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1. 发明申请

WO2012085665A3 NOVEL PROCESSES FOR PREPARING TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备三唑并[4,5-D]吡嗪衍生物的新方法及其中间体
公开(公告)号：WO2012085665A3
公开(公告)日：2013-01-10
申请号：PCT/IB2011003234
申请日：2011-12-16
申请人： ACTAVIS GROUP PTC EHF , NAIR VIGNESH , TRIVEDI NIKHIL , KHILE ANIL SHAHAJI , PRADHAN NITIN SHARADCHANDRA
发明人： NAIR VIGNESH , TRIVEDI NIKHIL , KHILE ANIL SHAHAJI , PRADHAN NITIN SHARADCHANDRA
IPC分类号： C07D239/48 , C07C269/00 , C07D317/44 , C07D405/12 , C07D487/04
CPC分类号： C07D487/04 , C07C271/24 , C07C2601/02 , C07D239/48 , C07D239/50 , C07D317/44 , C07D405/12
摘要： Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 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：本文提供了制备三唑并[4,5-d]嘧啶衍生物的新方法。本文特别地提供了一种用于制备高纯度泰格列洛或其药学上可接受的盐的新颖的，商业上可行的和工业上有利的方法。本文进一步提供了制备取代的环戊胺衍生物的新方法，其是三唑并[4,5-d]嘧啶化合物的制备中的有用中间体。本文特别提供了一种新颖的，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，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

WO2012001531A3 NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR 审中-公开
标题翻译：制备苯基环丙胺衍生物的新方法及其用于制备三癸酸酯的用途
公开(公告)号：WO2012001531A3
公开(公告)日：2012-08-16
申请号：PCT/IB2011002246
申请日：2011-06-28
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： C07C209/56 , C07C209/62 , C07C211/40
CPC分类号： C07C209/62 , C07B2200/13 , C07C209/56 , C07C211/35 , C07C211/40 , C07C2601/02 , C07C2601/16
摘要： Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：本文提供了制备苯基环丙胺衍生物的新方法，其为制备三唑并[4,5-d]嘧啶化合物的有用中间体。本文特别提供了制备基本上纯的替格瑞洛中间体反式 - （1R，2S）-2-（3,4-二氟苯基） - 环丙胺的新颖的，商业上可行的和工业上有利的方法。本文进一步提供反式 - （1R，2S）-2-（3,4-二氟苯基） - 环丙胺的新型酸加成盐及其制备方法。中间体及其酸加成盐可用于高产率和高纯度地制备替格瑞洛或其药学上可接受的盐。

3. 发明申请

WO2012085665A8 NOVEL PROCESSES FOR PREPARING TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备三唑并[4,5-D]吡嗪衍生物的新方法及其中间体
公开(公告)号：WO2012085665A8
公开(公告)日：2012-09-13
申请号：PCT/IB2011003234
申请日：2011-12-16
申请人： ACTAVIS GROUP PTC EHF , NAIR VIGNESH , TRIVEDI NIKHIL , KHILE ANIL SHAHAJI , PRADHAN NITIN SHARADCHANDRA
发明人： NAIR VIGNESH , TRIVEDI NIKHIL , KHILE ANIL SHAHAJI , PRADHAN NITIN SHARADCHANDRA
IPC分类号： C07D239/48
CPC分类号： C07D487/04 , C07C271/24 , C07C2601/02 , C07D239/48 , C07D239/50 , C07D317/44 , C07D405/12
摘要： Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 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：本文提供了制备三唑并[4,5-d]嘧啶衍生物的新方法。本文特别地提供了一种用于制备高纯度泰格列洛或其药学上可接受的盐的新颖的，商业上可行的和工业上有利的方法。本文进一步提供了制备取代的环戊胺衍生物的新方法，其是三唑并[4,5-d]嘧啶化合物的制备中的有用中间体。本文特别提供了一种新颖的，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，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。

