- AMIDE DERIVATIVES COMPRISING HETEROCYCLOALKYL RING
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PROBLEM TO BE SOLVED: To provide compounds or pharmacologically acceptable salts thereof that have excellent EP300 and/or CREBBP histone acetyltransferase inhibitory activity. SOLUTION: The invention provides compounds represented by the formula (1) in the figure or pharmacologically acceptable salts thereof. (In the formula (1), ring Q1, ring Q2, ring Q3, X and L are as defined in the specification.) SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT
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Paragraph 0295; 0296; 0298; 0300-0302
(2020/05/20)
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- Phenoxypropanolamine derivatives as selective inhibitors of the 20S proteasome β1 and β5 subunits
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New series of thiophene-containing phenoxypropanolamines were synthesized and evaluated for their potency to inhibit the three proteolytic activities of the mammalian 20S proteasome. Noticeable inhibition of both ChT-L and PA activities was obtained with
- Hovhannisyan, Anna A.,Pham, The Hien,Bouvier, Dominique,Tan, Xiao,Touhar, SiAmmar,Mkryan, Gevorg G.,Dallakyan, Ashot M.,El Amri, Chahrazade,Melikyan, Gagik S.,Reboud-Ravaux, Michèle,Bouvier-Durand, Michelle
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supporting information
p. 5172 - 5178
(2017/11/10)
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- A cascade approach to fused indolizinones through Lewis acid-copper(i) relay catalysis
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A relay catalytic cascade process involving Lewis acid triggered ring-opening of cyclopropyl ketones with nitriles, the copper(i)-catalyzed Ritter process, and acid-promoted N-acyliminium ion cyclization is described, which efficiently provides thieno-, furano-, and benzo-indolizinones in moderate to good yields. The Royal Society of Chemistry 2013.
- Huang, Huawen,Ji, Xiaochen,Wu, Wanqing,Jiang, Huanfeng
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supporting information
p. 3351 - 3353
(2013/06/04)
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- Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor
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The current work discloses a novel cyclohexylarylamine chemotype with potent inhibition of the serotonin, norepinephrine, and dopamine transporters and potential for treatment of major depressive disorder. Optimized compounds 1 (SERT, NET, DAT, IC50 = 169, 85, 21 nM) and 42 (SERT, NET, DAT IC50 = 34, 295, 90 nM) were highly brain penetrant, active in vivo in the mouse tail suspension test at 30 mpk po and were not general motor stimulants.
- Shao, Liming,Hewitt, Michael C.,Wang, Fengjiang,Malcolm, Scott C.,Ma, Jianguo,Campbell, John E.,Campbell, Una C.,Engel, Sharon R.,Spicer, Nancy A.,Hardy, Larry W.,Schreiber, Rudy,Spear, Kerry L.,Varney, Mark A.
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scheme or table
p. 1438 - 1441
(2011/04/16)
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- CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS
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The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
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Page/Page column 69
(2010/11/28)
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- Novel arylcycloalkanepolyalkylamines
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Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.
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