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    IMPROVED FORMS OF A PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS
    5.
    发明公开
    IMPROVED FORMS OF A PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS 审中-公开
    VERBESSERTE FORMEN EINES PO3K-DELTA-SELEKTIVEN HEMMERS ZUR VERWENDUNG in PHARMAZEUTISCHEN FORMULIERUNGEN

    公开(公告)号：EP3149000A1

    公开(公告)日：2017-04-05

    申请号：EP15733532.4

    申请日：2015-05-26

    申请人： Rhizen Pharmaceuticals S.A.

    发明人： VAKKALANKA, Swaroop Kumar Venkata Satya

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

    CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  C07B2200/13 ,  C07C309/30

    摘要： The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.

    摘要翻译： 本发明涉及选择性PI3Kδ抑制剂（S）-2-（1-（4-氨基-3-（3-氟-4-异丙氧基苯基） - 嘧啶-2-基）-3-甲基苯磺酸的对甲苯磺酸盐（PTSA） 乙基）-6-氟-3-（3-氟苯基）-4H-色烯-4-酮（TGR-1202）。 本发明还涉及其制备方法，含有它们的药物组合物，以及通过施用PI3K激酶介导的疾病或病症如癌症的方法。

    PROCESS FOR PREPARATION OF OPTICALLY PURE AND OPTIONALLY SUBSTITUTED 2- (1 -HYDROXY- ALKYL) - CHROMEN - 4 - ONE DERIVATIVES AND THEIR USE IN PREPARING PHARMACEUTICALS
    10.
    发明公开
    PROCESS FOR PREPARATION OF OPTICALLY PURE AND OPTIONALLY SUBSTITUTED 2- (1 -HYDROXY- ALKYL) - CHROMEN - 4 - ONE DERIVATIVES AND THEIR USE IN PREPARING PHARMACEUTICALS 审中-公开
    PROCESS生产光学纯和可选取代的2-（1-羟烷基）苯并吡喃-4- ON衍生物及其在药物方面的制造

    公开(公告)号：EP2844647A1

    公开(公告)日：2015-03-11

    申请号：EP13729095.3

    申请日：2013-05-03

    申请人： Rhizen Pharmaceuticals S.A.

    发明人： RAMAN, Jayaraman Venkat ,  VAKKALANKA, Swaroop Kumar Venkata Satya

    IPC分类号： C07D311/36 ,  C07D405/06

    摘要： The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives represented by formula (IA) and (IB), processes for preparing the alcohol derivatives and their use in preparing pharmaceuticals.

    摘要翻译： 本发明涉及化合物作为药物中间体是有用的，的制备方法的中间体，在方法中使用的中间体，并在药物的制备中使用的中间体。 特别地，本发明涉及对映体纯OPTIONALLY substituiertem 2-（1-羟基烷基）苯并吡喃-4-酮衍生物由式（IA）和（IB）表示，用于制备在制备药物的醇衍生物和它们的使用 ，