773887-32-4Relevant academic research and scientific papers
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7- methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl) piperidine-1-carboxamide (BMS-694153): A potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure
Degnan, Andrew P.,Chaturvedula, Prasad V.,Conway, Charles M.,Cook, Deborah A.,Davis, Carl D.,Denton, Rex,Han, Xiaojun,Macci, Robert,Mathias, Neil R.,Moench, Paul,Pin, Sokhom S.,Ren, Shelly X.,Schartman, Richard,Signor, Laura J.,Thalody, George,Widmann, Kimberly A.,Xu, Cen,Macor, John E.,Dubowchik, Gene M.
supporting information; experimental part, p. 4858 - 4861 (2009/08/09)
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein, we describe the optimization of these leads to give 4 (BMS-694153), a molecule with outstanding potency, a favorable predictive toxicology profile, and remarkable aqueous solubility. Compound 4 has good intranasal bioavailablity in rabbits and shows dose-dependent activity in validated in vivo and ex vivo migraine models.
Novel therapeutic agents for the treatment of migraine
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Page/Page column 47, (2010/02/14)
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 u
HETEROCYCLIC ANTI-MIGRAINE AGENTS
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Page/Page column 38, (2008/06/13)
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.
Calcitonin gene related peptide receptor antagonists
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, (2008/06/13)
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.
