Invention Grant
US09562038B2 Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus
有权
具有针对人类免疫缺陷病毒的抗体募集和进入抑制活性的双功能分子
- Patent Title: Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus
- Patent Title (中): 具有针对人类免疫缺陷病毒的抗体募集和进入抑制活性的双功能分子
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Application No.: US13988251Application Date: 2011-11-17
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Publication No.: US09562038B2Publication Date: 2017-02-07
- Inventor: David Spiegel , Christopher Parker
- Applicant: David Spiegel , Christopher Parker
- Applicant Address: US CT New Haven
- Assignee: YALE UNIVERSITY
- Current Assignee: YALE UNIVERSITY
- Current Assignee Address: US CT New Haven
- Agent Henry D. Coleman; R. Neil Sudol
- International Application: PCT/US2011/061174 WO 20111117
- International Announcement: WO2012/068366 WO 20120524
- Main IPC: C07D405/14
- IPC: C07D405/14 ; A61K31/496 ; A61K45/06

Abstract:
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.
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