1095273-53-2Relevant academic research and scientific papers
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine
Nichols, Paula L.,Brand, Jonathan,Briggs, Michael,D'Angeli, Mathilde,Farge, Jennifer,Garland, Stephen L.,Goldsmith, Paul,Hutchings, Rio,Kilford, Ian,Li, Ho Y.,MacPherson, David,Nimmo, Fiona,Sanderson, Francis Dominic,Sehmi, Sanjeet,Shuker, Nicola,Skidmore, John,Stott, Michael,Sweeting, Jennifer,Tajuddin, Hasmi,Takle, Andrew K.,Trani, Giancarlo,Wall, Ian D.,Ward, Robert,Wilson, David M.,Witty, David
scheme or table, p. 1368 - 1372 (2010/07/02)
A pharmacophore model was built, based on known CGRP receptor antagonists, and this was used to aid the identification of novel leads. Analogues were designed, modelled and synthesised which incorporated alternative 'LHS' fragments linked via either an amide or urea to a privileged 'RHS' fragment commonly found in CGRP receptor antagonists. As a result a novel series of oxadiazole CGRP receptor antagonists has been identified and the subsequent optimisation to enhance both potency and bioavailability is presented.
5-PHENYL-1,3,4-OXADIAZOL-2-YL-ACETYL-4-PIPERIDINYL DERIVATIVES AS CGRP RECEPTOR ANTAGONISTS
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Page/Page column 75, (2009/03/07)
The present invention relates to novel compounds that are CGRP receptor antagonists, processes for their preparation, to compositions containing them and to their use in the treatment of migraine, headache, and cluster headache.
