Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Link Medicine Corporation

Peter Lin

Matthew J Wyvratt

Mark T Goulet

Lin Chu

Michael H Fisher

Wallace T Ashton

Narindar N Girotra

Jonathan R Young

Robert J DeVita

Mitree M Ponpipom

Lehua Chang

Sander G Mills

Mark E Duggan

Thomas F Walsh

Scott D Edmondson

Jinlong Jiang

Gregori J Morriello

William R Schoen

Peter T Lansbury

Robert L Bugianesi

Roy G Smith

Yi Tien Yang

Judith M Pisano

Danny Chaung

MyLe Hoang

Andreas W Sailer

Craig J Justman

Ross A Fredenburg

Robin Kate Meray

Robert J Devita

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of &#x3b2;3-adrenoceptor. 

Pyrrolidine-derived beta 3 adrenergic receptor agonists

Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. The treatment including administering to a subject a therapeutically effective amount of an inventive farnesyl transferase inhibitor compound.

Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications

This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

Anti-hypercholesterolemic compounds

The present invention is directed to certain phenyl pyrrolidine ether compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, depression, and anxiety.

Phenyl pyrrolidine ether tachykinin receptor antagonists

The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

2-Aminoquinoline compounds

There are disclosed compounds of formula (I)

Antagonists of gonadotropin releasing hormone

There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

There are disclosed certain compounds identified as substituted dipeptide analogs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such substituted dipeptide analogs as the active ingredient thereof are also disclosed.

Biphenyl substituted dipeptide analogs promote release of growth hormone

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Edison, NJ, United States of America

Peter Lin