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1. 发明申请

US20130165696A1 NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR 审中-公开
标题翻译：用于制备苯甲酰胺衍生物的新方法及其制备TICAGRELOR的用途
公开(公告)号：US20130165696A1
公开(公告)日：2013-06-27
申请号：US13805150
申请日：2011-06-28
申请人： Anil Shahaji Khile , Vignesh Nair , Nikhil Trivedi , Nitin Sharadchandra Pradhan
发明人： Anil Shahaji Khile , Vignesh Nair , Nikhil Trivedi , Nitin Sharadchandra Pradhan
IPC分类号： C07C209/46
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。本文特别提供了用于制备基本上纯的泰格列洛中间体，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。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以高产率和纯度制备泰格列洛或其药学上可接受的盐。

2. 发明申请

US20120164188A1 PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES 审中-公开
标题翻译： PALIPERIDONE或其药物接受的盐，无特殊物质
公开(公告)号：US20120164188A1
公开(公告)日：2012-06-28
申请号：US13381716
申请日：2010-09-10
申请人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan
发明人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan
IPC分类号： A61K31/519 , A61K9/14 , A61P25/18 , C07D471/04
CPC分类号： C07D471/04
摘要： Provided herein are impurities of paliperidone, 3-[2-[4-[1-(4-fluoro-2-hydroxyphenyl)methanoyl]piperidinyl-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (methanoyl impurity), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-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：本文提供的是普利培酮，3- [2- [4- [1-（4-氟-2-羟基苯基）甲酰基]哌啶-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-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。本文进一步提供了基本上不含甲酰基，脱羟基和9-酮杂质的高度纯的普利培酮或其药学上可接受的盐，其制备方法和包含高度纯的普利培酮或其药学上可接受的盐基本上不含甲酰基的药物组合物，脱羟基和9-酮杂质。本文还提供了用于制备利培酮中间体的改进和有效的方法。

3. 发明授权

US08101597B2 Quetiapine salts and their polymorphs 失效
标题翻译：喹硫平盐及其多晶型物
公开(公告)号：US08101597B2
公开(公告)日：2012-01-24
申请号：US12599085
申请日：2008-05-07
申请人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61P25/18 , A61K31/55 , C07D281/16
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

US20140206867A1 Process for Preparing Cyclopentylamine Derivatives and Intermediates Thereof 审中-公开
标题翻译：制备环戊胺衍生物及其中间体的方法
公开(公告)号：US20140206867A1
公开(公告)日：2014-07-24
申请号：US14126102
申请日：2012-06-13
申请人： Anil Shahaji Khile , Vignesh Nair , Nikhil Trivedi , Nitin Sharadchandra Pradhan
发明人： Anil Shahaji Khile , Vignesh Nair , Nikhil Trivedi , Nitin Sharadchandra Pradhan
IPC分类号： C07D317/44 , C07D487/04
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，其是制备三唑并[4,5-d]嘧啶化合物的有用中间体。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-（3aα，4α，6α，6aα）-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。

5. 发明授权

US08859769B2 Processes for preparing ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine 有权
标题翻译：制备泰格列洛中间体，4,6-二氯-5-硝基-2-（丙硫基）嘧啶的方法
公开(公告)号：US08859769B2
公开(公告)日：2014-10-14
申请号：US13521780
申请日：2011-02-15
申请人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
发明人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
IPC分类号： C07D239/38 , C07D239/60 , C07D487/04 , C07D239/47
CPC分类号： C07D239/47 , C07D239/60 , C07D487/04
摘要： Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
摘要翻译：本文提供了在制备基本上纯的泰格列洛中间体4,6-二氯-5-硝基-2-（丙硫基）嘧啶，式（II）的改进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。

6. 发明申请

US20130317220A1 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：US20130317220A1
公开(公告)日：2013-11-28
申请号：US13996100
申请日：2011-12-16
申请人： Vignesh Nair , Nikhil Trivedi , Anil Shahaji Khile , Nitin Sharadchandra Pradhan
发明人： Vignesh Nair , Nikhil Trivedi , Anil Shahaji Khile , Nitin Sharadchandra Pradhan
IPC分类号： C07D487/04 , C07D317/44 , C07D405/12 , C07C271/24 , 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。

7. 发明申请

US20130030176A1 PROCESSES FOR PREPARING TICAGRELOR INTERMEDIATE, 4,6-DICHLORO-5-NITRO-2-(PROPYLTHIO)PYRIMIDINE 有权
标题翻译：制备中间体的方法，4,6-二氯-5-硝基-2-（丙基）吡啶
公开(公告)号：US20130030176A1
公开(公告)日：2013-01-31
申请号：US13521780
申请日：2011-02-15
申请人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
发明人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
IPC分类号： C07D239/47 , C07D487/04 , C07D239/60
CPC分类号： C07D239/47 , C07D239/60 , C07D487/04
摘要： Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
摘要翻译：本文提供了在制备基本上纯的泰格列洛中间体4,6-二氯-5-硝基-2-（丙硫基）嘧啶，式（II）的改进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。

8. 发明申请

US20100260851A1 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态性及其用于制备无定形阿托伐他汀钙的方法
公开(公告)号：US20100260851A1
公开(公告)日：2010-10-14
申请号：US12668433
申请日：2008-07-11
申请人： Girish Dixit , Anil Shahaji Khile , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Anil Shahaji Khile , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K9/14 , A61K31/40 , C07D207/34 , A61P3/06 , A61P9/10
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-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl-1H-pyrrole-1-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，药物组合物及其处理方法。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） - [[b]]，[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用于制备无定形阿托伐他汀钙的用途。

9. 发明申请

US20130150577A1 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：US20130150577A1
公开(公告)日：2013-06-13
申请号：US13642239
申请日：2011-04-19
申请人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
发明人： Anil Shahaji Khile , Jayesh Patel , Nikhil Trivedi , Nitin Sharadchandra Pradhan
IPC分类号： C07C209/34 , C07C205/26 , C07C205/05 , C07C205/45
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。本文特别提供了一种用于制备基本上纯粹的泰格列洛中间体反式 - （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。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。

10. 发明申请

US20120100188A1 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：US20120100188A1
公开(公告)日：2012-04-26
申请号：US13318664
申请日：2010-05-25
申请人： Girish Dixit , Anil Shahaji Khile , Vignesh Nair , Nitin Sharadechandra Pradhan
发明人： Girish Dixit , Anil Shahaji Khile , Vignesh Nair , Nitin Sharadechandra Pradhan
IPC分类号： A61K31/519 , A61K9/14 , C07D471/04
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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