메뉴 건너뛰기




Volumn 21, Issue 9, 2011, Pages 2683-2686

Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: Discovery of MK-2918

Author keywords

Calcitonin gene related peptide; CGRP; Migraine; MK 2918; Telcagepant

Indexed keywords

AZABENZOXAZINONE SPIROPIPERIDINE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; CAPROLACTAM; DIMETHYL ETHER; IMIDAZOAZEPANE DERIVATIVE; IMIDAZOLE; MK 2918; PIPERIDINE DERIVATIVE; TELCAGEPANT; UNCLASSIFIED DRUG;

EID: 79955466716     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.054     Document Type: Conference Paper
Times cited : (13)

References (30)
  • 18
    • 79955483944 scopus 로고    scopus 로고
    • For the details of these assays see: Bell, I. M.; Graham, S. L.; Williams, T. M.; Stump, C. A. WO 2004/087649
    • For the details of these assays see: Bell, I. M.; Graham, S. L.; Williams, T. M.; Stump, C. A. WO 2004/087649.
  • 19
    • 79955479805 scopus 로고    scopus 로고
    • Aqueous solubilities at pH 7.4: telcagepant = 30 μg/mL; triazole 1 = 158 μg/mL
    • Aqueous solubilities at pH 7.4: telcagepant = 30 μg/mL; triazole 1 = 158 μg/mL.
  • 20
    • 79955477690 scopus 로고    scopus 로고
    • As a general trend, fused heterocycles in this series with low permeability resulted in low oral exposures
    • As a general trend, fused heterocycles in this series with low permeability resulted in low oral exposures.
  • 24
    • 79955482106 scopus 로고    scopus 로고
    • For additional synthetic details, see: Burgey, C. S.; Paone, D. V.; Shaw, A. W.; Nguyen, D. N.; Deng, Z. J.; Vacca, J. P.; Selnick, H. G.; Williams, T. M.; Potteiger, C. WO 2006/044504 A2
    • For additional synthetic details, see: Burgey, C. S.; Paone, D. V.; Shaw, A. W.; Nguyen, D. N.; Deng, Z. J.; Vacca, J. P.; Selnick, H. G.; Williams, T. M.; Potteiger, C. WO 2006/044504 A2.
  • 25
    • 79955478606 scopus 로고    scopus 로고
    • 1H NMR, HRMS, and HPLC
    • 1H NMR, HRMS, and HPLC.
  • 29
    • 79955480580 scopus 로고    scopus 로고
    • -OH = (po normalized AUC 31 upon dosing of 30)/ (iv normalized AUC 31 upon dosing of 31)
    • -OH = (po normalized AUC 31 upon dosing of 30)/ (iv normalized AUC 31 upon dosing of 31).
  • 30
    • 79955471613 scopus 로고    scopus 로고
    • Additions of both amino alcohols and amino ketones to thioamides were rapid, typically complete in <10 min. Cyclization of the intermediate amidine to 38 required and additional 18 h
    • Additions of both amino alcohols and amino ketones to thioamides were rapid, typically complete in <10 min. Cyclization of the intermediate amidine to 38 required and additional 18 h.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.