Amgen Inc.

Biovitrum Ab

Randall W Hungate

Michael D Bartberger

Christopher Michael Tegley

Brian K Albrecht

Patricia Lopez

Qingyian Liu

Qiufen May Xue

Wenge Zhong

Yuan Cheng

Ted Charles Judd

Craig E Masse

Vinod Francis Patel

Matthew M Weiss

Jennifer Rebecca Allen

Stephen A Hitchcock

Holger Monenschein

Thomas T Nguyen

Christopher Harold Fotsch

Scott S Harried

Daniel La

James A Brown

Russell Graceffa

Lewis D Pennington

Nianhe Han

Michael D Croghan

Thomas Nixey

Charles Kreiman

Bryant Yang

Stuart C Chaffee

Ryan Brown

Matthew R Kaller

Michael J Frohn

Guolin Cai

Qi Huang

Chester Chenguang Yuan

Roland W Burli

Aiwen Li

David Joseph St Jean, Jr

Susana C Neira

George Moniz

Meredith Williams

Evert Homan

Lars Johansson

Martin Henriksson

Matthew J Frizzle

Eric A Bercot

Jennifer Elizabeth Golden

Kaustav Biswas

Stephanie J Mercede

Kristine M Muller

Denise Lyn Andersen

Jennifer Dao

Ning Xi

Mark Henry Norman

Anthony B Reed

Robert Michael Rzasa

Shimin Xu

Deborah Choquette

Andrew Stewart Tasker

Jean-Christophe P Harmange

Longbin Liu

Kevin Chao Yang

Shon Booker

Ryan D White

Liping H Pettus

Richard Thomas Lewis

Ana Elena Minatti

Dawei Zhang

Aaron C Siegmund

Angel Guzman-Perez

Laurie B Schenkel

Steven F Bellon

Paul E Harrington

Daniel B Horne

Tae-Seong Kim

Markian Myroslaw Stec

Elizabeth M Doherty

Alessandro Boezio

James Richard Falsey

Shannon Rumfelt

Karina Romero

Jason Brooks Human

Michele Potashman

Philip R Olivieri

Derin C D'amico

Zihao Hua

Bradley J Herberich

David Bauer

Xiao Mei Zheng

Oleg Epstein

Kelvin K C Sham

Guo-Qiang Cao

Partha P Chakrabarti

Julia Winslow Lohman

John Stellwagen

Emily Anne Peterson

Derin D'Amico

Katrina Woodin Copeland

Christiane M Bode

Satoko Hirai

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, R, R, R, Rand n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding 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 Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II. 

Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Fused heterocyclic derivatives and methods of use

The present invention relates to compounds with the formula (I), (II), (III) or (IV): 

Inhibitors of 11-&#x3b2;-hydroxy steroid dehydrogenase type 1

The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-&#x3b2;-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-&#x3b2;-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1

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, B, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Beta-secretase modulators and methods of use

Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

Heterocyclic quinolone derivatives that inhibit prolyl hydroxylase activity

This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.

Quinolone based compounds exhibiting, prolyl hydroxylase inhibitory activity, and compositions, and uses thereof

Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof

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, B, W, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

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 R, W, B, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein B, R, R, R, Rand Rare d.efined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Phthalazine compounds and methods of use

Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity

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Camarillo, CA, United States of America

Randall W Hungate