88457-32-3Relevant academic research and scientific papers
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors
Murray, Christopher W.,Berdini, Valerio,Buck, Ildiko M.,Carr, Maria E.,Cleasby, Anne,Coyle, Joseph E.,Curry, Jayne E.,Day, James E. H.,Day, Phillip J.,Hearn, Keisha,Iqbal, Aman,Lee, Lydia Y. W.,Martins, Vanessa,Mortenson, Paul N.,Munck, Joanne M.,Page, Lee W.,Patel, Sahil,Roomans, Susan,Smith, Kirsten,Tamanini, Emiliano,Saxty, Gordon
supporting information, p. 798 - 803 (2015/07/15)
The DDR1 and DDR2 receptor tyrosine kinases are activated by extracellular collagen and have been implicated in a number of human diseases including cancer. We performed a fragment-based screen against DDR1 and identified fragments that bound either at th
IMIDAZO-CONDENSED BICYCLES AS INHIBITORS OF DISCOIDIN DOMAIN RECEPTORS (DDRS)
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Page/Page column 90, (2015/02/02)
The invention provides a compound of formula (I) (Formula (I)) or a tautomeric form, stereochemically isomeric form, N-oxide, pharmaceutically acceptable salt or solvate thereof, wherein R2, R3, R4, Ra, Rb
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
Zhao, Guohua,Bolton, Scott A.,Kwon, Chet,Hartl, Karen S.,Seiler, Steven M.,Slusarchyk, William A.,Sutton, James C.,Bisacchi, Gregory S.
, p. 309 - 312 (2007/10/03)
The serine protease tryptase has been associated with a broad range of allergic and inflammatory diseases and, in particular, has been implicated as a critical mediator of asthma. The inhibition of tryptase therefore has the potential to be a valuable therapy for asthma. The synthesis, employing solution phase parallel methods, and SAR of a series of novel 2-azepanone tryptase inhibitors are presented. A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC50=38 nM) with selectivity ≤330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa).
Novel monoazo and disazo colorants from aminoalkylanilines and bis(aminoalkyl)anilines
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, (2008/06/13)
Water-insoluble azo dyestuffs of the formula STR1 and water-soluble acid addition salts thereof useful for coloring natural fibers, synthetic fiber-forming material and cellulosic materials as well as in the manufacture of paper, varnishes, inks, coatings and plastics in which A represents an azoic coupling radical derived from a coupling component selected from the group consisting of arylides of hydroxy-substituted carbocyclic aromatic carboxylic acids, 1-aryl-5-hydroxy-pyrazoles, 6-amino-1-naphthol-3-sulfonic acid, and compounds having an enolizable ketomethylene group of the formula STR2 R is hydrogen, lower-alkyl, lower-alkoxy or halogen; R2 is hydrogen, lower-alkyl, lower-alkoxy, halogen, aminomethyl or 2-aminoethyl with the proviso that A is other than β-naphthol when R2 is aminomethyl or 2-aminoethyl; R1 and R3 are the same or different and are each hydrogen, lower-alkyl, lower-alkoxy, halogen or aminomethyl with the proviso that at least one of R1 and R3 is aminomethyl when R2 is other than aminomethyl or 2-aminoethyl; and n represents an integer whose value is 1 or 2 and corresponds to the number of azo linkages, which dyestuffs are obtained by coupling a diazotized amine of the formula STR3 in which R, R1, R2 and R3 are as defined above with said coupling component.
Monoazo and diazo colorants from aminoalkylanilines and bis(aminoalkyl)anilines
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, (2008/06/13)
Water-insoluble azo dyestuffs of the formula STR1 AND WATER-SOLUBLE ACID ADDITION SALTS THEREOF USEFUL FOR COLORING NATURAL FIBERS, SYNTHETIC FIBER-FORMING MATERIAL AND CELLULOSIC MATERIALS AS WELL AS IN THE MANUFACTURE OF PAPER, VARNISHES, INKS, COATINGS AND PLASTICS IN WHICH A represents an azoic coupling radical derived from a coupling component selected from the group consisting of arylides of hydroxysubstituted carbocyclic aromatic carboxylic acids, 1-aryl-5-hydroxypyrazoles, 6-amino-1-naphthol-3-sulfonic acid, and compounds having an enolizable ketomethylene group of the formula STR2 R is hydrogen, lower-alkyl, lower-alkoxy or halogen; R2 is hydrogen, lower-alkyl, lower-alkoxy, halogen, aminomethyl or 2-aminoethyl with the proviso that A is other than β-naphthol when R2 is aminomethyl or 2-aminoethyl; R1 and R3 are the same or different and are each hydrogen, lower-alkyl, lower-alkoxy, halogen or aminomethyl with the proviso that at least one of R1 and R3 is aminomethyl when R2 is other than aminomethyl or 2-aminoethyl; and n represents an integer whose value is 1 or 2 and corresponds to the number of azo linkages, which dyestuffs are obtained by coupling a diazotized amine of the formula STR3 in which R, R1, R2 and R3 are as defined above with said coupling component.
