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1. 发明申请

WO2012172426A1 IMPROVED PROCESS FOR PREPARING CYCLOPENTYLAMINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备环戊二烯衍生物的改进方法及其中间体
公开(公告)号：WO2012172426A1
公开(公告)日：2012-12-20
申请号：PCT/IB2012/001344
申请日：2012-06-13
申请人： ACTAVIS GROUP PTC EHF , KHILE, Anil, Shahaji , NAIR, Vignesh , TRIVEDI, Nikhil , PRADHAN, Nitin, Sharadchandra
发明人： KHILE, Anil, Shahaji , NAIR, Vignesh , TRIVEDI, Nikhil , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D317/44 , C07F7/08
CPC分类号： C07D317/44 , C07D487/04
摘要： Disclosed herein is an improved process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Particularly described is an improved, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, [3aR-(3aα,4α,6α,6aα]-2-[[6-amino-2,2-dimethyltetrahydro-4H-cyclopenta-1,3-dioxol-4- yl]oxy]-ethanol, alternatively named, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro- 3aH-cyclopenta[d] [1,3] -dioxol-4-yl]oxy] -1-ethanol.
摘要翻译：本文公开了一种制备取代的环戊胺衍生物的改进方法，其是三唑并[4,5-d]嘧啶化合物的制备中的有用中间体。特别描述了一种改进的，商业上可行的和工业上有利的制备泰格列洛中间体的方法，[3aR-（3aa，4a，6a，6aa）-2 - [[6-氨基-2,2-二甲基四氢-4H-环戊二烯 -1,3-二氧杂环戊烯-4-基]氧基]乙醇，或者名称为2 - [[（3aR，4S，6R，6aS）-6-氨基-2,2-二甲基四氢-3HH-环戊二烯并[d] [ 1,3] - 二氧杂环戊烯-4-基]氧基] -1-乙醇。

2. 发明申请

WO2012063126A3 IMPROVED PROCESSES FOR PREPARING PURE (3AR,4S,6R,6AS)-6-AMINO-2,2-DIMETHYLTETRAHDRO-3AH-CYCLOPENTA[D] [1,3]-DIOXOL-4-OL AND ITS KEY STARTING MATERIAL 审中-公开
公开(公告)号：WO2012063126A3
公开(公告)日：2012-05-18
申请号：PCT/IB2011/002889
申请日：2011-10-25
申请人： ACTAVIS GROUP PTC EHF , KUMAR, Arvapally, Seshu , TRIVEDI, Nikhil , PRADHAN, Nitin, Sharadchandra , SHARMA, Krishnadatt
发明人： KUMAR, Arvapally, Seshu , TRIVEDI, Nikhil , PRADHAN, Nitin, Sharadchandra , SHARMA, Krishnadatt
IPC分类号： C07D317/06
摘要： Provided herein is an improved, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, (3aR,4S,6R,6aS)-6-amino-2,2- dimethyltetrahydro-3aH-cyclopenta[d][l,3]-dioxol-4-ol, which is useful for preparing ticagrelor or a pharmaceutically acceptable salt thereof in high yield and purity. The present invention further relates to an improved process for the preparation of (lS,4R)-cis-4-acetoxy- 2-cyclopenten-l-ol, which is a key starting material in the preparation of the ticagrelor intermediate.

3. 发明申请

WO2011128784A3 NOVEL PROCESS FOR PREPARING HIGHLY PURE TAPENTADOL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：制备高纯度扁桃醇或其药学上可接受的盐的新方法
公开(公告)号：WO2011128784A3
公开(公告)日：2012-01-19
申请号：PCT/IB2011001484
申请日：2011-04-04
申请人： ACTAVIS GROUP PTC EHF , KHUNT MAYUR DEVJIBHAI , BONDGE SANDIPAN PRABHURAO , PATIL NILESH SUDHIR , PAGIRE HAUSHABHAU SHIVAJI , PRADHAN NITIN SHARADCHANDRA
发明人： KHUNT MAYUR DEVJIBHAI , BONDGE SANDIPAN PRABHURAO , PATIL NILESH SUDHIR , PAGIRE HAUSHABHAU SHIVAJI , PRADHAN NITIN SHARADCHANDRA
IPC分类号： C07C215/54
CPC分类号： C07C213/00 , C07B2200/07 , C07C213/02 , C07C213/10 , C07C215/08 , C07C215/62 , C07C221/00 , C07C225/06 , C07C225/16
摘要： Provided herein is a novel, commercially viable and industrially advantageous process for the preparation of 3-[(1R,2R)-3-(dimethylamino)-l-ethyl-2-methylpropyl]phenol (Tapentadol), or a pharmaceutically acceptable salt thereof, and its intermediates, in high yield and purity. Provided also herein are novel solid state forms of tapentadol intermediates and processes for their preparation thereof. Provided further herein is a purification process for preparing highly pure tapentadol hydrochloride.
摘要翻译：本文提供了一种用于制备3 - [（1R，2R）-3-（二甲基氨基）-1-乙基-2-甲基丙基]苯酚（他喷他多））或其药学上可接受的盐的新型商业上可行的和工业上有利的方法，及其中间体，产率高，纯度高。本文还提供了新的固体形式的他喷他多中间体及其制备方法。本文进一步提供用于制备高纯度盐酸他喷他多的纯化方法。

