291509-61-0Relevant articles and documents
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
-
Paragraph 0404; 0470, (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.
CGRP ANTAGONISTS
-
Page/Page column 67, (2011/04/18)
The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
3-(4-PIPERIDINYL)-2,3,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-2(1H)-ON
-
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
-
Page/Page column 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
-
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
BENZODIAZEPINE CGRP RECEPTOR ANTAGONISTS
-
Page 40, (2010/02/10)
The present invention is directed to compounds of Formula I: I (where variables R1, R2, R3, R6, R7, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Calcitonin gene related peptide receptor antagonists
-
, (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.