IP Library Granted Patent US 8,299,093
Granted Patent B2
US 8,299,093 · App. 12/536,738 · Granted Oct 30, 2012

Small molecule inhibitors of retroviral assembly and maturation

Assignee: New York Blood Center, Inc.
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Quick Facts
Patent No.
US 8,299,093
App. No.
12/536,738
Granted
Oct 30, 2012
Kind
B2
Abstract

Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection.

Claims (13)

1. A method for disrupting HIV assembly and replication comprising:

administering to a patient in need thereof a pharmaceutical composition comprising a pharmaceutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof,

wherein R 1 is substituted or unsubstituted phenyl, or substituted or unsubstituted furanyl;

R 2 is substituted or unsubstituted benzyl, or substituted or unsubstituted alkyl furanyl;

R 3 is a moiety selected from the group consisting of H, and substituted or unsubstituted (C 1-6 )alkyl;

Z is C═O or C═S; and

T, U, V, W and X are independently selected from CR 4 or N, wherein R 4 is a moiety selected from the group consisting of hydrogen, substituted or unsubstituted (C 1-6 )alkyl, substituted or unsubstituted (C 1-6 )alkoxy, hydroxyl alkyl, Cl, Br, and F;

disrupting HIV assembly and replication.

2. The method of claim 1 , further comprising administering at least one additional therapeutic agent selected from the group consisting of reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, integrase inhibitors, chemokine receptor (CXCR4, CCR5) inhibitors, interleukin-2, hydroxyurea, monoclonal antibodies, and cytokines.

3. The method of claim 1 , wherein said compound is selected from the group consisting of:

4. The method of claim 1 , wherein said compound has the structure:

5. The method of claim 1 , wherein said composition further comprises at least one pharmaceutically acceptable excipient.

6. The method of claim 1 , wherein said composition further comprises at least one additional therapeutically active agent.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jul 12, 2017
From: NEW YORK BLOOD CENTER
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 043162/0778 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 4, 2009
From: DEBNATH, ASIM KUMAR; ZHANG, HONGTAO; CURRELI, FRANCESCA
To: NEW YORK BLOOD CENTER
Reel/Frame 023197/0096 →
Continuity (2)
Provisional Application 61087574 · Aug 8, 2008
Related Publication 20100035912A1 · Feb 11, 2010