# US 8,541,415 B2 · Targeting an HIV-1 nef-host cell kinase complex

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 8,541,415 B2
- Document ID: US8541415B2
- Status: Granted
- Kind: B2
- Application number: 12/988,501
- Filed: 2009-05-14
- Published: 2011-08-04
- Granted: 2013-09-24
- Earliest claimed: 2008-05-14
- Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education
- Applicants: Lori Emert-Sedlak; Toshiaki Kodama; Billy W. Day; Weixiang Dai; Ronald P. Trible; Thomas E. Smithgall
- Inventors: Lori Emert-Sedlak; Toshiaki Kodama; Billy W. Day; Weixiang Dai; Ronald P. Trible; Thomas E. Smithgall
- Web page: https://patentgrep.com/patent/US8541415B2

## CPC

- C07D 491/048: the oxygen-containing ring being five-membered
- A61P 31/18: for HIV
- C07D 241/44: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 491/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

## Claims

### Claim 1

A method for treating HIV-1 in a subject in need thereof, comprising (a) identifying a subject infected with HIV-1 and then (b) administering to said subject a therapeutic dose of a Formula I compound
wherein
Cy1 is selected from the group consisting of aryl and heteroaryl, wherein the aryl or heteroaryl group is optionally substituted with one or more members selected from the group consisting of —OH, chloroacetyl halogen, sulfonic acid, nitro and —O-alkyl;
Cy2 is an aryl optionally substituted with one or more members selected from the group consisting of halogen, alkyl, amino and —O-alkyl;
R5, R6, R7, and R8 are independently selected from the group consisting of hydrogen and —OR11, and
R11 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said compound is selected from the group consisting of

### Claim 3 (depends on 1)

The method according to claim 1, wherein Cy1 is selected from the group consisting of
and
X is a halogen.

### Claim 4 (depends on 3)

The method according to claim 3, wherein X is chlorine.

### Claim 5 (depends on 1)

The method according to claim 1, wherein Cy1 is