- HISTONE DEACETYLASE INHIBITORS
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Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
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Paragraph 00172; 00173
(2018/07/29)
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- CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER
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[Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)
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Page/Page column 28
(2010/12/29)
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- 1-Substituted 4-(3-Hydroxyphenyl)piperazines are pure opioid receptor antagonists
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This report describes the discovery that 1-substituted 4-(3-hydroxyphenyl) piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine and (3R)-3-methyl-4-(3-hydroxyphenyl)piperazine, both of which display low nanomolar potencies at μ, δ, and κ receptors and pure antagonist properties in a [35S]GTPγS assay.
- Carroll, F. Ivy,Cueva, Juan Pablo,Thomas, James B.,Mascarella, S. Wayne,Runyon, Scott P.,Navarro, Hernan A.
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scheme or table
p. 365 - 369
(2010/11/18)
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- Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles
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Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38α MAP kinase inhibitors are described. Biological evaluation of these compounds focused on maintaining activity while improving pharmacokinetic (PK) properties. Improved properties were observed for structures bearing substitutions on the benzylic methylene.
- Tan, Xuefei,Tester, Richland W.,Luedtke, Gregory R.,Chakravarty, Sarvajit,Mavunkel, Babu J.,Perumattam, John J.,Lu, Qing,Nashashibi, Imad,Jung, Joon,Hu, Jie,Liclican, Albert,Almirez, Ramona,Tabora, Jocelyn,Tran, Vinh,Laney, Maureen,Levy, Daniel E.,Dugar, Sundeep
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scheme or table
p. 828 - 831
(2010/06/13)
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- Indole-type derivatives as inhibitors of p38 kinase
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The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
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Page/Page column 29
(2008/06/13)
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