- Hydrogen peroxide-responsive nitrogen mustard anti-tumor pro-drug and preparation method thereof
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The invention discloses a hydrogen peroxide-responsive nitrogen mustard anti-tumor pro-drug and a preparation method thereof, and belongs to the field of pharmaceutical chemistry. The compound contains an alpha-ketoamide structure and a nitrogen mustard structure, can rapidly respond to H2O2, can be used as the nitrogen mustard anti-tumor pro-drug, has good response effect to H2O2, has high cell selectivity and small toxic and side effects, provides an effective, safe and highly selective anti-tumor drug, enriches the types of nitrogen mustard anti-tumor drugs, and has a good market prospect.
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- 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
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- 1,3-Dihydroxybenzene derivatives and colorants containing said compounds
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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.
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- One step hair coloring compositions using salts
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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.
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- Synthesis and antiproliferative activity of some new DNA-targeted alkylating pyrroloquinolines
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Two novel DNA-direct alkylating agents, consisting of aniline mustard linked to an angular 3H-pyrrolo[3,2-f]quinoline nucleus, were synthetized and assayed for their in vitro antiproliferative activity. Simple convergent synthesis, consisting of separate preparation of 9-chloro-3H-pyrrolo[3,2-f] quinoline and p-amino-aniline derivatives, and following their linkage by substitution reactions 8a, b and 10, yielded the corresponding diol derivatives 7b and 9. Biological properties were evaluated with respect to cell growth inhibition, ability to form cross-links with DNA, and capacity to give rise to a molecular complex with the macromolecule for 7b, 8b, 9 and 10.
- Ferlin,Via, L. Dalla,Gia
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p. 771 - 777
(2007/10/03)
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- Transition metal complexes as dye forming catalysts in hair coloring compositions
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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.
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- Enhanced color deposition for hair with sequestering agents
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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.
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- Means and method for dying keratinic fibers
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Composition for coloring keratin fibers based on a developer-coupler combination characterized in that it contains as the coupler 3-(2,4-diaminophenoxy)-1-propanol and as the developer a p-phenylenediamine derivative monosubstituted on the benzene ring and having general formula (I) ?and/or a 4,5-diamino-1H-pyrazole derivative of general formula (II) ?and/or a p-aminophenol derivative of general formula (III) ?as well as a method for the oxidative coloring of hair, and the use of said composition.
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- 1,4-diazacycloheptane derivatives and their use in hair oxidation dyes
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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.
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- Process for dyeing keratinous fibers with aminoindoles and oxidation dye precursors at basic Ph's and dyeing agents
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The invention relates to a process for dyeing keratinous fibres, which consists in applying to these fibres a composition containing, in a suitable medium for dyeing, at least one coupler of formula: STR1 where R1 denotes hydrogen or alkyl, R2 and R3 denote hydrogen, alkyl, COOR' where R' is alkyl or hydrogen, at least one of the groups R2 and R3 denoting hydrogen, R4 denotes hydrogen, alkyl, hydroxyalkyl, polyhydroxyalkyl or aminoalkyl, Z1 and Z2 denote hydrogen, alkyl, hydroxyl, halogen, alkoxy, at least one of the groups Z1 and Z2 is other than hydrogen at least one oxidation dye precursor, at least one oxidizing agent, the pH of the composition applied to the fibres being higher than 7.
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- Methods for dyeing keratinous fibers with compositions which contain aminoindole couplers, oxidation dye precursors, and oxidizing agents at acid pHs
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A method for dyeing keratin fibers, wherein a composition is applied to said fibers which contains, in a suitable dyeing medium, at least one coupler having formula (I) STR1 wherein R1 is hydrogen or alkyl; R2 and R3 are hydrogen, alkyl, COOR', where R' is alkyl or hydrogen; R4 is hydrogen, hydroxyalkyl, alkyl, polyhydroxyalkyl or acetyl or aminoalkyl wherein the amine may be mono- or disubstituted by alkyl; Z1 and Z2 are hydrogen, alkyl, hydroxy, halogen, alkoxy or a salt thereof; at least one precursor of an oxidation hair dye; and at least one oxidizing agent, the pH of the composition applied to the fibers being less than 7.
