- JNK inhibitor as well as pharmaceutical composition and application thereof
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The invention provides a compound represented by a formula (I), racemates, stereoisomers, tautomers, isotope markers, solvates, polymorphic substances, nitrogen oxides, or pharmaceutically acceptablesalts thereof, and application as a JNK inhibitor. The invention also provides a preparation method of the compound shown in the formula (I), a pharmaceutical composition containing the compound shownin the formula (I), and application of the compound shown in the formula (I) to preparation of a medicine, and the medicine is used for treating diseases which can be treated by inhibiting the activity of JNK.
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Paragraph 0541-0545
(2021/03/31)
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- 2 - (amino) ethyl methyl sulphone salt and wherein the intermediate preparation method
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The invention discloses a preparation method of a 2-(amino)ethyl methyl sulfone salt represented by formula 1. The preparation method comprises: (1) in an organic solvent and under the action of a substitution reaction catalyst, a compound 3 is reacted with a compound 4; and X is a halogen, and M is an alkali metal or an alkaline earth metal; and (2) a compound 2 prepared by the step (1) is reacted with an acidic aqueous solution to obtain a compound 1; n is equal to 1 or 2; m is equal to 1 or 2; and HmA is an organic acid or an inorganic acid. The invention also discloses a preparation method of the compound 2. The preparation method of the compound 2 comprises: 1) in an organic solvent and under the action of an alkali, a compound 5 is reacted with a halogenation reagent; and 2) in the organic solvent, under the action of the substitution reaction catalyst, the compound 4 is reacted with the compound 3 prepared by the step 1), X is a halogen, and M is an alkali metal or an alkaline earth metal. The preparation methods have low cost and easy availability of raw materials, have no environmental pollution factors, and are suitable for industrial mass production.
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Paragraph 0037; 0038
(2017/02/28)
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- HETEROCYCLIC COMPOUND
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The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
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Paragraph 0590
(2015/01/18)
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- Kinase inhibitor compounds
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The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
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Page/Page column 42
(2009/04/24)
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- KINASE INHIBITOR COMPOUNDS
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The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
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Page/Page column 83
(2008/06/13)
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- THE CHEMISTRY OF 1,1'-THIOBIS(2-CHLOROETHANE) (SULPHUR MUSTARD) PART I: SOME SIMPLE DERIVATIVES
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Some derivatives of 1,1'-thiobis(2-chloroethane) (sulphur mustard) have been synthesized for use as reference compounds in a wide range of studies embracing analysis, metabolism, environmental degradation and decontamination.Compounds include products formed by hydrolysis, substitution and elimination reactions and their oxidised sulphoxide and sulphone analogues.A comprehensive series of methylthio, methylsulphinyl and methylsulphonyl derivatives has been synthesised in support of metabolic studies. Key words: Thiobis(2-chloroethane) and derivatives; analysis; metabolism; environmental degradation; decontamination
- Black, R. M.,Brewster, K.,Harrison, J. M.,Stansfield, N.
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- ANODIC OXIDATION OF 1,n-HALO(ALKYLTHIO)ALKANES AND 1,n-CHLORO(ALKYLSULFINYL)ALKANES
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Anodic oxidation of 1,n-halo(alkylthio)alkanes n-S-R, X=Cl, Br, I> and 1,n-halo(alkylsulfinyl)alkanes n-S(O)-R> was studied by cyclic voltammetry in anhydrous acetonitrile and by controlled potential electrolyses.The ease of sulfur oxidation was not affected by the alkyl substituents R or the number of methylene groups n in compounds with n>2.The oxidation of the 1,2-halo(alkylthio)ethanes (n=2) occurred at slightly higher potentials.The peak potentials decreased slightly in the order Cl>Br>I which is probably due to the electronegativity of the halogen atoms.The investigated anodic oxidation was shown to be a two electron irreversible process.Electrolyses in aqueous acetonitrile led to the corresponding sulfoxides and sulfones in good yields.
- Aced, Ahmed,Anklam, Elke,Asmus, Klaus-Dieter,Pohl, Klaus,Glass, Richard S.,et al.
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- Reaction Mechanism of Cathodic Crossed Coupling of Acetone with Unsaturated Compounds in Acidic Solution
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It was confirmed that the cathodic crossed coupling of acetone with unsaturated compounds in aqueous sulfuric acid could proceed smoothly, when the compounds which had radical-acceptable double bonds and were adsorbed on a mercury cathode were used.From this fact, it was concluded that the coupling occurs via the addition of a radical intermediate formed by the one-electron reduction of acetone to the double bonds on the cathode surface.Possibility of the addition of an anionic intermediate derived from acetone was excluded by no occurrence of the coupling of acetone with a polar acetylenic triple bond compound adsorbed on the cathode.
- Koizumi, Toshio,Fuchigami, Toshio,Kandeel, Zaghloul El-Shahat,Sato, Norio,Nonaka, Tsutomu
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p. 757 - 762
(2007/10/02)
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