194032-41-2Relevant articles and documents
HISTONE DEACETYLASE INHIBITORS
-
Paragraph 00172; 00173, (2018/07/29)
Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
MANUFACTURING METHOD OF OPTICALLY ACTIVE CARBINOL COMPOUND
-
, (2016/11/14)
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
ARYLPIPERAZINE OPIOID RECEPTOR ANTAGONISTS
-
Page/Page column 14, (2012/12/13)
Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.
CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER
-
Page/Page column 27, (2010/12/29)
[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.)
Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles
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
scheme or table, p. 828 - 831 (2010/06/13)
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.
1-Substituted 4-(3-Hydroxyphenyl)piperazines are pure opioid receptor antagonists
Carroll, F. Ivy,Cueva, Juan Pablo,Thomas, James B.,Mascarella, S. Wayne,Runyon, Scott P.,Navarro, Hernan A.
scheme or table, p. 365 - 369 (2010/11/18)
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.
Micelles for delivery of nitric oxide
Jo, Yun Suk,Van Der Vlies, Andrej,Gantz, Jay,Thacher, Tyler N.,Antonijevic, Sasa,Cavadini, Simone,Demurtas, Davide,Stergiopulos, Nikolaos,Hubbell, Jeffrey A.
supporting information; experimental part, p. 14413 - 14418 (2010/02/16)
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.
KINASE INHIBITORS
-
Page/Page column 15, (2010/11/27)
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.
Indole-type derivatives as inhibitors of p38 kinase
-
Page/Page column 29, (2008/06/13)
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.
Enantioconvergent synthesis of (-)-(2R,5S)-1-allyl-2,5-dimethylpiperazine, an intermediate to δ-opioid receptor ligands
Janetka, James W.,Furness, M. Scott,Zhang, Xiaoyan,Coop, Andrew,Folk, John E.,Mattson, Mariena V.,Jacobson, Arthur E.,Rice, Kenner C.
, p. 3976 - 3980 (2007/10/03)
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.
