Merck Sharp + Dohme Corp.

Sam Kattar

Joey Lee Methot

Matthew G Stanton

Benito Munoz

Thomas Allen Miller

Christopher J Dinsmore

David James Witter

Kevin J Wilson

Phieng Siliphaivanh

David Joseph Guerin

Jianmin Fu

Norman Kong

Christian Fischer

Mark E Scott

Peter H Fuller

Matthew Christopher

Alexey A Rivkin

Rachel Nicola MacCoss

Jed Hubbs

Chaomin Li

Adam J Schell

Yunfeng Bai

Zhixiang Zheng

Yumei Liu

Sean P Ahearn

William Colby Brown

Danielle F Molinari

Andrew Rosenau

Stephanie M Chichetti

Jiamin Fu

The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds. 

Ethyl N-boc piperidinyl pyrazolo pyridones as Janus kinase inhibitors

According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A&#x3b2;42 and hence are useful in treatment of Alzheimer's disease and related conditions. 

Triazole derivatives for treatment of Alzheimer's disease

The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

Benzothiophene hydroxamic acid derivatives

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Arlington, MA, United States of America

Sam Kattar