773886-92-3Relevant academic research and scientific papers
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists
Mercer, Stephen E.,Chaturvedula, Prasad V.,Conway, Charles M.,Cook, Deborah A.,Davis, Carl D.,Pin, Sokhom S.,Macci, Robert,Schartman, Richard,Signor, Laura J.,Widmann, Kimberly A.,Whiterock, Valerie J.,Chen, Ping,Xu, Cen,Herbst, John J.,Kostich, Walter A.,Thalody, George,Macor, John E.,Dubowchik, Gene M.
, (2020/12/17)
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP Ki = 0.023 nM) that has
NOVEL HETEROCYCLIC COMPOUNDS AND USE THEREOF IN MEDICINE AND IN COSMETICS
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Paragraph 0403; 0469, (2018/03/25)
The invention relates to novel heterocyclic compounds of general formula (I), as well as their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to the use thereof as a medicinal product, preferably in the prevention and/or treatment of inflammatory diseases with a neurogenic component or use thereof as a cosmetic. The compounds of the present invention act as antagonists of the CGRP-R receptor.
AMIDE-SUBSTITUTED ARYL PIPERIDINES
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Page/Page column 54-55, (2008/12/05)
Amide-substituted aryl piperidines derivatives of the following Formulas are provided:(Formulas), in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache, such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
BIARYL KETONE-SUBSTITUTED PIPERIDINES
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Page/Page column 52, (2008/12/06)
Biaryl ketone-substituted piperidines of the following Formulas are provided:, and in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
3-(4-PIPERIDINYL)-2,3,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-2(1H)-ON
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Page/Page column 3, (2008/06/13)
The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one of formula which is to be found as a structural element in CGRP antagonists which are suitable above all for the oral th
CONSTRAINED COMPOUNDS AS CGRP-RECEPTOR ANTAGONISTS
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Page/Page column 108-109, (2008/06/13)
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.
3-(4-PIPERIDINYL)-2,3,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-2(1H)-ONE
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Page/Page column 3, (2010/02/15)
The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1-one of formula which is to be found as a structural element in CGRP-antagonists, which are particularly suitable for the oral
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.
