22162-19-2Relevant articles and documents
The discovery of highly potent CGRP receptor antagonists
Stump, Craig A.,Bell, Ian M.,Bednar, Rodney A.,Bruno, Joseph G.,Fay, John F.,Gallicchio, Steven N.,Johnston, Victor K.,Moore, Eric L.,Mosser, Scott D.,Quigley, Amy G.,Salvatore, Christopher A.,Theberge, Cory R.,Blair Zartman,Zhang, Xu-Fang,Kane, Stefanie A.,Graham, Samuel L.,Vacca, Joseph P.,Williams, Theresa M.
, p. 214 - 217 (2009)
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the hydantoin that consistently improved
HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS
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Page/Page column 112; 116-118, (2020/06/05)
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein HET, R1, R2, R3, R4, R5, L, L1, X1, X2, X3 and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.
FlICk (fluorescent isoindole crosslinking) for peptide stapling
Todorovic, Mihajlo,Perrin, David M.
, p. 313 - 332 (2020/05/18)
The rigidification of peptide secondary structure via stapling is an important and enduring goal in the development of functional peptides for biochemical and pharmaceutical applications. In addition, the incorporation of fluorophores and chromophores has