Purdue Research Foundation

Yamasa Corporation

Kumamoto University

National Institutes of Health, a Component of the US Dept. of Health & Human Services

University of Illinois

Ono Pharmaceuticals Co., Ltd.

Hiroaki Mitsuya

National University Corporation Kumamoto University

National University Corporation of Kumamoto University

Arun K Ghosh

Hiroshi Ohrui

Satoru Kohgo

Eiichi Kodama

Masao Matsuoka

John W Erickson

Sergei V Gulnik

Bruno D Chapsal

Haruhiko Machida

Shiro Shigeta

Garth L Parham

Cuthbert D Martyr

Prasanth Reddy Nyalapatla

Chun-Xiao Xu

Shiro Shibayama

Yoshikazu Takaoka

Andrew Mesecar

Margherita Brindisi

Kenji Kitano

Jianfeng Li

Yasuhiro Koh

Venkateswara Rao Kalapala

Kenji Maeda

Arun E Ghosh

Dana Shahabi

Sofiya Yashchuk

Satish Kovela

Sean Fyvie

Venkateswararao Kalapala

Venkateswara Kalapala Rao

Compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof are disclosed. The compounds HIV-protease and, as a result, are useful in the treatment of HIV infection.

HIV-1 protease inhibitors and uses thereof

Bis-amide inhibitors of SARS-CoV-2 (COVID); pharmaceutical compositions comprising same; and methods of treating a severe acute respiratory syndrome.

Compounds for the treatment of SARS

Various embodiments relate to a compound of the formula (I) and (II), wherein X, X, X, X, and R-Rare defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and/or (II) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I) and/or (II), or a pharmaceutical composition comprising compounds of the formula (I) and/or (II), to a patient in need thereof.

Tricyclic P2-ligand containing potent HIV-protease inhibitors against HIV/AIDS

Described herein are compounds of the formulae (I), (Ia), (Ib), and (II) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods of making and using compounds of the formulae (I), (Ia), (Ib), and (II) to, among other things, treat HIV/AIDS.

Macrocyclic HIV-1 protease inhibitors and uses thereof

Various embodiments relate to a compound of the formula (I): wherein X, X, R&#x2014;Rand Rare defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I), or a pharmaceutical compositions comprising compounds of the formula (I), to a patient in need thereof. 

The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy. The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of formulas (A), (B), (C) or (D); R, R, R, Ror Ris H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH, O, S, SO, SO, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO; m is from 0 to 6; Ris OH, &#x2550;O (keto), NH, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO. Optionally, Rand R, together with the N&#x2014;W bond of formula (I), comprise a macrocyclic ring. 

Fitness assay and associated methods

Described herein are compounds and compositions that are useful in the treatment of HIV, AIDS, and AIDS-related diseases. In addition, compounds are described herein that are capable of inhibiting the dimerization of HIV proteases.

Methods and compositions for treating HIV infections

Various embodiments of the present invention are directed to compounds of the formula (I) or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof, wherein X, X, X, R, R, R, and n are defined herein. These compounds are useful as inhibitors of HIV-1 protease and, as a result, are useful in the treatment of HIV infection. 

Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.

Compounds and methods for treating HIV

Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described.

Fused tricyclic ether carbamates and their use

Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.

HIV-1 protease inhibitors having gem-di-fluoro bicyclic P2-ligands

C3-functionalized-cyclopentanyltetrahydrofuranyl carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are described. Compositions comprising the disclosed compound and methods of using the compounds and/or compositions for treating patients infected with HIV are also described.

C-3 substituted bicyclooctane based HIV protease inhibitors

Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.

Growing community of inventors

Kumamoto, Japan

Hiroaki Mitsuya