- 专利标题: BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS
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申请号: US16037678申请日: 2018-07-17
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公开(公告)号: US20190002447A1公开(公告)日: 2019-01-03
- 发明人: David Spiegel , Christopher Parker
- 申请人: YALE UNIVERSITY
- 主分类号: C07D405/14
- IPC分类号: C07D405/14 ; A61K9/00 ; A61K45/06 ; A61K31/496
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 gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 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 gp120-expressing cells. Compounds and methods are described herein.