1004-74-6Relevant articles and documents
Imidazopyridine- and purine-thioacetamide derivatives: Potent inhibitors of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1)
Chang, Lei,Lee, Sang-Yong,Leonczak, Piotr,Rozenski, Jef,De Jonghe, Steven,Hanck, Theodor,Müller, Christa E.,Herdewijn, Piet
, p. 10080 - 10100 (2014)
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) belongs to the family of ecto-nucleotidases, which control extracellular nucleotide, nucleoside, and (di)phosphate levels. To study the (patho)physiological roles of NPP1 potent and selective inhibitors with drug-like properties are required. Therefore, a compound library was screened for NPP1 inhibitors using a colorimetric assay with p-nitrophenyl 5′-thymidine monophosphate (p-Nph-5′-TMP) as an artificial substrate. This led to the discovery of 2-(3H-imidazo[4,5-b]pyridin-2-ylthio)-N-(3,4-dimethoxyphenyl)acetamide (5a) as a hit compound with a Ki value of 217 nM. Subsequent structure-activity relationship studies led to the development of purine and imidazo[4,5-b]pyridine analogues with high inhibitory potency (Ki values of 5.00 nM and 29.6 nM, respectively) when assayed with p-Nph-5′-TMP as a substrate. Surprisingly, the compounds were significantly less potent when tested versus ATP as a substrate, with Ki values in the low micromolar range. A prototypic inhibitor was investigated for its mechanism of inhibition and found to be competitive versus both substrates.
1,3-Dihydroxybenzene derivatives and colorants containing said compounds
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, (2008/06/13)
1,3-Dihydroxybenzene derivatives of general formula (I) or (Ia) or physiologically tolerated, water-soluble thereof wherein R′1 denotes substituted pyridyl group, a pyrimidyl group, a group of formula (IIa) or (IIIa) and the dyeing agents for keratin fibers containing these compounds.
One step hair coloring compositions using salts
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, (2008/06/13)
A hair coloring composition comprising the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an amino phenol, a naphthol, a polyhydric phenol, a catechol and mixtures thereof; wherein the composition comprising one or more oxidative hair coloring agents further comprises al least one water soluble carbonate releasing salts; and optionally a water soluble ammonium salt, is described.
Transition metal complexes as dye forming catalysts in hair coloring compositions
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, (2008/06/13)
A hair coloring composition comprising a first composition which comprises: (a) a dye forming transition metal salt or complex; which is first applied to the hair; and a second composition which comprises the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an aminophenol, a polyhydric phenol a catechol and mixtures thereof.
Enhanced color deposition for hair with sequestering agents
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, (2008/06/13)
Hair coloring compositions which comprise: (A) non-nitrogenous chelating agents from the group consisting of polyphosphate; phosphonates; hydroxycarboxylates; polyacrylates; zeolite; and mixtures thereof; (B) an oxidative dye primary intermediate; and (C) an oxidative dye coupler; (D) and water are described. The present invention also relates to a method for coloring hair which comprises contacting said hair with a hair coloring composition as described above.
1,4-diazacycloheptane derivatives and their use in hair oxidation dyes
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, (2008/06/13)
A 1,4-diazacycloheptane derivative and an oxidative hair colorant containing the derivative as a primary intermediate is presented. The 1,4-diazacycloheptane derivative is of the formula: STR1 where R1, R2, R3 and R4 independently of one another represent hydrogen, a C1-4 alkyl or hydroxyalkyl group or a C2-4, dihydroxyalkyl group, X and Y independently of one another represent hydrogen, chlorine, fluorine, a C1-4 alkyl, hydroxyalkyl, aminoakyl or alkoxy group, a C2-4 dihydroxyalkyl group or an allyl group and R5 and R6 independently of one another represent hydrogen or a C1-4 alkyl group. Natural color tones can be obtained in keratin fibers with oxidative hair colorants containing the 1,4-diazacycloheptane derivative, without the use of additional primary intermediates.
Hair dye composition
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, (2008/06/13)
Hair dye compositions based on oxidation hair dyes which contain developer components, coupling components and oxidation components, characterized in that they contain one or more aminopyrrole derivatives of the formula: STR1
Hair dyeing agents
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, (2008/06/13)
New coupling or shading (nuance) components are described which in combination with pertinent developers are used for dyeing of hair. These coupling components are dinitropyridine derivatives of the general formula: STR1 whereby the substituents X, Y, Rs
Oxidation hair dyes comprising resorcinol derivatives as coupling components
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, (2008/06/13)
This invention is directed to compositions of the developer-coupler type of the dyeing of hair consisting essentially of resorcinol derivatives or salts thereof as coupling components and, as developer components, the conventional components used in oxida
Pteridines, LXIX. Synthesis and Reactivity of 2,4-Diamino-6-(hydroxymethyl)pteridine
Boyle, Peter H.,Pfleiderer, Wolfgang
, p. 1514 - 1523 (2007/10/02)
Condensation of 2,4,5,6-tetraaminopyridine (2) with 1,3-dihydroxyacetone in the presence of gaseous oxygen, rather than air, resulted in 2,4-diamino-6-(hydroxymethyl)pteridine (3) virtually uncontaminated with 2,4-diamino-6-methylpteridine (4).Acetylation of 3 led to 6-acetoxymethyl-2,4-bis(acetylamino)pteridine (5) which turned out to be very labile forming various di- and monoacetyl derivatives (6, 7, 9, 10) on mild hydrolytic conditions.Their structures are proven by physical-chemical means.Silylation of 3 to the tris(trimethylsilyl) derivative 11 followed by treatment with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose (12) and 1,2,3,4,6-penta-O-acetyl-β-D-glucopyranose (15), respectively, in the presence of boron trifluoride,led to selective formation of the corresponding acylated 2,4-diamino-6-pteridinyl O-glycosides 13 and 15, respectively.Deacylations of these afforded the free O-glycosides 14 and 17 which have been characterized by UV- and NMR spectra as well as pKa measurements.
