Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Frosst Canada, Inc.

Mark T Goulet

Matthew J Wyvratt

Thomas F Walsh

Feroze Ujjainwalla

Lin Chu

Jonathan R Young

Peter J Sinclair

Frederick Wong

Michael H Fisher

William H Parsons

Wallace T Ashton

Peter Lin

Robert Joseph Devita

Narindar N Girotra

Daniel Warner

Ravi P Nargund

Helen M Organ

Stephanie L Witkin

William K Hagmann

Shrenik K Shah

Jinlong Jiang

Mitree M Ponpipom

Linus S Lin

James Patrick Jewell

Thomas R Beattie

Eric E Allen

Robert L Bugianesi

Richard B Toupence

Roy G Smith

Joung L Goulet

Yi Tien Yang

John Howard Hutchinson

Yves Girard

Michel Therien

Ping Liu

John S Debenham

Richard Frenette

Raman Kumar Bakshi

Anthony K Ogawa

Linda L Chang

Zhixiong Ye

Hyun O Ok

Christina B Madsen-Duggan

Derek J Von Langen

Dwight Macdonald

Iyassu K Sebhat

Terence G Hamill

H Donald Burns

Raymond E Gibson

Alex Minhua Chen

Andrey V Peresypkin

Bonnie Louridas

Derek Von Langen

The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

Radiolabeled cannabinoid-1 receptor modulators

Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperidine derivatives as melanocortin-4 receptor agonists

The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents. 

Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use

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

Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinsons disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Substituted furo[2,3-b]pyridine derivatives

Certain novel-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-receptor (MC-R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

There are disclosed compounds of formula (I)

Antagonists of gonadotropin releasing hormone

There are disclosed compounds of formula (I) 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 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.

Growing community of inventors

Westfield, NJ, United States of America

Mark T Goulet