93469-29-5Relevant academic research and scientific papers
Compounds and methods for treating diseases mediated by protease activated receptors
-
, (2016/09/26)
The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.
Discovery of 1,3-diaminobenzenes as selective inhibitors of platelet activation at the PAR1 receptor
Dockendorff, Chris,Aisiku, Omozuanvbo,Verplank, Lynn,Dilks, James R.,Smith, Daniel A.,Gunnink, Susanna F.,Dowal, Louisa,Negri, Joseph,Palmer, Michelle,MacPherson, Lawrence,Schreiber, Stuart L.,Flaumenhaft, Robert
, p. 232 - 237 (2012/05/04)
A high-throughput screen of the NIH-MLSMR compound collection, along with a series of secondary assays to identify potential targets of hit compounds, previously identified a 1,3-diaminobenzene scaffold that targets protease-activated receptor 1 (PAR1). We now report additional structure-activity relationship (SAR) studies that delineate the requirements for activity at PAR1 and identify plasma-stable analogues with nanomolar inhibition of PAR1-mediated platelet activation. Compound 4 was declared as a probe (ML161) with the NIH Molecular Libraries Program. This compound inhibited platelet aggregation induced by a PAR1 peptide agonist or by thrombin but not by several other platelet agonists. Initial studies suggest that ML161 is an allosteric inhibitor of PAR1. These findings may be important for the discovery of antithrombotics with an improved safety profile.
Reactive dyestuffs comprising a triazine moiety and a vinylsulfonyl moiety both being linked by a substituted alkylene bridge member
-
, (2008/06/13)
A reactive dye of the formula STR1 in which: F is a radical selected from the group consisting of metal-free or metal-containing monoazo or disazo dyes containing at least one --SO3 H group, anthraquinone dyes, sulfophthalocyanine dyes, formazan dyes, phenazine dyes, oxazine dyes and nitroaryl dyes, R is hydrogen, C1 -C4 alkyl which is unsubstituted or substituted with --COOH or --SO3 H, cyanoethyl, or hydroxyethyl, X is fluorine, chlorine, bromine, --SO3 H, phenylsulfonyl or C1 -C4 -alkylsulfonyl, p is 1 or 2 and A is a radical of the formula STR2 in which: Y is chlorine, bromine, fluorine, --OH, --OSO3 H, --O-acyl, --CN, --COOH, --COO--C1 -C4 -alkyl, --CONH2 or --SO2 --Z, the group designated "alk" is a straight or branched polymethylene radical having 2 to 6 carbon atoms, V is STR3 hydrogen or C1 -C4 -alkyl which is unsubstituted or substituted by C1 -C2 -alkoxy, carboxyl, sulfo, halogen or hydroxy, Z is β-halogenoethyl, vinyl or β-acetoxyethyl, or A is a radical of the formulae STR4 in all of which R' is C1-6 -alkyl or hydrogen, Z is as defined above, o is 0 to 6, and m is 2 to 6.
Triazinyl reactive dyes containing additional fiber reactive groups bound through the sulfonylalkylaminoalkylamino bridge
-
, (2008/06/13)
The invention relates to novel useful reactive dyes of the formula I STR1 in which: F is a radical selected from the group consisting of metal-free or metal-containing monoazo or disazo dyes containing at least one --SO3 H group, anthraquinone dyes, sulfophthalocyanine dyes, formazan dyes, phenazine dyes, oxanine dyes and nitroaryl dyes, R is hydrogen, C1 -C4 alkyl which is unsubstituted or substituted with --COOH or --SO3 H, cyanoethyl, or hydroxyethyl, X is fluorine, chlorine, bromine, --SO3 H, phenylsulfonyl or C1 -C4 -alkylsulfonyl, P is 1 or 2 and A is a radical of the formula STR2 in which: the groups designated "alk" are independently of each other straight or branched polymethylene radicals having 2 to 6 carbon atoms, and Z is β-halogenoethyl, vinyl, β-sulfatoethyl, β-thiosulfatoethyl or βacetoxyethyl.
Synthesis and Spectral Characterization of Blue Dyes of the Benzene Series
Thiel, W.,Mayer, R.,Jauer, E.-A.,Modrow, H.,Dost, H.
, p. 497 - 514 (2007/10/02)
53 Donor-acceptor substituted azo dyes of the benzene series were prepared by diazonium-coupling reactions (1a-s) or halogen-cyanide exchange (->2a-x, 3a-j).Described are the preparation of the amines 4a-m and the coupling compounds 5a-t and the procedure of diazotizing and coupling.The colouristic and spectroscopic data show that compounds of the general formula 1 are excellent brilliant blue azo dyes usefull for dyeing polyester material.
