169884-67-7Relevant articles and documents
Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups
Jeffries, Benjamin,Wang, Zhong,Troup, Robert I.,Goupille, Ana?s,Le Questel, Jean-Yves,Fallan, Charlene,Scott, James S.,Chiarparin, Elisabetta,Graton, Jér?me,Linclau, Bruno
supporting information, p. 2141 - 2150 (2021/02/05)
A systematic comparison of lipophilicity modulations upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl substituents, at a single carbon atom, is provided using directly comparable, and easily accessible model compounds. In addition, comparison with relevant linear chain derivatives is provided, as well as lipophilicity changes occurring upon chain extension of acyclic precursors to give cyclopropyl containing compounds. For the compounds investigated, fluorination of the isopropyl substituent led to larger lipophilicity modulation compared to fluorination of the cyclopropyl substituent.
4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS
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Page/Page column 624; 625, (2016/06/14)
The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.