1800345-36-1Relevant articles and documents
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity
Degnan, Andrew P.,Everlof, Gerry,Fang, Haiquan,Fanslau, Carolynn,Gavai, Ashvinikumar V.,Haarhoff, Zuzana,Hill, Matthew D.,Huang, Christine,Kramer, Melissa,Lee, Francis,Marsilio, Frank,Menard, Krista,Monereau, Laura,Morrison, John,Ranasinghe, Asoka,Sheriff, Steven,Shields, Eric E.,Tokarski, John,Tye, Ching Kim,Westhouse, Richard,Yan, Chunhong,Zhang, Lisa,Zvyaga, Tatyana
, (2021)
We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 “cap” phenyl moiety with various heteroaryls, coupled with additional modifications to the carboline core, provided analogs with similar potency, improved pharmacokinetic properties, and increased solubility compared to our backup lead, BMS-986225 (2). Rapid SAR exploration was enabled by a convergent, synthetic route. These efforts provided a potent BET inhibitor, 3-fluoropyridyl 12, that demonstrated robust efficacy in a multiple myeloma mouse tumor model at 1 mg/kg.
SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A] PYRIDINE DERIVATIVES AND USE THEREOF
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Page/Page column 194; 401, (2020/10/27)
Provided herein are 2-amino-pyrazolyl-[ 1,2,4]triazolo [1,5a]pyridine derivatives. Such compounds are useful, for example, for the treatment and/or prevention of neurodegenerative diseases or disorders such as ophthalmological neurodegenerative disorders. This disclosure also features compositions containing the same as well as methods of using and making the same.
TRICYCLIC COMPOUND FOR BROMODOMAIN-CONTAINING PROTEIN INHIBITOR AND PREPARATION, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
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, (2019/01/04)
The present applicationpresent application relates to a compound represented by Formula (III) or a pharmaceutically acceptable salt, solvent compound, active metabolite, crystal polymorph, ester, isomer, or prodrug thereof. The application further provides a pharmaceutical composition comprising the compound represented by Formula (III) and a use thereof for preparing a bromodomain inhibitor for preventing or treating various diseases, such as inflammation and cancer, related to the bromodomain.