Invention Grant
US09403763B2 CD4-mimetic inhibitors of HIV-1 entry and methods of use thereof
有权
HIV-1进入的CD4-模拟抑制剂及其使用方法
- Patent Title: CD4-mimetic inhibitors of HIV-1 entry and methods of use thereof
- Patent Title (中): HIV-1进入的CD4-模拟抑制剂及其使用方法
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Application No.: US14365389Application Date: 2012-12-14
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Publication No.: US09403763B2Publication Date: 2016-08-02
- Inventor: Joseph Sodroski , Judith M. LaLonde , Amos B. Smith, III , Peter D. Kwong , Young Do Kwon , David M. Jones , Alexander W. Sun , Joel R. Courter , Takahiro Soeta , Toyoharu Kobayashi , Amy M. Princiotto , Xueling Wu , John R. Mascola , Arne Schon , Ernesto Freire , Navid Madani , Matthew Le-Khac , Wayne A. Hendrickson , Jongwoo Park
- Applicant: Dana-Farber Cancer Institute, Inc. , The Trustees of the University of Pennsylvania , The United States of America As Represented By The Secretary, Department of Health and Human Services , Bryn Mawr College , The Johns Hopkins University , The Trustees of Columbia University in the City of New York
- Agency: Baker & Hostetler, LLP
- International Application: PCT/US2012/069708 WO 20121214
- International Announcement: WO2013/090696 WO 20130620
- Main IPC: C07C237/06
- IPC: C07C237/06 ; A61K31/167 ; A61K31/185 ; C07C279/16 ; C07D233/88 ; C07D235/02 ; C07D235/06 ; C07D271/07 ; C07D207/335 ; C07D207/34 ; C07D209/88 ; C07D209/94 ; C07D307/52 ; C07C279/12 ; C07C233/56 ; C07C237/22
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.
Public/Granted literature
- US20140350113A1 CD4-MIMETIC INHIBITORS OF HIV-1 ENTRY AND METHODS OF USE THEREOF Public/Granted day:2014-11-27
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