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    Crystalline forms of aliskiren hemifumarate
    3.
    发明授权
    Crystalline forms of aliskiren hemifumarate 失效
    结晶形式的阿利吉仑半富马酸盐

    公开(公告)号：US08119841B2

    公开(公告)日：2012-02-21

    申请号：US12312320

    申请日：2007-11-05

    申请人： Frank Stowasser ,  Stephanie Monnier

    发明人： Frank Stowasser ,  Stephanie Monnier

    IPC分类号： C07C237/14 ,  A61K31/16

    CPC分类号： C07C237/22

    摘要： This invention relates to crystal forms of aliskiren hemifumarate and various embodiments related thereto, e.g. pharmaceutical preparations, processes for the manufacture of the crystal forms, pharmaceuticals uses and the like. The crystal forms have particularly advantageous properties e.g. they are useful in the manufacture of blood-pressure lowering pharmaceutical preparations and the like.

    摘要翻译： 本发明涉及阿利吉仑半富马酸盐的晶体形式及其相关的各种实施方案，例如， 药物制剂，晶型的制造方法，药物用途等。 晶体形式具有特别有利的特性，例如 它们可用于制造降血压药物制剂等。

    NOVEL ADAMANTYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND USE THEREOF
    9.
    发明公开
    NOVEL ADAMANTYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND USE THEREOF 审中-公开

    公开(公告)号：US20240158352A1

    公开(公告)日：2024-05-16

    申请号：US18547822

    申请日：2022-02-25

    申请人： CAN-Therapy Inc.

    发明人： Hyun Seock SHIN ,  Kee Dal NAM

    IPC分类号： C07D211/60 ,  A61P35/00 ,  C07C237/14

    CPC分类号： C07D211/60 ,  A61P35/00 ,  C07C237/14

    摘要： The present disclosure relates to a novel adamantyl derivative or a pharmaceutically acceptable salt thereof, and a use thereof. The adamantyl derivative may be a dipeptidyl peptidase-4 (DPP4) inhibitor and may be utilized in the prevention or treatment of cancer, rheumatoid arthritis, Parkinson's disease, autoimmune diseases, skin diseases, non-alcoholic steatohepatitis, aortic valve contraction, cerebrovascular diseases, or the like. In particular, the adamantyl derivative suppresses DPP4 in a tumor microenvironment (TME) and guides T cells to tumor tissues, thereby killing cancer cells, and thus can be effectively used for preventing or treating cancer or inhibiting cancer metastasis. The cancer may be prostate cancer, thyroid cancer, kidney cancer, carcinoma, endometrial cancer, lung cancer, urinary epithelial cancer, colorectal cancer, breast cancer, rectal cancer, cervical cancer, glioma, colon cancer, head and neck cancer, stomach cancer, liver cancer, pancreatic cancer, testicular cancer, ovarian cancer, blood cancer, skin cancer, brain tumor, etc.

    PROCESS FOR THE PREPARATION OF ALPHA-ACYLOXY BETA-FORMAMIDO AMIDES
    10.
    发明申请
    PROCESS FOR THE PREPARATION OF ALPHA-ACYLOXY BETA-FORMAMIDO AMIDES 审中-公开
    制备α-氨基-β-甲酰胺类氨基酸的方法

    公开(公告)号：US20140213788A1

    公开(公告)日：2014-07-31

    申请号：US14228978

    申请日：2014-03-28

    申请人： Eelco RUIJTER ,  Romano ORRU ,  Anass ZNABET ,  Marloes POLAK ,  Nicholas TURNER

    发明人： Eelco RUIJTER ,  Romano ORRU ,  Anass ZNABET ,  Marloes POLAK ,  Nicholas TURNER

    IPC分类号： C07C291/10 ,  C07D209/52 ,  C07D403/12 ,  C07C237/14 ,  C07C231/06

    CPC分类号： C07C291/10 ,  C07C231/06 ,  C07C237/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07D209/52 ,  C07D209/58 ,  C07D209/94 ,  C07D241/24 ,  C07D403/06 ,  C07D403/12

    摘要： The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.

    摘要翻译： 本发明涉及制备通式（I）化合物的方法，包括：a）使通式（II）的化合物与式III的化合物R 2 COOH和通式 IV R3NC在这样的条件下形成化合物I，其中R 1表示取代或未取代的烷基，烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 2表示取代或未取代的烷基 烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 3表示取代或未取代的烷基，烯基或炔基结构。 在另一方面，本发明涉及所获得的产物作为各种肽模拟物的中间体的用途，优选作为脯氨酰二肽结构的会聚合成中的结构单元。