Merck Sharp + Dohme Corp.

Novartis Ag

Other

Alexey A Rivkin

Xiaolin Li

Peichao Lu

Zachary Kevin Sweeney

Benito Munoz

Christopher J Dinsmore

David James Witter

Jiping Fu

Joon Jung

Christian Fischer

Matthew Christopher

Aregahegn Yifru

Meiliana Tjandra

Hua Zhou

Philip Jones

Haiying He

Javier De Vicente Fidalgo

Joey Lee Methot

David Joseph Guerin

Sean P Ahearn

Wosenu Mergo

Subramanian Karur

Andrew Weiss

Stephanie M Chichetti

Mark E Scott

John W Butcher

Cheng Hu

Zhigan Jiang

Qinglin Pu

Xiaojing Michael Wang

Daniel Mutnick

Brandon D Cash

Rachel Nicola MacCoss

Adam J Schell

June J Kim

Hyun Chong Woo

Chaomin Li

Folkert Reck

Jianhua Xia

William Colby Brown

Yongjin Xu

Sam Kattar

Andrew Rosenau

John T Hendrix

Colin Keith Skepper

Raksha Archarya

John Hendrix

This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.

Quinolone derivatives as antibacterials

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R, R, R, R, R, and A-B are as defined herein, which are non-immunosuppressive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.

Cyclic peptides and use as medicines

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.

Azaindoles as Janus kinase inhibitors

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein the variables R, R, R, R, R, and A-B are defined herein, which are non-immunosuppresive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.

The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

Pyrrolopyrimidines as janus kinase inhibitors

The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.

Pyrimidine derivatives for treatment of alzheimer's disease

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

Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain. 

Piperidine derivatives

The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.

Therapeutic agents

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Boston, MA, United States of America

Alexey A Rivkin