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    Lysine specific demethylase-1 inhibitors and their use
    4.
    发明授权
    Lysine specific demethylase-1 inhibitors and their use 有权

    公开(公告)号：US10202330B2

    公开(公告)日：2019-02-12

    申请号：US14843095

    申请日：2015-09-02

    申请人： ORYZON GENOMICS S.A.

    发明人： Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

    IPC分类号： A61K31/165 ,  C07C217/74 ,  A61K45/06 ,  C07C211/42 ,  C07C211/40 ,  C07C237/24 ,  A61K31/135 ,  A61N5/10

    摘要： The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

    NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR
    9.
    发明申请
    NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR 审中-公开
    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：US20140350301A1

    公开(公告)日：2014-11-27

    申请号：US14298319

    申请日：2014-06-06

    申请人： Actavis Group PTC ehf

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

    IPC分类号： 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。