Sgx Pharmaceuticals, Inc.

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Ardea Biosciences, Inc

Chixu Chen

Brian Walter Eastman

Ruo W Steensma

Stephanie Hopkins

Stefan N Gradl

Mark E Wilson

William D Arnold

Nicholas D P Cosford

Andreas Gosberg

Nicholas D Smith

Ian A McDonald

Zhe Li

Pierre Bounaud

Paul A Sprengeler

Jean-Michel Andre Vernier

Benito Munoz

Dehua Huang

Jeffrey Roger Roppe

Thomas S Reger

Samedy Ouk

Esmir Gunic

Essa H Hu

Masaki Tomimoto

Mark T Bilodeau

Zhicai Wu

Gavin C Hirst

Peter J Manley

Lida R Tehrani

Lou Anne Neilson

John C Hartnett

Steve Fong Poon

Richard Pracitto

Khanh Thi Tuong Nguyen

Paul E Sprengeler

Steven F Poon

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Thioacetate compounds, compositions and methods of use

The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.

Fused ring heterocycle kinase modulators

The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.

The present invention provides novel pyrimidinyl-thiophene kinase modulators and methods of using the novel pyrimidinyl-thiophene kinase modulators to treat diseases mediated by kinase activity.

Pyrimidinyl-thiophene kinase modulators

The present invention is directed to compounds which contain substituted napthyridines 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.

Inhibitors of Akt activity

The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity.

Pyrrolo-pyridine kinase modulators

The instant invention provides for 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 activity

Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.

Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5

Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.

Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5

Tetrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Heteroaryl substituted tetrazole modulators of metabotrophic glutamate receptor-5

Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

Solid phase synthesis of heterocycles

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San Diego, CA, United States of America

Chixu Chen