Amgen Inc.

Smithkline Beecham Corporation

Cephalon, Inc.

Kelvin C Sham

Jennifer Rebecca Allen

Robert Michael Rzasa

Ryan D White

Michael J Frohn

Paul E Harrington

James Richard Falsey

Shannon Rumfelt

Ning Chen

Patricia Lopez

Matthew R Kaller

Qiufen May Xue

Yuan Cheng

Ana Elena Minatti

Thomas T Nguyen

Alexander J Pickrell

Vu Van Ma

Andreas Reichelt

Kaustav Biswas

Jason Brooks Human

Roxanne Kay Kunz

Xiao Mei Zheng

Oleg Epstein

Essa Hu Harrington

Guomin Yao

Holger Monenschein

Bin Wu

Nobuko Nishimura

Albert Kudzovi Amegadzie

Ted Charles Judd

Angel Guzman-Perez

Jonathan Dante Low

Leslie Phillip Miranda

Daniel B Horne

James A Brown

Wenyuan Qian

Bryant Yang

Robert A Daines

Adrian Leonard Smith

Frank Chavez

Jerry Ryan Holder

Frenel Fils De Morin

Christopher Michael Tegley

Jian Jeffrey Chen

John P Mallamo

Sankar Chatterjee

Qingyian Liu

Wenge Zhong

Scott S Harried

Kurt A Josef

Aaron C Siegmund

Jing M Xu

Derek D Dunn

Elizabeth M Doherty

Murielle M Veniant-Ellison

Vijay Keshav Gore

Bradley J Herberich

William D Kingsbury

Junming Yie

Zi-Qiang Gu

Justin K Murray

Malgorzata Wanska

Shu-Chen Lu

Chawita Netirojjanakul

Shanaka Stanislaus

Jason C Long

Israel Pendrak

Daniel B Home

Biswas Kaustav

Methods of treating metabolic diseases and disorders using a composition comprising an antigen binding protein specific for the GIPR polypeptide conjugated to a GLP-1 receptor agonist are provided. In various embodiments the metabolic disease or disorder is type 2 diabetes, obesity, dyslipidemia, elevated glucose levels, elevated insulin levels and diabetic nephropathy. In certain embodiments the composition comprises an antibody or functional fragment thereof comprising a cysteine at one or more conjugation site(s) wherein the GLP-1 receptor agonist is conjugated to the antibody or functional fragment thereof through the side-chain of the cysteine residue.

Method of treating or ameliorating metabolic disorders using GLP-1 receptor agonists conjugated to antagonists for gastric inhibitory peptide receptor (GIPR)

Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Na1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Na1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

Potent and selective inhibitors of Nav1.7

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, A, A, A, A, A, A, L, R, R, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I. 

Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, A, A, A, A, A, L, R, R, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I. 

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, A, A, A, each of R, R, R, R, Rand Rof Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

Chroman derivatives as TRPM8 inhibitors

Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors

Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R, R, R, R, R, R, R, X, X, X, X, X, X, X, X, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R, R, R, R, R, R, R, R, X, X, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R, R, R, R, R, R, R, X, X, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors

This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH useful in treating bacterial infections.

Indole compounds useful for treating bacterial infections

The present invention is directed to quinoline-containing .alpha.-ketoamide inhibitors of cysteine and serine proteases are disclosed. Methods for making these compounds, and methods for using the same are also disclosed.

Quinoline-containing .alpha.-ketoamide cysteine and serine protease

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King of Prussia, PA, United States of America

Kelvin C Sham