Bristol-myers Squibb Compnay

California Institute of Technology

University of Kansas

Cleave Biosciences, Inc.

Samuel Gerritz

Annapurna Pendri

Shirong Zhu

Shuhao Shi

Weixu Zhai

Chongqing Sun

Guo Li

William R Ewing

Natesan Murugesan

Bruce A Ellsworth

Yanting Huang

Paul Michael Scola

Tao Wang

Zhongxing Zhang

Li-Qiang Sun

Eric Mull

Doree F Sitkoff

Zhengxiang Gu

David R Langley

Yong-Jin Wu

Richard B Sulsky

Philip Michael Sher

Qian Zhao

Guixue Yu

Amarendra B Mikkilineni

Ximao Wu

Ying Wang

Nicholas A Meanwell

John E Macor

Andrew Charles Good

B Narasimhulu Naidu

Joseph Anthony Tino

Dharmpal S Dodd

Zhiwei Yin

Han-Jie Zhou

Manoj Patel

Kenneth M Boy

Stanley V D'Andrea

Kevin M Peese

Jeffrey Aube

Frank John Schoenen

Gang Wu

Bradley C Pearce

George L Trainor

Lorin A Thompson, Iii

Zhongyu Wang

Raymond J Deshaies

Kevin Frankowski

Chong-qing Sun

Christopher W Cianci

Kelin Li

Tsui-Fen Chou

Charles John Andres, Jr

Stephen R Johnson

Sean Kim

The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. 

Inhibitors of human immunodeficiency virus replication

Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.

Methods and compositions for inhibition of the transitional endoplasmic reticulum ATPase

The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. 

Compounds for the treatment of hepatitis C

A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with &#x2014;N, &#x2014;O, or &#x2014;S adjacent to the &#x2014;Ar substituent or adjacent to the point of attachment for the &#x2014;Ar substituent;Ar is aryl or heteroaryl;R is &#x2014;CH, &#x2014;CHF, or &#x2014;CH&#x2550;CH;W is &#x2014;NO, &#x2014;Cl, &#x2014;Br, &#x2014;CHO, &#x2014;CH&#x2550;CH, or &#x2014;CN;X is &#x2014;Cl, &#x2014;CH, or &#x2014;CN;Y is &#x2014;CH or &#x2014;N; andZ is C-Calkyl, C-Ccycloalkyl, substituted aryl, substituted heteroaryl, OR, or NHR, wherein Ris selected from the group of H, aryl, heteroaryl, C-Calkyl and C-Ccycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.

Piperazine analogs as broad-spectrum influenza antivirals

The invention provides for compounds of formula I  Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.

Tetrahydroquinoline derivatives as cannabinoid receptor modulators

The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I. including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R, R, R, R, R, m and n are described herein.

Azabicyclic heterocycles as cannabinoid receptor modulators

There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R, R, R, R, R, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Macrocyclic acyl guanidines as beta-secretase inhibitors

The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R, R, R, n, and Z are described herein.

Tetrahydroquinoline cannabinoid receptor modulators

There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R, R, R, R, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Oxime-containing macrocyclic acyl guanidines as &#x3b2;-secretase inhibitors

There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R, R, Rand Ras defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Acyl guanidines as beta-secretase inhibitors

The present application describes compounds according to Formula I, wherein A, B, E, R, R, R, R, Y and Z are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents. Finally, the present application describes methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. 

Pyrazole derivatives as cannabinoid receptor modulators

Growing community of inventors

Guilford, CT, United States of America

Samuel Gerritz