- 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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- MANUFACTURING METHOD OF OPTICALLY ACTIVE CARBINOL COMPOUND
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PROBLEM TO BE SOLVED: To provide a manufacturing method of an optically active carbinol compound having LXRβ activation action and a manufacturing intermediate thereof. SOLUTION: A manufacturing method of an optically active compound represented by the formula (1) comprises manufacturing a 2-(4-(2,5-dimethylpiperazin-1-yl)-3-propylphenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol compound which is an important optically active intermediate. COPYRIGHT: (C)2015,JPOandINPIT
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- ARYLPIPERAZINE OPIOID RECEPTOR ANTAGONISTS
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Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
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Page/Page column 14
(2012/12/13)
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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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- 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 27
(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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- Micelles for delivery of nitric oxide
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We designed block copolymer pro-amphiphiles and amphiphiles for providing very long-term release of nitric oxide (NO). A block copolymer of N-acryloylmorpholine (AM, as a hydrophile) and N-acryloyl-2,5-dimethylpiperazine (AZd, as a hydrophilic precursor) was synthesized. The poly(N-acryloyl-2,5- dimethylpiperazine) (PAZd) is water-soluble, but chemical reaction of the secondary amines with NO to form a N-diazeniumdiolate (NONOate) converts the hydrophilic PAZd into a hydrophobic poly(sodium-1-(N-acryloyl-2,5- dimethylpiperazin-1-yl)diazen-1-ium-1,2-diolate) (PAZd·NONOate), driving aggregation. The PAM block guides this process toward micellization, rather than precipitation, yielding ca. 50 nm spherical micelles. The hydrophobic core of the micelle shielded the NONOate from the presence of water, and thus protons, which are required for NO liberation, delaying release to a remarkable 7 d half-life. Release of the NO returned the original soluble polymer. The very small NO-loaded micelles were able to penetrate complex tissue structures, such as the arterial media, opening up a number of tissue targets to NO-based therapy.
- Jo, Yun Suk,Van Der Vlies, Andrej,Gantz, Jay,Thacher, Tyler N.,Antonijevic, Sasa,Cavadini, Simone,Demurtas, Davide,Stergiopulos, Nikolaos,Hubbell, Jeffrey A.
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supporting information; experimental part
p. 14413 - 14418
(2010/02/16)
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- KINASE INHIBITORS
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The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.
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Page/Page column 15
(2010/11/27)
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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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- Enantioconvergent synthesis of (-)-(2R,5S)-1-allyl-2,5-dimethylpiperazine, an intermediate to δ-opioid receptor ligands
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A convenient, high-yield enantioconvergent synthesis of (-)-1-allyl-(2S,5R)-dimethylpiperazine from trans-2,5-dimethylpiperazine has been developed. This compound is an important intermediate in the synthesis of Δ-opioid receptor ligands. The process allows for the laboratory preparation of 100 g quantities of this enantiomerically pure diamine without chromatography. The key steps in the sequence were an efficient optical resolution using relatively inexpensive resolving agents, followed by interconversion of the unwanted (+)-enantiomer into the desired (-)-enantiomer.
- Janetka, James W.,Furness, M. Scott,Zhang, Xiaoyan,Coop, Andrew,Folk, John E.,Mattson, Mariena V.,Jacobson, Arthur E.,Rice, Kenner C.
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p. 3976 - 3980
(2007/10/03)
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- Fused imidazopyridine derivatives as antihyperlipidemic agents
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A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring; One of R0, R1and R2is —Y0—Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group; Y0is a bond or an optionally substituted bivalent hydrocarbon group; Z0is a basic group which may be bonded via oxygen, nitrogen, —CO—, —CS—, —SO2N(R3)— (where R3is hydrogen or an optionally substituted hydrocarbon group), or S(O)n(wherein n is to 0, 1 or 2); .........is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.
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