Merck Sharp + Dohme Corp.

Panmira Pharmaceuticals, LLC

Merck + Co., Inc.

Amira Pharmaceuticals, Inc.

Yiwei Li

John Howard Hutchinson

Mark T Bilodeau

Jeannie M Arruda

Jun Liang

Nicholas Simon Stock

Brian Andrew Stearns

Mustapha Haddach

Peter J Manley

Petpiboon Peppi Prasit

Mark Moran

Jillian Frances Evans

John C Hartnett

Mark E Layton

Jeffrey Roger Roppe

Tony Siu

Nicholas D P Cosford

Essa H Hu

Kevin J Rodzinak

Jasmine Eleanor Zunic

Melissa S Egbertson

James C Barrow

Christopher D Cox

Zhicai Wu

B Wesley Trotter

Philip E Sanderson

Lida R Tehrani

Jiabing Wang

Brian T Campbell

William D Shipe

Michael J Kelly, Iii

Lou Anne Neilson

Jacob M Hoffman

Nathan R Kett

Amy Zartman

Jeffrey Melamed

Ahren Iver Green

Donna J Armstrong

Michael J Rossi

Michael J Iii Kelly

Ahren Green

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

5-lipoxygenase-activating protein (FLAP) inhibitors

The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

TRPA1 antagonists

A method for treating a human comprises administering a therapeutically effective amount of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid or a pharmaceutically acceptable salt or a pharmaceutically acceptable N-oxide thereof, to the human in need.

The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.

Quinolone neuropeptide S receptor antagonists

The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Inhibitors of akt activtiy

5-lipdxygenase-activating protein (FLAP) inhibitors

The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.

Inhibitors of Akt activity

The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Growing community of inventors

Lower Gwynedd, PA, United States of America

Yiwei Li