Merck Sharp + Dohme Corp.

Amgen Inc.

Merck + Co., Inc.

Steve Fong Poon

Nicholas D Smith

Dehua Huang

Brian Walter Eastman

Jeffrey Roger Roppe

Jean-Michel Andre Vernier

Joseph E Payne

Thomas Jon Seiders

Jeannie M Arruda

Bowei Wang

Nicholas David Cosford

Xiumin Zhao

Chris King

Christopher Harold Fotsch

David Joseph St Jean, Jr

Kate Ashton

Christopher Michael Tegley

Ning Xi

Michael G Kelly

Andrew Stewart Tasker

Mark Henry Norman

Stephen A Hitchcock

Patricia Lopez

Nobuko Nishimura

Longbin Liu

Kevin Chao Yang

Qiufen May Xue

Wenge Zhong

Yuan Cheng

Scott S Harried

Nuria A Tamayo

Ted Charles Judd

Michael D Bartberger

Thomas S Reger

Paul E Harrington

James A Brown

Markian Myroslaw Stec

Lewis D Pennington

Michael D Croghan

Nicholas D P Cosford

Thomas Nixey

Chixu Chen

Thomas Stephen Coulter

Nick A Paras

Roxanne Kay Kunz

Yunxin Y Bo

Marian C Bryan

Chiara Ghiron

Timothy Powers

Clarence Henderson Hale

Adam James Davenport

Qing Ping Zeng

Nicholas D Cosford

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 ring A, B, B, B, L, R, R, Rand m 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 (AD), 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 heteroaryl compounds as beta-secretase modulators and methods of use

The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.

Thiazolyl mGluR5 antagonists and methods for their use

The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Compounds that interact with glucokinase regulatory protein for the treatment of diabetes

The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes. 

Calcium receptor modulating agents

Thiazolyl mglur5 antagonists and methods for their use

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

Growing community of inventors

South Pasadena, CA, United States of America

Steve Fong Poon