Bristol-myers Squibb Compnay

Graham S Poindexter

Marc A Bruce

John E Macor

Guanglin Luo

Prasad V Chaturvedula

Gene Michael Dubowchik

Graham Johnson

Ling Chen

Xiaojun Han

Xiang Jun J Jiang

R Michael Lawrence

Sing-Yuen Sit

Edward H Ruediger

Guixue Yu

George C Morton

George O Tora

Kevin W Gillman

Andrew P Degnan

Rejean Ruel

Timothy F Herpin

Rita Civiello

Carl Thibault

Karen LeBoulluec

Katherine S Takaki

Charles P Sloan

Mendi A Higgins

George N Karageorge

Brett T Watson

Shikha Vig

Leah M Giupponi

Ildiko Antal

Robert H Stoffel

Joseph P Yevich

Scott W Martin

James Breitenbucher

Brett R Beno

Michael R Kozlowski

Haiquan Fang

Stephen E Mercer

Yazhong Huang

Ivo Monkovic

James R Epperson

R Thomas Swann

Ramakrishna Seethala

Jeffrey W Noonan

James Guy Breitenbucher

Mendi A Morton

Charles Mark Conway

The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors ('CGRP-receptor'), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Anti-migraine spirocycles

Spirocyclic anti-migraine compounds

The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors. 

Constrained compounds as CGRP-receptor antagonists

The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I) 

Anti-migraine treatments

Calcitonin gene related peptide receptor antagonists

Compounds having the formula (I), G is a novel side chain selected from Calkenyl, A-aryl, &#x2014;OR, heteroaryl, A-cyano, A&#x2014;OR, A&#x2014;C(&#x2550;O)R, A&#x2014;COR, A&#x2014;C(&#x2550;O)NRR, A&#x2014;OC(&#x2550;O)R, A&#x2014;NRC(&#x2550;O)R, A&#x2014;OC(&#x2550;O)NRR, A&#x2014;NRCOR, A&#x2014;NRSOR, A&#x2014;SOR, A&#x2014;NRC(&#x2550;O)NRR, and A&#x2014;SR; or when y is 0 or when W is not NHR, G may be A-heterocyclo, wherein Ais a bond, Calkylene or C-alkenylene, Ais Calkylene or Calkenylene, and Ais Calkenylene; W is selected from &#x2014;NRR, &#x2014;OR, &#x2014;NRC(&#x2550;O)R, &#x2014;NRCOR, amidino, guanidino, or a heteroaryl, heterocyclo or Ccycloalkyl as defined in the specification, and X and Rthrough Rare as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.

Compounds useful as modulators of Melanocortin Receptors and pharmaceutical compositions comprising same

Novel azetidinyl and pyrrolidinyl compounds are ligands of melanocortin-4 receptors and are useful for treating conditions responsive to the modulation of melanocortin-4 receptors such as obesity, diabetes, and sexual dysfunction. 

Amidoheterocycles as modulators of the melanocortin-4 receptor

Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof,in which E isX is N or CH, W is &#x2014;NRR, &#x2014;NRC(&#x2550;O)R, &#x2014;NRCOR, &#x2014;OR, or a heteroaryl or heterocyclo group as defined in the specification, and Rthrough R, R, R, R, R, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.

Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same

Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.

Alpha-aminoamide derivatives as melanocortin agonists

Oxadiazole and thiadiazole derivatives of dihydropyridine NPY antagonists

Alkylamine derivatives of dihydropyridine NPY antagonists

Squarate derivatives of dihydropyridine NPY antagonists

NPY antagonists: spiroisoquinolinone derivatives

A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of heteroaryl derivatives of imidazolone compounds of Formula 1. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Imidazolone anorectic agents: III. heteroaryl derivatives

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Old Saybrook, CT, United States of America

Graham S Poindexter