Bristol-myers Squibb Compnay

Viiv Healthcare UK (no.5) Limited

Lion Bioscience Ag

Shirong Zhu

Samuel Gerritz

Shuhao Shi

Yong-Jin Wu

Annapurna Pendri

Nicholas A Meanwell

John E Macor

Andrew Charles Good

Makonen Belema

David R Langley

Guo Li

Weixu Zhai

John A Bender

Kenneth M Boy

Robert G Gentles

Bradley C Pearce

Zhong Yang

Scott Channing Sutton

Brett R Beno

Lorin A Thompson, Iii

Christopher W Cianci

Yuewu Chen

Amy L Hannah

Sean Kim

Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth: 

Inhibitors of human immunodeficiency virus replication

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

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

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

There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R, R, R, R, R, R, R, and p as 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.

N-aryl pyrrolidine derivatives as beta-secretase inhibitors

There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R, R, R, R, R, R, and Rare as 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.

Oxime-containing acyl guanidines as beta-secretase inhibitors

There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R, 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.

Aminoacetamide acyl guanidines as &#x3b2;-secretase inhibitors

2-aminobenzoxazole derivatives and combinatorial libraries thereof

Growing community of inventors

Cheshire, CT, United States of America

Shirong Zhu