192661-36-2Relevant academic research and scientific papers
DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
-
Paragraph 0710-0712, (2020/12/13)
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.
DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
-
Page/Page column 163, (2019/06/11)
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3- dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for huntington's disease
Bürli, Roland W.,Luckhurst, Christopher A.,Aziz, Omar,Matthews, Kim L.,Yates, Dawn,Lyons, Kathy. A.,Beconi, Maria,McAllister, George,Breccia, Perla,Stott, Andrew J.,Penrose, Stephen D.,Wall, Michael,Lamers, Marieke,Leonard, Philip,Müller, Ilka,Richardson, Christine M.,Jarvis, Rebecca,Stones, Liz,Hughes, Samantha,Wishart, Grant,Haughan, Alan F.,O'Connell, Catherine,Mead, Tania,McNeil, Hannah,Vann, Julie,Mangette, John,Maillard, Michel,Beaumont, Vahri,Munoz-Sanjuan, Ignacio,Dominguez, Celia
supporting information, p. 9934 - 9954 (2014/01/17)
Inhibition of class IIa histone deacetylase (HDAC) enzymes have been suggested as a therapeutic strategy for a number of diseases, including Huntington's disease. Catalytic-site small molecule inhibitors of the class IIa HDAC4, -5, -7, and -9 were developed. These trisubstituted diarylcyclopropanehydroxamic acids were designed to exploit a lower pocket that is characteristic for the class IIa HDACs, not present in other HDAC classes. Selected inhibitors were cocrystallized with the catalytic domain of human HDAC4. We describe the first HDAC4 catalytic domain crystal structure in a "closed-loop" form, which in our view represents the biologically relevant conformation. We have demonstrated that these molecules can differentiate class IIa HDACs from class I and class IIb subtypes. They exhibited pharmacokinetic properties that should enable the assessment of their therapeutic benefit in both peripheral and CNS disorders. These selective inhibitors provide a means for evaluating potential efficacy in preclinical models in vivo.
HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
-
Page/Page column 71, (2012/08/08)
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
CEPHEM COMPOUNDS
-
Page 26-27, (2010/02/09)
The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl which may have suitable substituent(s), R2 is amino, protected amino or guanidino, R3 is carboxy or protected carboxy, R4 /sup
AGENT FOR PREVENTING OR TREATING NEUROPATHY
-
Page/Page column 161-162, (2010/02/06)
The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula:wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s);B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;X is a divalent acyclic hydrocarbon group;Z is -O-, -S-, -NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group);Y is a bond or a divalent acyclic hydrocarbon group;R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be -O-, or a salt thereof.
Piperazine derivatives as tachykinin antagonists
-
, (2008/06/13)
PCT No. PCT/JP96/03641 Sec. 371 Date Jun. 18, 1998 Sec. 102(e) Date Jun. 18, 1998 PCT Filed Dec. 12, 1996 PCT Pub. No. WO97/22597 PCT Pub. Date Jun. 26, 1997
