Merck & Company, Inc.

Other

Meiji Seika Kaisha, Ltd.

Arthur A Patchett

William J Greenlee

Prasun K Chakravarty

Lihu Yang

Ravi P Nargund

Thomas F Walsh

Nathan B Mantlo

William H Parsons

Elbert E Harris

Eugene D Thorsett

James R Tata

Meng Hsin Chen

Malcolm MacCoss

Gregori J Morriello

Eric E Allen

Daljit S Dhanoa

William R Schoen

David B Johnston

Ralph A Rivero

Kenneth J Fitch

Mu T Wu

Stephen E De Laszlo

Matthew J Wyvratt

Alexander Pasternak

Dooseop Kim

Janet C Onishi

David G Hangauer

Janos Kollonitsch

Michael H Fisher

Wallace T Ashton

Raman Kumar Bakshi

Zhixiong Ye

David Taub

Meng-Hsin Chen

Brenda L Palucki

Edward W Tristram

Clarence S Rooney

Edward J Grabowski

Leonardus H T Van Der Ploeg

Haydn W Williams

Liangqin Guo

Kevin Tyler Chapman

Robert T Goegelman

Linda L Chang

Richard B Toupence

Masao Taniguchi

Gregory D Berger

Joel Peter Berger

Khaled J Barakat

Jan Ten Broeke

Tomasz W Glinka

David E Moller

Mark D Leibowitz

Edward J Cragoe, Jr

Zhijian Lu

Yoshiharu Morita

John C Chabala

Scott C Berk

Scott W Bagley

Iyassu K Sebhat

Haruyuki Chaki

Thomas W Doebber

Burton G Christensen

Richard L Tolman

Suresh B Singh

Bruce E Witzel

Ann E Weber

Nathaniel Grier

Changyou Zhou

Seiji Shibahara

Donald W Graham

Richard A Dybas

Soumya P Sahoo

Yusheng Xiong

Alan L Maycock

Gideon A Rodan

Andrew D Howard

Alan D Adams

Raymond F White

Stephen Marburg

Tsuneo Okonogi

Derek J Von Langen

Douglas J MacNeil

Min K Park

Henry Joshua

Scott D Feighner

Roy G Smith

Carina P Tan

Conrad Santini

Elizabeth M Naylor

Jian Guo

Ching C Wang

Chan-Hwa Kuo

Michael D Greenspan

William V Ruyle

Shokichi Ohuchi

Yasuyuki Ichimaru

Frank L VanMiddlesworth

Raymond George Hill

Yingjie Lai

This invention relates to compounds of formula (I), and a method for treating anthrax or inhibiting lethal factor by administrating a composition containing a compound of formula (I) and a pharmaceutically acceptable carrier. This invention further relates to the use of the compounds of formula (I) to treat other conditions related to an anthrax infection.

Compounds useful in the treatment of anthrax and inhibiting lethal factor

The motilin receptor has been isolated and cloned, and nucleic acid sequences are given. Two spice variants have been identified. Also, assays for motilin receptor ligands are given. The identification of the cloned motilin receptor may be used to screen and identify compounds which bind to the receptor for use in a variety of gastric conditions, including gastric motility disorders.

Cloning and identification of the motilin receptor

Certain novel 4-substituted piperidine compounds 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.

Substituted piperidines as melanocortin receptor agonists

The present invention relates to benzimidazolinylpiperidine derivatives useful as ligands for CGRP (Calcitonin Gene-Related Peptide) receptors, their use in therapy, pharmaceutical compositions comprising them and methods of treatment using them.

Benzimidazolinyl piperidines as CGRP ligands

Amido spiropiperidines promote the release of growth hormone

Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

Spiropiperidine derivatives as melanocortin receptor agonists

This invention relates to non-peptide somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are orally active.

Somatostatin agonists

Certain novel substituted piperidine compounds 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. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

Substituted piperidines as melanocortin-4 receptor agonists

The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Naphthyl compounds promote release of growth hormone

This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.

The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

Benzisoxazole-derived antidiabetic compounds

This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.

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Westfield, NJ, United States of America

Arthur A Patchett