The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 02, 2016

Filed:

Dec. 14, 2012
Applicants:

Dana-farber Cancer Institute, Inc., Boston, MA (US);

The Trustees of the University of Pennsylvania, Philadelphia, PA (US);

The United States of America As Represented BY the Secretary, Department of Health and Human Services, Washington, DC (US);

Bryn Mawr College, Bryn Mawr, PA (US);

The Johns Hopkins University, Baltimore, MD (US);

The Trustees of Columbia University IN the City of New York, New York, NY (US);

Inventors:

Joseph Sodroski, Medford, MA (US);

Judith M. LaLonde, Havertown, PA (US);

Amos B. Smith, III, Merion, PA (US);

Peter D. Kwong, Washington, DC (US);

Young Do Kwon, Kensington, MD (US);

David M. Jones, Philadelphia, PA (US);

Alexander W. Sun, Eugene, OR (US);

Joel R. Courter, Philadelphia, PA (US);

Takahiro Soeta, Kanazawa, JP;

Toyoharu Kobayashi, Tokyo, JP;

Amy M. Princiotto, Attleboro, MA (US);

Xueling Wu, Potomac, MD (US);

John R. Mascola, Rockville, MD (US);

Arne Schon, Baltimore, MD (US);

Ernesto Freire, Baltimore, MD (US);

Navid Madani, Westboro, MA (US);

Matthew Le-Khac, Brooklyn, NY (US);

Wayne A. Hendrickson, New York, NY (US);

Jongwoo Park, Daejeon, KR;

Assignee:

Other;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C 237/06 (2006.01); A61K 31/167 (2006.01); A61K 31/185 (2006.01); C07C 279/16 (2006.01); C07D 233/88 (2006.01); C07D 235/02 (2006.01); C07D 235/06 (2006.01); C07D 271/07 (2006.01); C07D 207/335 (2006.01); C07D 207/34 (2006.01); C07D 209/88 (2006.01); C07D 209/94 (2006.01); C07D 307/52 (2006.01); C07C 279/12 (2006.01); C07C 233/56 (2006.01); C07C 237/22 (2006.01);
U.S. Cl.
CPC ...
C07C 279/16 (2013.01); C07C 233/56 (2013.01); C07C 237/06 (2013.01); C07C 237/22 (2013.01); C07C 279/12 (2013.01); C07D 207/335 (2013.01); C07D 207/34 (2013.01); C07D 209/88 (2013.01); C07D 209/94 (2013.01); C07D 233/88 (2013.01); C07D 235/02 (2013.01); C07D 235/06 (2013.01); C07D 271/07 (2013.01); C07D 307/52 (2013.01); A61K 31/167 (2013.01); A61K 31/185 (2013.01); C07C 2101/14 (2013.01); C07C 2102/08 (2013.01);
Abstract

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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