31163-12-9Relevant articles and documents
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
-
, (2021/02/25)
The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS)
Come, Jon H.,Collier, Philip N.,Henderson, James A.,Pierce, Albert C.,Davies, Robert J.,Le Tiran, Arnaud,O'Dowd, Hardwin,Bandarage, Upul K.,Cao, Jingrong,Deininger, David,Grey, Ron,Krueger, Elaine B.,Lowe, Derek B.,Liang, Jianglin,Liao, Yusheng,Messersmith, David,Nanthakumar, Suganthi,Sizensky, Emmanuelle,Wang, Jian,Xu, Jinwang,Chin, Elaine Y.,Damagnez, Veronique,Doran, John D.,Dworakowski, Wojciech,Griffith, James P.,Jacobs, Marc D.,Khare-Pandit, Suvarna,Mahajan, Sudipta,Moody, Cameron S.,Aronov, Alex M.
, p. 5245 - 5256 (2018/06/08)
The lipid kinase phosphoinositide 3-kinase γ (PI3Kγ) has attracted attention as a potential target to treat a variety of autoimmune disorders, including multiple sclerosis, due to its role in immune modulation and microglial activation. By minimizing the number of hydrogen bond donors while targeting a previously uncovered selectivity pocket adjacent to the ATP binding site of PI3Kγ, we discovered a series of azaisoindolinones as selective, brain penetrant inhibitors of PI3Kγ. This ultimately led to the discovery of 16, an orally bioavailable compound that showed efficacy in murine experimental autoimmune encephalomyelitis (EAE), a preclinical model of multiple sclerosis.
SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
-
, (2016/04/10)
Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
