Aza-quinolinol phosphonate integrase inhibitor compounds

a technology of aza-quinolinol and integrase, which is applied in the direction of antiinfective drugs, group 5/15 element organic compounds, drug compositions, etc., can solve the problems of inability to inhibit the hiv infection and related diseases, limited usefulness of resistant strains, and inability to fully integrate inhibitory complexes,
US20070185007A1Inactive Publication Date: 2007-08-09JIN HAOLUN +2
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
JIN HAOLUN
Publication Date
2007-08-09
Estimated Expiration
Not applicable · inactive patent

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Abstract

Aza-quinolinol phosphonate compounds and methods for inhibition of HIV-integrase are disclosed. Formula (I). Ar is aryl or heteroaryl connecting R6 to L. L is a bond or a linker connecting a ring atom of Ar to N. The ring atoms, X1-X5 may be N, substituted nitrogen, or substituted carbon, and form rings. The compounds include at least one phosphonate group covalently attached at any site.
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Description

FIELD OF THE INVENTION

[0001] The invention relates generally to compounds with antiviral activity and more specifically with HIV-integrase inhibitory properties. BACKGROUND OF THE INVENTION

[0002] Human immunodeficiency virus (HIV) infection and related diseases are a major public health problem worldwide. A virally encoded integrase protein mediates specific incorporation and integration of viral DNA into the host genome. Integration is essential for viral replication. Accordingly, inhibition of HIV integrase is an important therapeutic pursuit for treatment of HIV infection and related diseases.

[0003] Human immunodeficiency virus type 1 (HIV-1) encodes three enzymes which are required for viral replication: reverse transcriptase, protease, and integrase. Although drugs targeting reverse transcriptase and protease are in wide use and have shown effectiveness, particularly when employed in combination, toxicity and development of resistant strains have limited their usefulness (Pa...

Claims

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