61P25/16
CPC分类号： C07C211/42 , A61K9/14 , A61K9/1688 , A61K31/205 , C07C2602/08 , Y10T428/2982
摘要： Provided herein is rasagiline mesylate having a 90 volume-percent of the particles (D90) with a size of about 600 microns to about 1500 microns, and a process for the preparation thereof. Provided also herein are pharmaceutical compositions comprising rasagiline mesylate particles having a particle size which is suitable for homogeneous distribution of the drug substance in a tablet blend, in particular 90 volume-percent of the particles (D90) have a size of about 255 microns to about 1500 microns, and a process the preparation thereof.
摘要翻译：本文提供了具有90体积％的具有约600微米至约1500微米尺寸的颗粒（D90）的甲磺酸雷沙吉兰及其制备方法。本文还提供包含具有适于药物物质在片剂混合物中均匀分布的粒度的雷沙吉兰甲磺酸盐颗粒的药物组合物，特别是90体积％的颗粒（D90）具有约255微米至约 1500微米，以及其制备方法。

18. 发明申请

WO2009037569A3 AN IMPROVED PROCESS FOR THE PREPARATION OF FESOTERODINE 审中-公开
标题翻译：改进法西酯的制备方法
公开(公告)号：WO2009037569A3
公开(公告)日：2009-07-16
申请号：PCT/IB2008003098
申请日：2008-09-22
申请人： ACTAVIS GROUP PTC EHF , CHARUGUNDLA KISHORE , KUMAR UDHAYA , PATIL RAJENDRA SURYABHAN , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： CHARUGUNDLA KISHORE , KUMAR UDHAYA , PATIL RAJENDRA SURYABHAN , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07C209/16 , C07C43/235 , C07C209/88 , C07C219/28 , C07D311/08
CPC分类号： C07D311/08 , C07B2200/07 , C07C41/26 , C07C213/00 , C07C213/02 , C07C213/10 , C07C227/18 , C07C303/28 , C07C309/73 , C07C229/38 , C07C215/54 , C07C217/62 , C07C43/23
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Fesoterodine or a pharmaceutically acceptable salt thereof in high yield and purity. Disclosed also herein is an improved and industrially advantageous optical resolution method of racemic (±)-N,N-Diisopropyl-3-(2-benzyloxy- 5-bromophenyl)-3-phenylpropylamine and use thereof for the preparation of Fesoterodine.
摘要翻译：本文公开了一种改进的，商业上可行的和工业上有利的方法，其以高产率和纯度制备西索酸或其药学上可接受的盐。本文还公开了外消旋（±）-N，N-二异丙基-3-（2-苄氧基-5-溴苯基）-3-苯基丙胺的改进和工业上有利的光学拆分方法及其用于制备非索特罗定的方法。

19. 发明申请

WO2009007853A2 NOVEL POLYMORPHS OF DARIFENACIN FREE BASE AND ITS HYDROBROMIDE SALT 审中-公开
标题翻译： DARIFENACIN FREE BASE及其盐酸盐的新型多聚体
公开(公告)号：WO2009007853A2
公开(公告)日：2009-01-15
申请号：PCT/IB2008002571
申请日：2008-06-09
申请人： ACTAVIS GROUP PTC EHF , KODALI ESWARA RAO , MEDIKONDURI SREEKANTH , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： KODALI ESWARA RAO , MEDIKONDURI SREEKANTH , NEELA PRAVEEN KUMAR , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
CPC分类号： C07D405/06
摘要： The present invention provides a novel and stable amorphous form of darifenacin free base, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a novel and stable polymorphic form of darifenacin hydrobromide, process for preparation, pharmaceutical compositions, and method of treating thereof.
摘要翻译：本发明提供了一种新颖稳定的无限形式的达赖芬酸游离碱，其制备方法，药物组合物及其治疗方法。本发明进一步提供了一种新颖稳定的多卡因多巴胺氢溴酸盐，其制备方法，药物组合物及其治疗方法。

20. 发明申请

WO2008107799A3 IMPROVED PROCESS FOR PREPARING IRBESARTAN 审中-公开
标题翻译：改进IRBESARTAN的方法
公开(公告)号：WO2008107799A3
公开(公告)日：2008-11-06
申请号：PCT/IB2008000973
申请日：2008-03-06
申请人： ACTAVIS GROUP PTC EHF , NEELA PRAVEEN KUMAR , KUMAR UDHAYA , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
发明人： NEELA PRAVEEN KUMAR , KUMAR UDHAYA , PRADHAN NITIN SHARADCHANDRA , VALGEIRSSON JON
IPC分类号： C07D403/10
CPC分类号： C07D403/10
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Irbesartan, or a pharmaceutically acceptable salt thereof, in high yield and purity, which comprises: a) reacting 2-n-butyl-3-[[2'-cyanobiphenyl-4-yI]methyI]- 1,3-diazaspiro-[4.4]non-1 - en-4-one with an alkali metal azide and tri(C 1-4 )alkylamine hydrohalide in the presence of a phase transfer catalyst in a non-polar aprotic solvent to produce an alkaline salt of 2-n-butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3- diazasp?ro[4.4]non-1 -en-4-one; and b) neutralizing the alkaline salt of 2-n-butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4- yl]methyl]-1,3-diazaspiro[4.4]n on-1-en-4-one in aqueous medium with an acid to produce Irbesartan and optionally converting the Irbesartan obtained into its pharmaceutically acceptable salts thereof.
摘要翻译：本文公开了一种用于以高产率和纯度制备厄贝沙坦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，其包括：a）使2-正丁基-3 - [[2'- 氰基联苯-4-基]甲基] -1,3-二氮杂螺[4.4]壬-1-烯-4-酮与碱金属叠氮化物和三（C 1-4 - ）烷基胺氢卤化物反应，在非极性非质子溶剂中存在相转移催化剂以产生2-正丁基-3 - [[2' - （四唑-5-基）联苯-4-基]甲基] -1 ，3-二氮杂[4.4]壬-1-烯-4-酮; 和b）中和2-正丁基-3 - [[2' - （四唑-5-基）联苯-4-基]甲基] -1,3-二氮杂螺[4.4]萘-1-基的碱性盐， en-4-酮在含有酸的水性介质中产生厄贝沙坦，并任选地将获得的厄贝沙坦转化为其药学上可接受的盐。

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