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    CYTOTOXIC-DRUG DELIVERING MOLECULES TARGETING HIV (CDM-HS), CYTOTOXIC ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS AND METHODS OF USE
    1.
    发明公开
    CYTOTOXIC-DRUG DELIVERING MOLECULES TARGETING HIV (CDM-HS), CYTOTOXIC ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS AND METHODS OF USE 审中-公开
    针对HIV-LOOKING细胞毒性物质释放分子（CDM HS）细胞毒性作用抗人免疫缺陷病毒及使用该方法

    公开(公告)号：EP2841107A1

    公开(公告)日：2015-03-04

    申请号：EP13780662.6

    申请日：2013-03-15

    申请人： Yale University

    发明人： SPIEGEL, David ,  PARKER, Christopher

    IPC分类号： A61K47/22 ,  C07D407/14 ,  C07D471/04 ,  A61K31/496 ,  A61P25/00

    CPC分类号： C07H15/26 ,  A61K31/67 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/706 ,  A61K45/06 ,  A61K47/55 ,  A61K47/60 ,  C07D405/14 ,  A61K2300/00

    摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as CDM-Hs, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by introducing cytotoxic moieties to gp120-expressing cells, thereby causing cell death and preventing cell infection and spread of HIV. It is shown that CDM-Hs bind to gp120 and gp-120 expressing cells competitively with CD4, and these compounds cause cell death of HIV-infected cells, thereby decreasing viral infectivity. Compounds and methods are described herein.

    摘要翻译： 本发明涉及新的双官能化合物和方法用于治疗HIV感染。 由被称为CDM Hs为双功能的小分子，基因反弹，通过正交通路中起作用，通过抑制所述的gp120-CD4相互作用，并通过引入细胞毒性部分至gp120的表达细胞，从而引起细胞死亡和防止细胞感染和HIV的传播。 它被示做CDM HS结合gp120和gp120的表达细胞竞争性CD4，和合成的化合物引起的HIV感染细胞的细胞死亡，从而降低病毒感染性。 化合物和方法被描述英寸

    BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS
    2.
    发明公开
    BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS 审中-公开
    与针对人免疫缺陷病毒ANTIKÖRPERREKRUTIERENDER和条目锁定活性的双功能分子

    公开(公告)号：EP2640720A2

    公开(公告)日：2013-09-25

    申请号：EP11842404.3

    申请日：2011-11-17

    申请人： Yale University, Inc.

    发明人： SPIEGEL, David ,  PARKER, Christopher

    IPC分类号： C07D405/14 ,  A61K31/496 ,  A61P31/18

    CPC分类号： C07D405/14 ,  A61K9/0014 ,  A61K31/496 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM- HI's, function through orthogonal pathways, by inhibiting the gpl20-CD4 interaction, and by recruiting anti-DNP antibodies to gpl20-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gpl20 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gpl20-expressing cells. Compounds and methods are described herein.

    THE TOTAL SYNTHESIS OF GLUCOSEPANE AND COMPOUNDS OBTAINED THEREFROM
    9.
    发明公开
    THE TOTAL SYNTHESIS OF GLUCOSEPANE AND COMPOUNDS OBTAINED THEREFROM 审中-公开

    公开(公告)号：EP3353153A1

    公开(公告)日：2018-08-01

    申请号：EP16849738.6

    申请日：2016-09-23

    申请人： Yale University

    发明人： SPIEGEL, David

    IPC分类号： C07D223/14 ,  C07C281/16

    CPC分类号： C07D491/048 ,  A61K31/55 ,  A61K45/06 ,  C07C281/16 ,  C07D487/04

    摘要： Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Research in humans suggests that glucosepane plays a critical role in the pathophysiology of both diabetes and human aging; yet comprehensive biological investigations of this ‘metabolite have been’ greatly hindered by a scarcity of chemically homogeneous material available for study. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole (hereafter termed an “iso-imidazole”), rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane, enabled by the development of a novel one-pot method for preparation of the iso-imidazole core. The synthesis of the present invention is concise (8-steps starting from commercial materials), convergent, high-yielding (12% overall), and enantioselective. These results should prove useful to the art and practice of heterocyclic chemistry, and critical for the study of glucosepane and its role in human health and disease, especially the treatment of diabetic disorders or its impact on aging processes. Methods of synthesis, compounds obtained therefrom, pharmaceutical compositions and methods of treatment provide embodiments of the present invention.