Invention Grant
- Patent Title: Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus
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Application No.: US16037678Application Date: 2018-07-17
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Publication No.: US10703743B2Publication Date: 2020-07-07
- Inventor: David Spiegel , Christopher Parker
- Applicant: YALE UNIVERSITY
- 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
- Main IPC: C07D405/14
- IPC: C07D405/14 ; A61K31/496 ; A61K45/06 ; A61K9/00

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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