Amgen Inc.

Charles Kreiman

Matthew M Weiss

Vinod Francis Patel

Russell Graceffa

Thomas Dineen

Patricia Lopez

Wenge Zhong

Qiufen May Xue

Daniel La

Stephen A Hitchcock

Holger Monenschein

Thomas T Nguyen

Ted Charles Judd

Michael D Croghan

Bryant Yang

Yuan Cheng

Scott S Harried

Matthew R Kaller

James A Brown

Isaac E Marx

Lewis D Pennington

Craig E Masse

Brian K Albrecht

Michael D Bartberger

Hanh Nho Nguyen

Thomas Nixey

Randall W Hungate

Erin F DiMauro

Stuart C Chaffee

Ryan Brown

Daniel B Horne

Emily Anne Peterson

Hongbing Huang

Angel Guzman-Perez

Alan C Cheng

Alessandro Boezio

Christiane Boezio

Denise Lyn Andersen

Jonathan B Houze

Qingyian Liu

Ryan D White

Albert Kudzovi Amegadzie

Zhihua Ma

Paul John Dransfield

Vu Van Ma

Vatee Pattaropong

Wenyuan Qian

Mikkel V Debenedetto

Su-Jen Lai

Gayathri Swaminath

Jason Brooks Human

Yinhong Chen

Vijay Keshav Gore

Aarif Yusuf Khakoo

James S Harvey

Holly L Deak

Oleg Epstein

John R Butler

Margaret Chu-Moyer

Brian Andrew Sparling

Dean Hickman

Jian Jeffrey Chen

Ning Chen

Nobuko Nishimura

Ana Elena Minatti

Chester Chenguang Yuan

Wen-Chen Yeh

Julie Anne Heath

Stephanie Geuns-Meyer

Karina Romero

Nick A Paras

Zihao Hua

David C Moebius

Xiao Mei Zheng

Nagasree Chakka

Marian C Bryan

Bingfan Du

Benjamin Charles Milgram

Howard Bregman

Katrina Woodin Copeland

Ankit Sharma

James R Coats

Karina R Vaida

Dan Horne

Matthew Walker

Matthew K Kaller

Benjamin Charles Milgrim

James Brown

Jason B Human

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein. 

Triazole phenyl compounds as agonists of the APJ receptor

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the structures where the definitions of the variables are provided herein. 

Triazole pyridyl compounds as agonists of the APJ receptor

The present invention provides compounds of Formula I or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. 

Bicyclic sulfonamide compounds as sodium channel inhibitors

The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. 

Sulfamide sodium channel inhibitors

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7.  The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Bicyclic aryl and heteroaryl sodium channel inhibitors

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 other related conditions. In one embodiment, the compounds have a general Formula I wherein A, A, A, A, A, A, R, R, X and Y 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.

Spiro-tetracyclic ring 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 activity and for the treatment of diseases, including Alzheimer's disease (AD) and related CNS conditions, mediated thereby. In one embodiment, the compounds have a general Formula I or Formula II wherein R, B, Rand W of Formula I, and R, R, A, W, X, Z, m and n of Formula II are defined herein. The invention further provides compounds of Formula III and IV and sub-Formulas II-A-II-D and III-A-III-D. The compounds may be used in pharmaceutical compositions for treating, prophylactically or therapeutically, disorders related to the activity of beta-secretase protein, including without limitation, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.

Substituted hydroxyethyl amine 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, T, T, W, 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.

Spiro-tricyclic ring 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 R, R, R, B, W, R, Rand Rare defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A, A, A, A, R, R, R, R, R, R, W, X and Z 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 (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

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

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 or Formula II wherein R, R, R, B, R, R, Rand W of Formula I, and R, R, R, R, R, R, R, R, A, A, A, A, W, X, Z, m and n of Formula II are defined herein. The invention also provides compounds of Formula III, sub-Formulas II-A-II-D, sub-Formulas III-A-III-D and Formula IV. The invention further 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, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formulas I, II, III, IV and sub-formulas thereof, intermediates and processes useful for the preparation of compounds of Formulas I, II, III, IV and sub-formulas 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

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Watertown, MA, United States of America

Charles Kreiman