748166-19-0Relevant articles and documents
JAK kinase inhibitor and application
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Paragraph 0079-0080; 0082-0084, (2018/09/08)
The present invention discloses a compound having the following general formula (I). The present invention also discloses a JAK kinase inhibitor comprising the compound and application of the compoundin preparation of a medicament for treating JAK-associated diseases. The JAK kinase inhibitor can inhibit the biological activities of JAK1, JAK2, JAK3 and TYK2 kinases involved in various kinds of signal transduction, can effectively treat various inflammatory diseases and various JAK-mediated signal transduction-driven diseases, and has a very broad application prospect.
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: A ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation
Runyon, Scott P.,Mosier, Philip D.,Roth, Bryan L.,Glennon, Richard A.,Westkaemper, Richard B.
experimental part, p. 6808 - 6828 (2009/10/17)
The effects of 3-position substitution of 9-aminomethy 1-9,10- dihydroanthracene (AMDA) on 5-HT2A receptor affinity were determined and compared to a parallel series of DOB-like 1-(2,5-dimethoxyphenyl)-2- aminopropanes substituted at the 4-position. The results were interpreted within the context of 5-HT2A receptor models that suggest that members of the DOB-like series can bind to the receptor in two distinct modes that correlate with the compounds' functional activity. Automated ligand docking and molecular dynamics suggest that all of the AMDA derivatives, the parent of which is a 5-HT2A antagonist, bind in a fashion analogous to that for the sterically demanding antagonist DOB-like compounds. The failure of the F340 6.52L mutation to adversely affect the affinity of AMDA and the 3-bromo derivative is consistent with the proposed modes of orientation. Evaluation of ligand-receptor complex models suggest that a valine/threonine exchange between the 5-HT2A and D2 receptors may be the origin of selectivity for AMDA and two substituted derivatives.
Histamine H1 receptor ligands - Part II. Synthesis and in vitro pharmacology of 2-[2-(phenylamino)thiazol-4-yl]ethanamine and 2-(2-benzhydrylthiazol-4-yl)ethanamine derivatives
Walczynski, Krzysztof,Guryn, Roman,Zuiderveld, Obbe P.,Zhang, Ming-Qiang,Timmerman, Henk
, p. 569 - 574 (2007/10/03)
New 2-[2-(phenylamino)thiazol-4-yl]ethanamine and 2-(2-benzhydrylthiazol-4-yl)ethanamine derivatives were prepared and tested in vitro as H1 receptor antagonists. The compounds with 2-phenylamino substitution with meta-halide substituents at the phenyl ring, showed weak H1-antagonistic activity (pA2: 4.62-5.04) and this activity was completely lost in the case of meta-methyl substituent (pA2 : 4). When the phenylamino group was replaced by benzhydryl groups of classic antihistamines, the resulting compounds exhibited slightly improved H1-antagonistic activity (at the meta-position pA2: 6.38-6.15; at the para-position pA2: 6.04-5.87).