Hong Tao Lu

US Patent:

8309602, Nov 13, 2012

Filed:

Oct 7, 2008

Appl. No.:

12/682513

Inventors:

Lan Xie - Beijing, CN
Bingjie Qin - Beijing, CN
Kuo-Hsiung Lee - Chapel Hill NC, US
Shibo Jiang - Fresh Meadows NY, US
Hong Lu - Bayside NY, US

Assignee:

Institute of Pharmacology and Toxicology - Beijing
Academy of Military Medical Sciences P.L.A. China - Beijing

International Classification:

A61K 31/277
A61K 31/136
C07C 255/50
C07C 255/51
C07C 211/46

US Classification:

514524, 514525, 514658, 558418, 558420, 564441

Abstract:

The present invention relates to multi-substituted m-diarylanilines or pharmaceutically acceptable salts thereof, wherein X, R-Rare as defined in the claims, their preparation process, pharmaceutical compositions comprising them and their use for the manufacture of a medicament for anti-HIV.

US Patent:

20060287319, Dec 21, 2006

Filed:

Jun 6, 2006

Appl. No.:

11/448439

Inventors:

Shibo Jiang - Fresh Meadows NY, US
Asim Debnath - Fort Lee NJ, US
Hong Lu - Bayside NY, US

International Classification:

A61K 31/53
A61K 31/501
A61K 31/497
A61K 31/496
A61K 31/4439
A61K 31/427

US Classification:

514241000, 514252130, 514255050, 514252020, 514252050, 514369000, 514253090, 514341000, 514342000

Abstract:

A group of compounds that inhibit HIV replication by blocking HIV entry was identified. One representative compound, designated NB-206, and its analogs inhibited HIV replication (p24 production) with ICvalues at nanomolar levels. It was proved that NB-206 and its analogs are HIV entry inhibitors by targeting the HIV gp41 since: 1) they inhibited HIV-mediated cell fusion; 2) they inhibited HIV replication only when they were added to the cells less than one hour after virus addition; 3) they blocked the formation of the gp41 core that is detected by sandwich enzyme linked immunosorbent assay (ELISA) using a conformation-specific MAb NC-1; and 4) they inhibited the formation of the gp41 six-helix bundle revealed by fluorescence native-polyacrylamide gel electrophoresis (FN-PAGE). These results suggested that NB-206 and its analogs may interact with the hydrophobic cavity and block the formation of the fusion-active gp41 coiled coil domain, resulting in inhibition of HIV-1 mediated membrane fusion and virus entry.

US Patent:

20120053213, Mar 1, 2012

Filed:

Sep 28, 2009

Appl. No.:

13/123494

Inventors:

Lan Xie - Beijing, CN
Xingtao Tian - Beijing, CN
Kuo-Hsiung Lee - Chapel Hill NC, US
Shibo Jiang - Shanghai, CN
Hong Lu - Bayside NY, US

Assignee:

INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA - Beijing

International Classification:

A61K 31/4412
A61P 31/18
C07D 213/74

US Classification:

514349, 546297

Abstract:

The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, R, Rand X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.