199105-10-7Relevant academic research and scientific papers
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6
Shen, Yudao,Szewczyk, Magdalena M.,Eram, Mohammad S.,Smil, David,Kaniskan, H. ümit,Ferreira De Freitas, Renato,Senisterra, Guillermo,Li, Fengling,Schapira, Matthieu,Brown, Peter J.,Arrowsmith, Cheryl H.,Barsyte-Lovejoy, Dalia,Liu, Jing,Vedadi, Masoud,Jin, Jian
, p. 9124 - 9139 (2016/10/22)
Well-characterized selective inhibitors of protein arginine methyltransferases (PRMTs) are invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a fragment-like inhibitor of type I PRMTs, we conducted structure-activity
N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
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Page/Page column 5, (2010/08/18)
This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.
2-aryl indole derivatives and their use as therapeutic agents
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, (2008/06/13)
The present invention relates compounds of the formula (I): wherein R1a, R1b; and R2 represent a variety of substituents; R3 represents an optionally substituted phenyl, biphenyl or naphthyl or heteroaryl group; R4 represents hydrogen, C1-6alkyl, carbonyl (=O), (CH2)pphenyl or a C1-2alkylene bridge across the piperidine ring; R5 and R6 each independently represent a variety of substituents; or R5 and R6 together are linked so as to form an optionally substituted 5-or 6-membered ring; X represents an oxygen or a sulfur atom, two hydrogen atoms, ═NH or ═N(C1-6alkyl); Y is a straight or branched C1-4alkylene, C2-4alkenylene or C2-4alkynylene chain; the dotted line represents an optional double bond; m is zero or an integer from 1 to 4; n is an integer from 1 to 4; and p is an integer from 1 to 4; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
Serine derived NK1 antagonists 2: A pharmacophore model for arylsulfonamide binding
Elliott,Broughton,Cascieri,Chicchi,Huscroft,Kurtz,MacLeod,Sadowski,Stevenson
, p. 1851 - 1856 (2007/10/03)
Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.
