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    NOVEL PROCESSES FOR PREPARING TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
    1.
    发明申请
    NOVEL PROCESSES FOR PREPARING TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
    制备三唑并[4,5-D]嘧啶衍生物及其中间体的新方法

    公开(公告)号：WO2012085665A2

    公开(公告)日：2012-06-28

    申请号：PCT/IB2011/003234

    申请日：2011-12-16

    Applicant: ACTAVIS GROUP PATC EHF ,  NAIR, Vignesh ,  TRIVEDI, Nikhil ,  KHILE, Anil, Shahaji ,  PRADHAN, Nitin, Sharadchandra

    Inventor： NAIR, Vignesh ,  TRIVEDI, Nikhil ,  KHILE, Anil, Shahaji ,  PRADHAN, Nitin, Sharadchandra

    IPC: C07D239/48

    CPC classification number: C07D487/04 ,  C07C271/24 ,  C07C2601/02 ,  C07D239/48 ,  C07D239/50 ,  C07D317/44 ,  C07D405/12

    Abstract: 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.

    Abstract translation: 本文提供了制备三唑并[4,5-d]嘧啶衍生物的新方法。 本文特别提供了用于制备高纯度替格瑞洛或其药学上可接受的盐的新型商业上可行且工业上有利的方法。 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替格瑞洛中间体2 - [[（3aR，4S，6R，6aS）-6-氨基-2,2-二甲基四氢-3aH-环戊二烯并[d ] [1,3] - 间二氧杂环戊烯-4-基]氧基] -1-乙醇。

    PROCESS FOR THE PREPARATION OF MODAFINIL ENANTIOMERS
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF MODAFINIL ENANTIOMERS 审中-公开
    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

    Applicant: ACTAVIS GROUP PTC EHF ,  GIRISH, Dixit ,  KHILE, Anil, Shahaji ,  PRADHAN, Nitin, Sharadchandra ,  VALGEIRSSON, Jon

    Inventor： GIRISH, Dixit ,  KHILE, Anil, Shahaji ,  PRADHAN, Nitin, Sharadchandra ,  VALGEIRSSON, Jon

    IPC: C07C315/02 ,  C07C315/04 ,  C07C317/44

    CPC classification number: C07C315/02 ,  C07B2200/07 ,  C07C315/04 ,  C07C317/44

    Abstract: 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.

    Abstract translation: 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。

    PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES
    7.
    发明申请
    PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES 审中-公开
    帕利哌酮或药物可接受的盐，大部分不含杂质

    公开(公告)号：WO2011030224A3

    公开(公告)日：2011-03-17

    申请号：PCT/IB2010/002568

    申请日：2010-09-10

    Applicant: ACTAVIS GROUP PTC EHF ,  DIXIT, Girish ,  KHILE, Anil, Shahaji ,  PATEL, Jayesh, Laljibhai ,  PRADHAN, Nitin, Sharadchandra

    Inventor： DIXIT, Girish ,  KHILE, Anil, Shahaji ,  PATEL, Jayesh, Laljibhai ,  PRADHAN, Nitin, Sharadchandra

    IPC: C07D471/04 ,  A61K31/519 ,  A61P25/00

    Abstract: 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.

    Abstract translation: 本文提供了帕潘立酮，3- [2- [4- [1-（4-呋喃-2-羟基苯基）甲酰基]哌啶基-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-1,2-二氢 - 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。

    IMPROVED PROCESS FOR PREPARING CYCLOPENTYLAMINE DERIVATIVES AND INTERMEDIATES THEREOF
    9.
    发明申请
    IMPROVED PROCESS FOR PREPARING CYCLOPENTYLAMINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
    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

    Applicant: ACTAVIS GROUP PTC EHF ,  KHILE, Anil, Shahaji ,  NAIR, Vignesh ,  TRIVEDI, Nikhil ,  PRADHAN, Nitin, Sharadchandra

    Inventor： KHILE, Anil, Shahaji ,  NAIR, Vignesh ,  TRIVEDI, Nikhil ,  PRADHAN, Nitin, Sharadchandra

    IPC: C07D317/44 ,  C07F7/08

    CPC classification number: C07D317/44 ,  C07D487/04

    Abstract: 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.

    Abstract translation: 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。

    PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES
    10.
    发明申请
    PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES 审中-公开
    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

    Applicant: ACTAVIS GROUP PTC EHF ,  DIXIT GIRISH ,  KHILE ANIL SHAHAJI ,  PATEL JAYESH LALJIBHAI ,  PRADHAN NITIN SHARADCHANDRA

    Inventor： DIXIT GIRISH ,  KHILE ANIL SHAHAJI ,  PATEL JAYESH LALJIBHAI ,  PRADHAN NITIN SHARADCHANDRA

    IPC: C07D471/04 ,  A61K31/519 ,  A61P25/00

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

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