1380087-89-7Relevant articles and documents
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials
Albrecht, Brian K.,Gehling, Victor S.,Hewitt, Michael C.,Vaswani, Rishi G.,C?té, Alexandre,Leblanc, Yves,Nasveschuk, Christopher G.,Bellon, Steve,Bergeron, Louise,Campbell, Robert,Cantone, Nico,Cooper, Michael R.,Cummings, Richard T.,Jayaram, Hariharan,Joshi, Shivangi,Mertz, Jennifer A.,Neiss, Adrianne,Normant, Emmanuel,O'Meara, Michael,Pardo, Eneida,Poy, Florence,Sandy, Peter,Supko, Jeffrey,Sims, Robert J.,Harmange, Jean-Christophe,Taylor, Alexander M.,Audia, James E.
, p. 1330 - 1339 (2016)
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important disease-relevant genes, including MYC, BCL-2, and NF-κB. Here we describe the identification and characterization of a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor that attenuates BET-dependent gene expression in vivo, demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model, and is currently undergoing human clinical trials for hematological malignancies (CPI-0610).
CRYSTALLINE FORMS OF 2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4S5-E]AZEPIN-4-YL)ACETAMIDE
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Paragraph 0067-0068, (2016/06/28)
The present disclosure relates to a crystalline form of 2-((4S)-6-(4-chlorophenyl)-1- methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, which is useful as an inhibitor of bromodomain-containing proteins. The present disclosure also provides pharmac