Schering Corporation

Medivation Technologies, Inc.

Axys Pharmaceuticals, Inc.

Leland Stanford Junior University

Myoforte Therapeutics, Inc.

Other

Merck Sharp + Dohme Corp.

Merck Frosst Canada, Inc.

Merck Canada Inc.

Schering-plough Corporation

Virobay, Inc.

Lion Bioscience Ag

Auransa Inc.

Capulus Therapeutics, LLC

Michael J Green

John J Piwinski

Jesse K Wong

Ashit K Ganguly

Sarvajit Chakravarty

Neng-Yang Shih

Theodros Asberom

Derek B Lowe

Joseph A Kozlowski

Sundeep Dugar

Samuel Chackalamannil

John W Clader

Stuart W McCombie

Wayne D Vaccaro

Andrew Asher Protter

Joel G Berger

Margaret H Sherlock

Ho-Jane Shue

Wei K Chang

Wing C Tom

Susan F Vice

Allen Barnett

Robert D McQuade

Margaret E Browne

Lian-Yong Chen

Rajendra Parasmal Jain

Jayaram R Tagat

Anil K Saksena

Roopa Rai

Frank J Villani

Wang Yuguang

Cheuk K Lau

Michel Therien

Jacques Yves Gauthier

Serge Leger

Cameron Black

Chun Sing Li

Bernard Hirschbein

James T Palmer

Christophe Mellon

Chitra Baskaran

Dan McKay

Vouy-Linh Truong

James William Janc

Robert G Aslanian

Craig D Boyle

Alam Jahangir

Pietro Mangiaracina

Richard J Friary

Christopher I Bayly

Yuguang Wang

William Kreutner

Barry Patrick Hart

Vera A Seidl

Mehrdad Shamloo

Robert Booth

David J Blythin

Daniel M Solomon

Son Minh Pham

Timothy L McAllister

Richard W Draper

Chou-Hong Tann

Andrew T Lupo

John S Chiu

Gregory R Luedtke

Timothy Gahman

Junning Lee

Pek Yee Lum

Cesar Colon

Michael C Griffith

Kevin Ross Holme

Elliot L Shapiro

Amantullah Ansari

Charles J Casmer

Andrew Lupo, Jr

Tina M Cowan

T K Thiruvengadam

Karen J Watson-Straughan

Bitna Yi

Ming Qi

Hak Jin Chang

Christa Hamashin

Jeffrey Cramer

Michael Standen

Robert Tiberi

Bernard Katchen

Gregory M Enns

Rolando E Yanes

Tereza Moore

Margaret A Gentles

Satish C Bisarya

Andrew Kelley Evans

Javaram R Tagat

James E Macdonald

Jeff Dener

Oldrich Kocian

Dan Mckay

James W Janc

Methods of treatment and pharmaceutical formulations configured to treat primary and secondary mitochondrial dysfunction are provided. The methods and treatments use an agonist of AMPK. The agonist activates AMPK to activate ATP-producing pathways and inhibiting ATP-consuming pathways, thus allowing for the alleviation of symptoms associated with mitochondrial dysfunctions.

Methods and formulations to treat mitochondrial dysfunction

Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.

PGDH inhibitors and methods of making and using

Provided herein are compounds comprising a three-ring core, such as compounds of Formula (X), Formula (X-A), Formula (X-Ai), Formula (X-B), Formula (X-Bi), Formula (Z), Formula (Z-A), Formula (Z-Ai), Formula (Z-B), Formula (Z-Bi), Formula (I), Formula (I-A), Formula (I-Ai), Formula (I-B), and Formula (I-Bi), and pharmaceutically acceptable salts, solvates, tautomers, isotopes, or isomers thereof. Also provided herein are methods of inhibiting a component of the sterol regulatory element binding protein (SREBP) pathway, such as an SREBP or SREBP cleavage activating protein (SCAP), using these compounds, or pharmaceutically acceptable salts, solvates, tautomers, isotopes, or isomers thereof. Further provided are methods of treating a disorder in a subject in need thereof, such as liver disease, non-alcoholic steatohepatitis, insulin resistance, or cancer.

SREBP inhibitors comprising a 6-membered central ring

The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer.

Derivatives of piperlongumine and uses thereof

Adrenergic receptor modulating compounds and methods of using the same are provided. Also provided are methods of treating a subject for a disease or condition associated with an adrenergic receptor including administering a therapeutically effective amount of the subject compound. Aspects of the disclosure include a method of modulating an inflammatory pathway in a cell, such as the production of TNF-alpha in the cell. The method can include contacting a cell with &#x3b2;1-selective adrenergic receptor modulating compound to selectively activate a cAMP pathway over a beta-arrestin pathway in the cell. Pharmaceutical compositions and kits which include the subject compounds are provided.

Adrenergic receptor modulating compounds and methods of using the same

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor &#x3b1;. The compounds may also bind to and are an antagonist of the adrenergic receptor &#x3b1;; or the compounds are not antagonists of the adrenergic receptor &#x3b1;and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

Compounds and methods for treating diabetes

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor &#x3b1;antagonists. The compounds may also bind to and antagonize adrenergic receptor &#x3b1;. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Compounds and methods for treatment of hypertension

Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. Fused pyrimidine compounds that are inhibitors of Trk receptors (e.g., Trk A, Trk B and Trk C) are provided also. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.

Fused pyrimidine compounds and use thereof

The present invention provides fused pyrimidine compounds of the general Formula (I): or a salt thereof, wherein the variables are as defined in the specification. Fused pyrimidine compounds of the general Formula (I) are provided as kinase inhibitors, such as multi-kinase inhibitors. In one aspect, fused pyrimidine compounds of the general Formula (I) are provided as IGF-IR inhibitors. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compounds of the general Formula (I) and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound of the general Formula (I) or salt thereof and instructions for use, e.g., in a method of treating cancer.

Compounds and methods of treating diabetes

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Cathepsin cysteine protease inhibitors

The present invention relates to a process for the preparation of alkyl esters of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid, which are intermediates useful in the synthesis of (S)&#x2014;N-(1-cyanocyclopropyl)-5-cyclopropyl-4,4-difluoro-2-((S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethylamino)pentanamide and related compounds, which are compounds that are cysteine protease inhibitors.

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Skillman, NJ, United States of America

Michael J Green