4. 发明申请

WO2011048491A2 AMORPHOUS ROTIGOTINE CO-PRECIPITATES 审中-公开
标题翻译：异黄酮类抗生素
公开(公告)号：WO2011048491A2
公开(公告)日：2011-04-28
申请号：PCT/IB2010/002844
申请日：2010-10-18
申请人： ACTAVIS GROUP PTC EHF , KHUNT, Mayur, Devjibhai , KUMAR, Udhaya , PRADHAN, Nitin, Sharadchandra
发明人： KHUNT, Mayur, Devjibhai , KUMAR, Udhaya , PRADHAN, Nitin, Sharadchandra
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A61K31/381
摘要： Disclosed herein is a stable amorphous co -precipitate of (-)-(S)-5-hydroxy-2-[N-n- propyl-N-2-(2-thienyl)ethylamino]tetralin (Rotigotine) with pharmaceutically acceptable excipients, methods for the preparation, pharmaceutical compositions, and methods of treating thereof. Advantageously, the amorphous co-precipitates of rotigotine have improved physio chemical characteristics that assist in their effective bioavailability.
摘要翻译：本文公开了（ - ） - （S）-5-羟基-2- [正丙基-N-2-（2-噻吩基）乙基氨基]四氢化萘（罗替戈汀）与药学上可接受的赋形剂的稳定无定形共沉淀物，方法用于制备，药物组合物及其治疗方法。有利地，罗替戈汀的无定形共沉淀物具有改善的生理化学特性，有助于其有效的生物利用度。

5. 发明申请

WO2011030224A2 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：WO2011030224A2
公开(公告)日：2011-03-17
申请号：PCT/IB2010002568
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
CPC分类号： C07D471/04
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-氟-2-羟基苯基）甲酰基]哌啶基-1-基]乙基] -2-甲基-6,7,8,9-四氢 - 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-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）及其制备方法和分离方法。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。

6. 发明申请

WO2010133976A3 SUBSTANTIALLY PURE IMATINIB OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
公开(公告)号：WO2010133976A3
公开(公告)日：2010-11-25
申请号：PCT/IB2010/001476
申请日：2010-05-24
申请人： ACTAVIS GROUP PTC EHF , KHUNT, Mayur, Devjibhai , PATIL, Nilesh, Sudhir , PAGIRE, Haushabhau, Shivaji , PRADHAN, Nitin, Sharadchandra
发明人： KHUNT, Mayur, Devjibhai , PATIL, Nilesh, Sudhir , PAGIRE, Haushabhau, Shivaji , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07D401/04 , C07D401/14 , A61K31/506 , A61P35/02
摘要： Provided herein are impurities of imatinib, N-(2-Methyl-5-methylamino-phenyl)-N- (4-pyridin-3-yl-pyrimidin-2-yl)-formamide (formamide impurity) and 4-[4-(Imidazole-1- carbonyl)-piperazin-1 -ylmethyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide (carbonylimidazole impurity), and processes for the preparation and isolation thereof. Provided further herein is a highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of formamide and carbonylimidazole impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of impurities. Disclosed also herein is a process for preparing substantially pure α-form of imatinib mesylate.

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

WO2010067204A1 HIGHLY PURE CINACALCET OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：高纯度CINACALCET或其药学上可接受的盐
公开(公告)号：WO2010067204A1
公开(公告)日：2010-06-17
申请号：PCT/IB2009/007932
申请日：2009-12-08
申请人： ACTAVIS GROUP PTC EHF , SEBASTIAN, Sonny , PERI, Seetha, Rama, Sarma , RAMAMURTHY, Katikireddy , PRADHAN, Nitin, Sharadchandra
发明人： SEBASTIAN, Sonny , PERI, Seetha, Rama, Sarma , RAMAMURTHY, Katikireddy , PRADHAN, Nitin, Sharadchandra
IPC分类号： C07C211/30 , C07C291/04 , A61K31/135 , A61P13/12
CPC分类号： C07C211/30 , C07C291/04 , C07C2602/10
摘要： Provided herein are impurities of cinacalcet, (R)-α-methyl-N-[3-[3-(trifluoromethyl) phenyl]propyl]-1-(5,6,7,8-tetrahydronaphthalene)methaneamine (tetrahydro cinacalcet impurity), (R)-α-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1- naphthalenemethaneamine-N-oxide (cinacalcet N-oxide impurity) and (R)-α-methyl-N-[3-[3- (trifiuoromethyl)phenyl]methyl]-1-naphthalenemethaneamine (benzylamine impurity); and processes for preparation and isolation thereof. Provided further herein is a highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities.
摘要翻译：本文提供西那卡塞，（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]丙基] -1-（5,6,7,8-四氢萘）甲胺（四氢西那卡塞杂质），（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]丙基] -1-萘甲烷胺-N-氧化物（西那卡塞N-氧化物杂质）和（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]甲基] -1-萘甲烷胺（苄胺杂质）; 以及其制备和分离方法。本文进一步提供了基本上不含杂质的高纯度西那卡塞或其药学上可接受的盐，其制备方法和包含高纯度西那卡塞或其药学上可接受的盐基本上不含杂质的药物组合物。

9. 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。

10. 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）。

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