Bristol-myers Squibb Compnay

Shuhao Shi

Samuel Gerritz

Yong-Jin Wu

John E Macor

Andrew Charles Good

David R Langley

Shirong Zhu

Weixu Zhai

Annapurna Pendri

Kenneth M Boy

Bradley C Pearce

Lorin A Thompson, Iii

Guo Li

Christopher W Cianci

Sean Kim

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.

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Madison, CT, United States of America

Shuhao Shi