4. 发明申请

WO2011132083A3 NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES 审中-公开
标题翻译：使用新型中间体制备苯甲酰胺衍生物的新方法
公开(公告)号：WO2011132083A3
公开(公告)日：2012-01-05
申请号：PCT/IB2011001289
申请日：2011-04-19
申请人： ACTAVIS GROUP PTC EHF , KHILE ANIL SHAHAJI , PATEL JAYESH , TRIVEDI NIKHIL , PRADHAN NITIN SHARADCHANDRA
发明人： KHILE ANIL SHAHAJI , PATEL JAYESH , TRIVEDI NIKHIL , PRADHAN NITIN SHARADCHANDRA
IPC分类号： C07C45/46 , C07C49/233 , C07C201/10 , C07C201/12 , C07C205/10 , C07C205/16 , C07C205/45 , C07C209/34
CPC分类号： C07C209/34 , C07C45/46 , C07C201/10 , C07C201/12 , C07C205/05 , C07C205/10 , C07C205/16 , C07C205/26 , C07C205/45 , C07C211/40 , C07C2601/02 , C07C49/233
摘要： Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：本文提供了一种制备苯基环丙基胺衍生物的新方法，其是三唑并[4,5-d]嘧啶化合物的制备中的有用中间体。本文特别地提供了一种用于制备基本上纯粹的泰格列洛中间体，反 - （1R，2S）-2-（3,4-二氟苯基） - 环丙胺的新颖的，商业上可行的和工业上有利的方法。中间体可用于以高产率和纯度制备替卡格雷或其药学上可接受的盐。

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

WO2009004480A3 QUETIAPINE SALTS AND THEIR POLYMORPHS 审中-公开
标题翻译：喹硫平盐及其多晶型物
公开(公告)号：WO2009004480A3
公开(公告)日：2009-11-05
申请号：PCT/IB2008002341
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
IPC分类号： C07D281/16 , A61K31/55
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型稳定盐形式，制备方法，药物组合物及其治疗方法。更具体地说，本发明提供了喹硫平的新的酸加成盐，其中酸抗衡离子由选自苯磺酸，二苯甲酰基-L-（+） - 酒石酸和二 - 对甲苯甲酰基-L-酒石酸的酸提供。 L - （+） - 酒石酸。本发明还提供了喹硫平盐的新型多晶型物，所述奎硫平盐选自由氢溴酸奎硫平，硫酸喹硫平，硝酸喹硫平和柠檬酸喹硫平组成的组。

7. 发明申请

WO2009013633A3 AMORPHOUS COPRECIPITATES OF ATORVASTATIN PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
公开(公告)号：WO2009013633A3
公开(公告)日：2009-05-14
申请号：PCT/IB2008002808
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
CPC分类号： C07D207/416 , A61K9/146 , A61K9/1635 , A61K31/40
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

8. 发明申请

WO2009013633A2 AMORPHOUS COPRECIPITATES OF ATORVASTATIN PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译： ATORVASTATIN药物不良接种的非同源共培养
公开(公告)号：WO2009013633A2
公开(公告)日：2009-01-29
申请号：PCT/IB2008002808
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
CPC分类号： C07D207/416 , A61K9/146 , A61K9/1635 , A61K31/40
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
摘要翻译：本发明涉及阿托伐他汀药学上可接受的盐与药学上可接受的赋形剂的稳定无定形共沉淀物，制备方法，药物组合物及其治疗方法。有利地，本发明的阿托伐他汀药物可接受的盐的无定形共沉淀物具有改善的生理化学特征，其有助于有效的生物利用度

9. 发明申请

WO2009024863A3 PROCESS FOR THE PREPARATION OF MODAFINIL ENANTIOMERS 审中-公开
标题翻译：制备改性剂的方法
公开(公告)号：WO2009024863A3
公开(公告)日：2009-08-06
申请号：PCT/IB2008002634
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：本文公开了用于制备阿莫非尼的方便的，商业上可行的和环境友好的方法。本发明还提供了一种改进的，商业上可行的和工业上有利的方法，用于制备基本上不含砜杂质的纯2 - [（二苯基甲基）亚磺酰基]乙酸（也称为莫多芬酸），即2 - [（二苯基甲基）磺酰基 ]乙酸。该中间体可用于以高产率和纯度制备Modafmil及其对映体或其药学上可接受的盐。

10. 发明申请

WO2009007856A3 NOVEL POLYMORPH OF ATORVASTATIN CALCIUM AND USE THEREOF FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译： ATORVASTATIN钙的新型聚合物及其用于制备无定形ATORVASTATIN钙的方法
公开(公告)号：WO2009007856A3
公开(公告)日：2009-06-25
申请号：PCT/IB2008002624
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
IPC分类号： C07D237/34 , A61K31/40 , A61P3/06
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)- [ß],[d]-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：本发明提供了一种新型的阿托伐他汀钙多形态，称为形式A1，制备方法，药物组合物及其治疗方法。本发明还提供使用新型阿托伐他汀钙形式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称为[R-（R *，R *）] - 2-（4-氟苯基） - [ß]，[d] - 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用于制备无定形阿托伐他汀钙的用途。

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