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    CRYSTALLINE FORM OF SUNITINIB AND PROCESSES FOR ITS PREPARATION
    1.
    发明申请
    CRYSTALLINE FORM OF SUNITINIB AND PROCESSES FOR ITS PREPARATION 审中-公开
    SUNITINIB的结晶形式及其制备方法

    公开(公告)号：US20120029046A1

    公开(公告)日：2012-02-02

    申请号：US13060331

    申请日：2009-08-24

    Applicant: Vinayak Gore ,  Bharati Choudhari ,  Mahesh Hublikar ,  Prakash Bansode

    Inventor： Vinayak Gore ,  Bharati Choudhari ,  Mahesh Hublikar ,  Prakash Bansode

    IPC: A61K31/404 ,  A61P35/00 ,  C07D403/06

    CPC classification number: C07D403/06

    Abstract: The present invention relates to a novel crystalline form of sunitinib free base designated form I and to processes for its preparation. The invention also relates to its use as an API and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising the novel crystalline form and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.

    Abstract translation: 本发明涉及一种指定为I型的舒尼替尼游离碱的新结晶形式及其制备方法。 本发明还涉及其作为API和用于制备各种形式的舒尼替尼的用途。 此外，本发明涉及包含根据本发明制备的新结晶形式和盐，溶剂合物和水合物以及所述药物组合物在治疗和/或预防癌症中的用途的药物组合物。

    PROCESS FOR THE PRODUCTION OF ETRAVIRINE
    2.
    发明申请
    PROCESS FOR THE PRODUCTION OF ETRAVIRINE 有权
    生产乙酰胆碱的方法

    公开(公告)号：US20130116433A1

    公开(公告)日：2013-05-09

    申请号：US13456319

    申请日：2012-04-26

    Applicant: Vinayak Gore ,  Choudhari Bharati ,  Mahesh Hublikar ,  Prakash Bansode ,  Sandip Sinore

    Inventor： Vinayak Gore ,  Choudhari Bharati ,  Mahesh Hublikar ,  Prakash Bansode ,  Sandip Sinore

    IPC: C07D239/48

    CPC classification number: C07D239/48

    Abstract: A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula (IV). The condensation of formula (IV) with 3,5-dimethyl-4-hydroxybenzonitrile yields a compound of formula (VI), and an optional deprotection of the compound of formula (VI) results in Etravirine.

    Abstract translation: 一种制备依曲维林的新方法包括氰基乙酸乙酯与N-氰基苯基胍的缩合，得到式（II）的-OH化合物，其进一步转化成式（III）的离去基团。 任选地将式（III）化合物保护并溴化，得到式（IV）的化合物。 式（Ⅳ）与3,5-二甲基-4-羟基苄腈的缩合得到式（Ⅵ）化合物，式（Ⅵ）化合物任意脱保护得Etravirine。

    Process for the production of etravirine
    5.
    发明授权
    Process for the production of etravirine 有权
    生产依曲韦林的方法

    公开(公告)号：US08653266B2

    公开(公告)日：2014-02-18

    申请号：US13456319

    申请日：2012-04-26

    Applicant: Vinayak Gore ,  Choudhari Bharati ,  Mahesh Hublikar ,  Prakash Bansode ,  Sandip Sinore

    Inventor： Vinayak Gore ,  Choudhari Bharati ,  Mahesh Hublikar ,  Prakash Bansode ,  Sandip Sinore

    IPC: C07D239/24

    CPC classification number: C07D239/48

    Abstract: A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula (IV). The condensation of formula (IV) with 3,5-dimethyl-4-hydroxybenzonitrile yields a compound of formula (VI), and an optional deprotection of the compound of formula (VI) results in Etravirine.

    Abstract translation: 一种制备依曲维林的新方法包括氰基乙酸乙酯与N-氰基苯基胍的缩合，得到式（II）的-OH化合物，其进一步转化成式（III）的离去基团。 任选地将式（III）化合物保护并溴化，得到式（IV）的化合物。 式（Ⅳ）与3,5-二甲基-4-羟基苄腈的缩合得到式（Ⅵ）化合物，式（Ⅵ）化合物任意脱保护得Etravirine。

    NOVEL POLYMORPHS OF SUNITINIB AND PROCESSES FOR THEIR PREPARATION
    6.
    发明申请
    NOVEL POLYMORPHS OF SUNITINIB AND PROCESSES FOR THEIR PREPARATION 审中-公开
    SUNITINIB的新型聚合物及其制备方法

    公开(公告)号：US20110263670A1

    公开(公告)日：2011-10-27

    申请号：US13060322

    申请日：2009-08-24

    Applicant: Vinayak Gore ,  Bharati Choudhari ,  Mahesh Hublikar ,  Prakash Bansode

    Inventor： Vinayak Gore ,  Bharati Choudhari ,  Mahesh Hublikar ,  Prakash Bansode

    IPC: A61K31/404 ,  A61P35/00 ,  C07D403/06

    CPC classification number: C07D403/06

    Abstract: The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.

    Abstract translation: 本发明涉及指定为II型和III型的舒尼替尼游离碱的新型多晶型物及其制备方法。 本发明还涉及它们作为API和用于制备各种形式的舒尼替尼的用途。 此外，本发明涉及包含所述新型多晶型物和根据本发明制备的盐，溶剂合物和水合物以及所述药物组合物在治疗和/或预防癌症中的用途的药物组合物。

    Polymorphic forms
    9.
    发明授权
    Polymorphic forms 有权
    多形态

    公开(公告)号：US08288401B2

    公开(公告)日：2012-10-16

    申请号：US12599108

    申请日：2008-05-08

    Applicant: Abhay Gaitonde ,  Bindu Manojkumar ,  Sandeep Mekde ,  Dattaatraya Shinde ,  Prakash Bansode

    Inventor： Abhay Gaitonde ,  Bindu Manojkumar ,  Sandeep Mekde ,  Dattaatraya Shinde ,  Prakash Bansode

    IPC: A01N43/54 ,  A61K31/505

    CPC classification number: C07D403/04

    Abstract: Novel polymorphic forms of bosentan and processes for their preparation are disclosed. Further, pharmaceutical compositions comprising said polymorphic forms and the use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris are disclosed.

    Abstract translation: 公开了波形坦的新型多晶型物及其制备方法。 此外，公开了包含所述多形态形式的药物组合物和所述组合物在治疗患有内皮素受体介导的病症的患者中的用途，例如心血管疾病如高血压，肺动脉高压，局部缺血，血管痉挛和心绞痛。

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