103620-87-7Relevant articles and documents
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
Ding, Xiao,Dai, Xuedong,Long, Kai,Peng, Cheng,Andreotti, Daniele,Bamborough, Paul,Eatherton, Andrew J.,Edge, Colin,Jandu, Karamjit S.,Nichols, Paula L.,Philps, Oliver J.,Stasi, Luigi Piero,Wan, Zehong,Xiang, Jia-Ning,Dong, Kelly,Dossang, Pamela,Ho, Ming-Hsun,Li, Yi,Mensah, Lucy,Guan, Xiaoming,Reith, Alastair D.,Ren, Feng
supporting information, p. 4034 - 4038 (2017/08/23)
Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.
COMPOUND HAVING ZNF143 INHIBITORY ACTIVITY AND USE THEREOF
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, (2016/10/27)
PROBLEM TO BE SOLVED: To provide a compound having a ZNF143 inhibitory activity as well as to provide a ZNF143 inhibitory agent and pharmaceutical composition containing the same. SOLUTION: Provided is a compound represented by formula (I) or a salt thereof as well as a ZNF143 inhibitory agent containing the same and a pharmaceutical composition having the same as an active ingredient. A-B-C-D (I)[A is H, a methyl group, a naphthyl group, a phenyl group or a nitrogen-containing heterocyclic ring; B is as shown below, and C is an amide bond or a heteroaromatic ring containing N and O; D is a substituted/unsubstituted phenyl group or a monocyclic heteroaromatic ring containing N or S; and C and D are both fused heterocyclic ring or the like optionally having a substituent group.]. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2016,JPOandINPIT
Aci-reductone compounds belonging to the 6,7-disubstituted-3,4-dihydro benzopyan-2H-one class having antiaggregatory properties
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, (2008/06/13)
The present invention relates to novel benzopyranone aci-reductone compounds of the formula I wherein X and Y are selected from the group comprising H (except that X and Y are not both H, unless otherwise indicated) Cl or other halogen, OH, a straight or
Comparative Antiaggregatory Activity in Human Platelets of a Benzopyranone aci-Reductone, Clofibric Acid, and a 2,3-Dihydrobenzofuran Analogue
Witiak, Donald T.,Kim, Sung K.,Romstedt, Karl,Newman, Howard A. I.,Feller, Dennis R.
, p. 2170 - 2174 (2007/10/02)
A synthetic method for the preparation of aci-reductone 6-chloro-3,4-dihydroxy-2H-1-benzopyran-2-one (3) from 5-chlorosalicylate is presented.In human platelets, the benzopyranone derivative 3, clofibric acid (1), and the 2,3-dihydrobenzofuran analogue 4