84467-19-6Relevant academic research and scientific papers
Oxadiazole Amine Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the same
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Paragraph 1088-1091, (2017/07/18)
The present invention relates to a novel compound having an activity of inhibiting histone deacetylase 6 (HDAC6), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a use thereof for preparation of a drug for treatment, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing the same. The novel compound, an optical isomer thereof or a pharmaceutically acceptable salt thereof according to the present invention has an activity of inhibiting histone deacetylase 6 (HDAC6), and is effective for preventing or treating HDAC6-related diseases, including infectious diseases; neoplasm; endocrine, nutritional and metabolic diseases; mental and behavior disorders; nerve disorders; eye and adnexa diseases; cardiovascular diseases; respiratory diseases; digestive organ diseases; skin and subcutaneous tissue diseases; musculoskeletal and connective tissue diseases; or congenital malformation, deformation and chromosomal abnormality.COPYRIGHT KIPO 2017
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists
Gomtsyan, Arthur,Schmidt, Robert G.,Bayburt, Erol K.,Gfesser, Gregory A.,Voight, Eric A.,Daanen, Jerome F.,Schmidt, Diana L.,Cowart, Marlon D.,Liu, Huaqing,Altenbach, Robert J.,Kort, Michael E.,Clapham, Bruce,Cox, Phil B.,Shrestha, Anurupa,Henry, Rodger,Whittern, David N.,Reilly, Regina M.,Puttfarcken, Pamela S.,Brederson, Jill-Desiree,Song, Ping,Li, Bin,Huang, Susan M.,McDonald, Heath A.,Neelands, Torben R.,McGaraughty, Steve P.,Gauvin, Donna M.,Joshi, Shailen K.,Banfor, Patricia N.,Segreti, Jason A.,Shebley, Mohamad,Faltynek, Connie R.,Dart, Michael J.,Kym, Philip R.
, p. 4926 - 4947 (2016/06/13)
Transient receptor potential vanilloid 3 (TRPV3) is a Ca2+- and Na+-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recent studies suggest that TRPV3 may play a role in inflammation, pain sensation, and skin disorders. TRPV3 studies have been challenging, in part due to a lack of research tools such as selective antagonists. Herein, we provide the first detailed report on the development of potent and selective TRPV3 antagonists featuring a pyridinyl methanol moiety. Systematic optimization of pharmacological, physicochemical, and ADME properties of original lead 5a resulted in identification of a novel and selective TRPV3 antagonist 74a, which demonstrated a favorable preclinical profile in two different models of neuropathic pain as well as in a reserpine model of central pain.
Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor
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.
scheme or table, p. 1438 - 1441 (2011/04/16)
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.
PYRROLIDINE TRIPLE REUPTAKE INHIBITORS
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Page/Page column 49; 54, (2010/08/18)
In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including 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.
Process for the preparation of 1-aryl-1-cyanocyclobutane derivatives
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, (2008/06/13)
A process for the preparation of arylcyclobutylnitrile derivatives which involves reaction of a solution of a 1,3-dihalopropane and a cyanobenzyl derivative in a substantialy dimethyl sulphoxide-free solvent with a suspension of a base in a substantially dimethyl sulphoxide-free solvent at a temperature of at least 35° C.
Therapeutic agents
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, (2008/06/13)
Compounds of formula I STR1 in which R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R2 is H or C1-3 alkyl; R3 and/or R4 are H, formyl, C1-3 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-7 cycloalkyl or R3 and R4 together with the nitrogen atom form a heterocyclic ring system; R5 and/or R6 are H, halo, CF3, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylthio or R5 and R6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
Arylcyclobutylalkylamines and anti-depression composition and methods using same
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, (2008/06/13)
Compounds of formula I STR1 in which R1 is H or C1-3 alkyl; R2 is H or C1-3 alkyl; R3 and/or R4 are H, C1-3 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-7 cycloalkyl or R3 and R4 together with the nitrogen atom form a heterocyclic ring system; R5 and/or R6 are H, halo, CF3, or C1-3 alkyl (with the proviso that R5 and R6 cannot both be H or methyl) or R5 and R6 together with the carbon atoms to which they are attached form a second benzene ring and R7 and/or R8 are H or C1-3 alkyl show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
