38980-93-7Relevant academic research and scientific papers
Identification of Piperidine-3-carboxamide Derivatives Inducing Senescence-like Phenotype with Antimelanoma Activities
Oh, Sangmi,Kwon, Do Yoon,Choi, Inhee,Kim, Young Mi,Lee, Ji Young,Ryu, Jiyoung,Jeong, Hangyeol,Kim, Myung Jin,Song, Rita
, p. 563 - 571 (2021/05/06)
This study evaluated the potential use of senescence-inducing small molecules in the treatment of melanoma. We screened commercially available small-molecule libraries with high-throughput screening and high-content screening image-based technology. Our findings showed an initial hit with the embedded N-arylpiperidine-3-carboxamide scaffold-induced senescence-like phenotypic changes in human melanoma A375 cells without serious cytotoxicity against normal cells. A focused library containing diversely modified analogues were constructed and examined to evaluate the structure-activity relationship of N-arylpiperidine-3-carboxamide derivatives starting from hit 1. This work identified a novel compound with remarkable antiproliferative activity in vitro and demonstrated the key structural moieties within.
HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000316; 000532, (2016/05/02)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Page/Page column 40, (2012/08/28)
Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
Synthesis and histamine H3 and H4 receptor activity of conformationally restricted cyanoguanidines related to UR-PI376
Geyer, Roland,Buschauer, Armin
, p. 775 - 785 (2012/03/12)
Recently, we identified highly potent agonists of the human histamine H4 receptor (hH4R) among a series of imidazolylbutylcyanoguanidines. Aiming at improved selectivity for the hH 4R relative to the H3 receptor
TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page/Page column 90, (2011/06/11)
Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists
Ho, Koc-Kan,Auld, Douglas S.,Bohnstedt, Adolph C.,Conti, Paolo,Dokter, Wim,Erickson, Shawn,Feng, Daming,Inglese, Jim,Kingsbury, Celia,Kultgen, Steven G.,Liu, Rong-Qiang,Masterson, Christopher M.,Ohlmeyer, Michael,Rong, Yajing,Rooseboom, Martijn,Roughton, Andrew,Samama, Philippe,Smit, Martin-Jan,Son, Ellen,van der Louw, Jaap,Vogel, Gerard,Webb, Maria,Wijkmans, Jac,You, Ming
, p. 2724 - 2728 (2007/10/03)
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the o
NOVEL COMPOUNDS FOR TREATING INFLAMMATORY DISEASES
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Page/Page column 97-98, (2010/11/24)
The invention relates to novel compounds of formula (1), heteroderivatives thereof, and pharmacologically compatible salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, that are suitable for treating respiratory or gastrointestinal
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 40, (2008/06/13)
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
NOVEL AMIDE COMPOUNDS
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, (2008/06/13)
A compound of the formula (I):R1-A-X-NHCO-Y-R2 ???whereinR1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents,R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents,A is a group of the formula:-(CH2)t-(O)m- or in which R3 and R4 are each hydrogen or linked together to form imino,R5 is hydrogen or lower alkyl,t is 0, 1 or 2,p, m and n are each 0 or 1,X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents,Y is bond, lower alkylene, or lower alkenylene, and a salt thereof.
DERIVATIVES ...USE AS MEDICAMENTS
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, (2008/06/13)
A subject of the invention is, as new chemical products, the compounds of formula (I) in which X represents a hydrogen atom or a halogen atom and Z represents a hydrogen atom or the remainder of an acid as well as their addition salts with acids. The compounds of formula (I) have antibiotic properties.
