- Identification of Piperidine-3-carboxamide Derivatives Inducing Senescence-like Phenotype with Antimelanoma Activities
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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.
- Oh, Sangmi,Kwon, Do Yoon,Choi, Inhee,Kim, Young Mi,Lee, Ji Young,Ryu, Jiyoung,Jeong, Hangyeol,Kim, Myung Jin,Song, Rita
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p. 563 - 571
(2021/05/06)
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- HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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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.
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Paragraph 000316; 000532
(2016/05/02)
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- Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 40
(2012/08/28)
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- Synthesis and histamine H3 and H4 receptor activity of conformationally restricted cyanoguanidines related to UR-PI376
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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
- Geyer, Roland,Buschauer, Armin
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p. 775 - 785
(2012/03/12)
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- TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 90
(2011/06/11)
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- Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists
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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
- 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
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p. 2724 - 2728
(2007/10/03)
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- NOVEL COMPOUNDS FOR TREATING INFLAMMATORY DISEASES
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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
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Page/Page column 97-98
(2010/11/24)
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- Substituted indolines which inhibit receptor tyrosine kinases
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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.
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Page column 40
(2008/06/13)
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- NOVEL AMIDE COMPOUNDS
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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.
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- DERIVATIVES ...USE AS MEDICAMENTS
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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.
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- Novel synthesis of 4(5)-monosubstituted imidazoles via cycloaddition of tosylmethyl isocyanide to aldimines
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4(5)-Monosubstituted imidazoles (9) have been prepared via base-induced cycloaddition of tosylmethyl isocyanide (TosMIC) to N-(dimethylsulfamoyl)aldimines (2) or N-tosylaldimines (3). In the first case, N-(dimethylsulfamoyl)imidazoles 8 are the initial reaction products, from which the dimethylsulfamoyl group is readily removed with aqueous HBr. In the second case, the tosyl group of 1-tosylimidazoles 10 is lost spontaneously to give 4(5)-monosubstituted imidazoles 9 in one operation.
- Ten Have, Ronald,Huisman, Marco,Meetsma, Auke,Van Leusen, Albert M.
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p. 11355 - 11368
(2007/10/03)
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- The Reaction of Some N-(Nitrophenyl)azoles with Alkali: Preparation of the Corresponding Azoxybenzenes. X-Ray Structure of 2,2'-Bis(1'',2'',4''-triazol-1''-yl)azoxybenzene
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The reactions of some representative N-(nitrophenyl)azoles with boiling aqueous ethanolic potassium hydroxide solution gave the corresponding bis(azolyl)azoxybenzenes.It is deduced that, in these reactions, the N-attached azolyl groups concerned are acting as weak electron-withdrawing groups.The structure of 2,2'-bis(1'',2'',4''-triazol-1''-yl)azoxybenzene was determined in the solid state by X-ray crystallography.The monoclinic crystals belong to the space group P21/c with a 8.815(1), b 7.863(1), c 11.836(1) Angstroem, β 109.96(1) deg and Z 2.The structure was refined to an R index of 0.041 for 1172 observed terms.The midpoint of the exocyclic N=N bond lies on an inversion centre so that the azoxy oxygen is statistically distributed between two sites.The benzene ring atoms are coplanar to within experimental error, as are the triazole ring atoms, and the dihedral angle between the perpendiculars to the two rings is 35.3(3) deg.
- Mackay, Maureen F.,Trantino, Giuseppe J.,Wilshire, John F. K.
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p. 417 - 425
(2007/10/02)
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- Preparation of p-nitrophenyl-imidazoles
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A process for the preparation of imidazoles which are substituted with p-nitrophenyl in the 2- and/or 4- and/or 5-position and may carry additional substituents, by reacting imidazoles which are substituted by phenyl in the 2- and/or 4- and/or 5-position
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- CARBENIC REACTIONS OF 4-DIAZO-4H-IMIDAZOLE WITH BENZENE DERIVATIVES
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The electrophilic behavior of 4H-imidazolylidene is greatly modified by coordinating groups in benzene derivatives undergoing substitution.
- Amick, T. J.,Shechter, H.
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p. 901 - 904
(2007/10/02)
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