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- 3-substituted para-aminophenols
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The invention concerns the use of a 3-substituted para-aminophenol as an oxidation dye precursor for dyeing keratinous fibres, in particular human hair. The 3-substituted para-aminophenol has formula: STR1 where R1 represents alkyl, alkenyl, mono- or polyhydroxyalkyl, nitrile, cyanoalkyl, halogenoalkyl, aminoalkyl or alkoxyalkyl and R2 represents hydrogen, alkyl or mono- or polyhydroxyalkyl, provided that when R2 is hydrogen R1 is not methyl or trifluoromethyl, and to addition salts thereof with an acid. The invention also concerns dye compositions containing compound (I). The invention further concerns novel 3-substituted para-aminophenols.
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- Oxidation dye composition for keratinous fibres comprising a para-aminophenol, a meta-aminophenol and a para-phenylenediamine and/or a bis(phenylalkylenediamine)
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The invention relates to a dyeing composition for keratinous fibres and in particular for human keratinous fibres such as hair, comprising, in a suitable media for dyeing, at least one oxidation dye precursor chosen from 3-methyl-para-aminophenol, 2-methyl-para-aminophenol and 2-hydroxymethyl-para-aminophenol, and their addition salts with an acid; at least one coupling agent chosen from the 2-methyl-5-aminophenols of formula (I): STR1 in which R is methyl, ethyl, β-hydroxyethyl or γ-hydroxypropyl, and their addition salts with an acid; and at least one para-phenylenediamine and/or one bis(phenylalkylenediamine) or one of their addition salts with an acid as oxidation dye precursor.
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- Process for dyeing keratinous fibers with 2,4-diamino-1,3-dimethoxybenzene at an acid ph and compositions employed
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Process for dyeing keratinous fibres, especially human keratinous fibres such as the hair, characterised in that a composition containing, in a medium suitable for dyeing, at least 2,4-diamino-1,3-dimethoxybenzene as a coupler; an oxidation dye precursor; and an oxidising agent; is applied to these fibres, the pH of the composition applied to the fibres being less than 7.
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- Metaphenylenediamines in dyeing compositions for keratinic fibers
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Dye compositions comprising a coupler having to the formula STR1 in which formula R1 and R2 are identical or different and represent a hydrogen atom or an alkyl radical having 1 to 2 carbon atoms and n represents a number equal to 1 or 2 and a paraphenylenediamine. This coupler is particularly suitable for use in a dyeing composition comprising paraphenylenediamines responding to the formula STR2 or the corresponding acid salts; formula in which R1, R2 and R3 are identical or different and represent a hydrogen atom, an alkyl or alkoxy radical having 1 to 2 carbon atoms, R4 and R5 are identical or different and represent a hydrogen atom, a alkyl radical, hydroxyalkyl, alkoxyalkyl in which the alkoxy group comprises 1 to 2 carbon atoms, carbamylalkyl, mesylaminoalkyl, acetylaminoalkyl, ureidoaminoalkyl, carbethoxyaminoalkyl, the alkyl groups in R4 and R5 having 1 to 3 carbon atoms, with the reservation that R1 or R3 represents hydrogen when R4 and R5 do not represent a hydrogen atom.
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- Oxidative hair dye compositions
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Oxidative hair dye composition containing as "para component" compounds of the formula: SPC1 Or their acid addition salts, in which: R1 is alkyl or hydroxyalkyl; R2 is hydrogen or hydroxyalkyl; R3 is hydrogen, alkyl, alkoxy or halogen; and R4 occupies any one of the remaining positions on the benzene radical and is hydrogen, alkyl, alkoxy or halogen; providing that R2 is hydrogen when R3 is alkyl, alkoxy or halogen and providing that at least two of R1, R2, R3 or R4 are other than hydrogen.
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