136234-80-5Relevant articles and documents
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead
Williams, Theresa M.,Stump, Craig A.,Nguyen, Diem N.,Quigley, Amy G.,Bell, Ian M.,Gallicchio, Steven N.,Zartman, C. Blair,Wan, Bang-Lin,Penna, Kimberly Della,Kunapuli, Priya,Kane, Stefanie A.,Koblan, Ken S.,Mosser, Scott D.,Rutledge, Ruth Z.,Salvatore, Christopher,Fay, John F.,Vacca, Joseph P.,Graham, Samuel L.
, p. 2595 - 2598 (2008/12/23)
High-throughput screening of the Merck sample collection identified benzodiazepinone tetralin-spirohydantoin 1 as a CGRP receptor antagonist with micromolar activity. Comparing the structure of 1 with those of earlier peptide-based antagonists such as BIB
Benzodiazepine analogs
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, (2008/06/13)
Benzodiazepine analogs of the formula: STR1 wherein: R 3 is STR2 --NH(CH 2) 2 -- 3 NHCOR 7, STR3 or --X 11 NR 18 SO 2 (CH 2) q R 7 ; R 7 is O,S,HH, or NR 15 with the proviso that X 7 can be NR 15 only when R 1 is not H.are disclosed which are antagonists
New benzodiazepine analogs
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, (2008/06/13)
Pharmaceutical compositions containing benzodiazepine analogs of the formula: are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of oncologic disorders, con