CD4-mimetic inhibitors of HIV-1 entry and methods of use thereof

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United States of America Patent

PATENT NO 9403763
APP PUB NO 20140350113A1
SERIAL NO

14365389

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Abstract

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Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.

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Patent Owner(s)

Patent OwnerAddress
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK535 WEST 116TH STREET 412 LOW MEMORIAL LIBRARY NEW YORK NY 10027

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Courter, Joel R Philadelphia, US 17 410
Freire, Ernesto Baltimore, US 25 87
Hendrickson, Wayne A New York, US 11 30
Jones, David M Philadelphia, US 76 897
Kobayashi, Toyoharu Tokyo, JP 1 4
Kwon, Young Do Kensington, US 65 1270
Kwong, Peter D Washington, US 48 271
LaLonde, Judith M Havertown, US 4 5
Le-Khac, Matthew Brooklyn, US 3 5
Madani, Navid Westboro, US 4 11
Mascola, John R Rockville, US 32 85
Park, Jongwoo Daejeon, KR 61 167
Princiotto, Amy M Attleboro, US 4 5
Schon, Arne Baltimore, US 5 11
Smith,, III Amos B Merion, US 32 95
Sodroski, Joseph Medford, US 19 82
Soeta, Takahiro Kanazawa, JP 2 10
Sun, Alexander W Eugene, US 5 6
Wu, Xueling Potomac, US 14 82

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