26 results about "Thienopyridines" patented technology

The invention discloses a preparation method of a triazinyl covalent organic framework (COF) material and application of the triazinyl covalent organic framework material in photocatalytic production of hydrogen peroxide. The amino starting monomer is regulated and controlled through a side chain regulation and control strategy to obtain the COF with a functional group, and the COF can be connected into a ring by thienopyridine through post-modification to replace an original imine bond, so that the planarity and the conjugation degree of the COF are obviously improved, and the COF has good light absorption capacity and a proper band gap; therefore, the COFs photocatalyst has excellent photocatalytic hydrogen peroxide production capacity in a water-benzyl alcohol system under a light source, and a beneficial thought can be provided for designing a high-performance COFs photocatalyst.

The present description relates' to compounds of formula (I) useful for improving pre-mRNA splicing in a cell. In particular, another aspect of the present description relates to substituted thieno[3,2-b]pyridine compounds, forms, and pharmaceutical compositions thereof and methods of use for treating or ameliorating familial dysautonomia.

A cosmetic composition comprising: (a) 2-mercaptonicotinoyl glycine; (b) acyl glycinate surfactant; (c) a salt providing divalent cations having a charge density of about 40 to about 200 C / mm3 and a water solubility of at least 400 g / L; (d) anionic polymer; (e) glycerin; (f) water; and (g) reducing agent. The cosmetic composition is particularly useful in a method for brightening skin, depigmenting skin, treating hyperpigmentation of skin, treating melasmic skin, or evening skin tone.

The present invention relates to a composition comprising: (1) at least one thiopyridinone compound; and (2) caffeine. The present invention can provide a composition including (1) thiopyridinone compound(s) with increased photostabilization of the (1) thiopyridinone compound(s).

The present invention relates to a crystalline microparticle form of 6,7-dihydro-4-hydroxy-7-isopropyl-6-oxo-N-(3-(piperidin-1-yl)propyl)thieno[2,3-b]pyridine-5-carboxamide potassium salt (PRX-3140) (I) for a particle delivery system (PDS) having good bioavailability and stability for the treatment of Alzheimer's disease (AD) and other dementias including post-traumatic stress disorder (PTSD) that affect the cholinergic and / or serotonergic systems. In other aspects, the present invention relates to an oral dosage form, a method of synthesizing the crystalline microparticle form, the preparation of a particle delivery system (PDS), and a final dosage form (FDF). JPEG2025518713000025.jpg49169

The present invention relates to a composition comprising: (1) at least one thiopyridinone compound; and (2) at least one compound selected amongst Vitamin B3 and derivatives thereof. The present invention can provide a composition including (1) thiopyridinone compound(s) with increased solubility of the (1) thiopyridinone compound(s) over time.

The application discloses a synthesis method of 1-chlorobenzo[4,5]thieno[2,3-c]pyridine, and relates to the technical field of preparation of heterocyclic organic compounds containing thiophene and pyridine; the application comprises the following steps: taking 5-bromo-2-chloropyridine and phenylboronic acid as raw materials, and preparing 2-chloro-5-phenylpyridine intermediate product through Suzuki coupling; adding sulfur as a cyclization thiophene raw material; under electrocatalysis conditions, sulfur is solidified through nucleophilic addition, sulfur free radicals are generated through single electron transfer, and the cyclization thiophene synthesis under mild conditions is completed; 1-chlorobenzo[4,5]thieno[2,3-c]pyridine is obtained by separating the crude product; the raw materials are cheap and easy to obtain, the cost is low, the reaction process is simple and easy to operate, the reaction period is simplified, the reaction condition is mild, the three wastes are less, the product yield is good, and the method is suitable for large-scale production.

The invention relates to a thienopyridone compound, application thereof and an antituberculosis drug. The thienopyridone compound disclosed by the invention has a structure as shown in a formula (I), wherein-Ar1-(R1) n is a C6-C10 aromatic ring substituted by n R1 or a 4-10-membered heteroaromatic ring, n is selected from 0, 1, 2, 3 or 4, and n R1 is selected from C1-C6 alkyl, C1-C5 alkoxy, C3-C10 cycloalkyl, halogen, C1-C8 acyl, C1-C6 alkyl substituted by hydroxyl, C1-C6 alkyl substituted by halogen, nitro or cyano; -Ar2-(R2) n is a C6-C10 arylene ring substituted by n R2 or a 4-10-membered heteroaromatic ring, n is selected from 0, 1, 2, 3 or 4, and n R2 is respectively selected from C1-C6 alkyl, C1-C5 alkoxy, C3-C10 cycloalkyl, halogen or nitryl; and R3 is selected from the following groups: H or C1-C8 acyl groups. The thienopyridone compound has a novel mother nucleus structure and excellent anti-tubercle bacillus activity, and has a very strong inhibition effect on the growth of tubercle bacillus.

The present invention relates to crystalline forms of N-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (Compound 1), pharmaceutical compositions comprising the crystalline form, processes for preparing the crystalline form and methods of use therefore.

The application discloses a preparation method of 4-bromothieno[2,3-c]pyridine-2-carboxylic acid ethyl ester, which comprises the following steps: 5-bromo-4-iodopyridine-3-thiol and propargyl acid ethyl ester are subjected to a Sonogashira coupling and a ring-closing series reaction under the action of a catalyst and an alkali to obtain 4-bromothieno[2,3-c]pyridine-2-carboxylic acid ethyl ester. The raw material adopted by the method is cheap and easy to obtain, the synthesis method is simple to operate, the reaction condition is mild, the requirement for equipment is low, and the method is suitable for the needs of industrial large-scale production.

A method for synthesizing a halogen-substituted thienopyridine compound, namely, a method for synthesizing 3-chlorothieno[2,3-c]pyridine-2-carboxylic acid, is implemented by using a reinforced heating jacket to prepare 3-aminothieno[2,3-B]pyridine-2-carboxylic acid ethyl ester by reacting 3-chloro-4-cyanopyridine, ethyl mercaptoacetate, and sodium methoxide; then preparing 3-chlorothieno[2,3-c]pyridine-2-carboxylic acid ethyl ester; and finally obtaining the final product, 3-chlorothieno[2,3-c]pyridine-2-carboxylic acid.

The invention relates to new thienopyridinone compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as FGFR (fibroblast growth factor receptor) inhibitors and to their use in the treatment of diseases, e.g. cancer.

Composition comprising a thiopyridinone compound and an amino-sulfonic compound The present invention relates to a composition, in particular cosmetic, comprising at least one compound of formula (I), at least one amino-sulfonic compound of formula (II) and strictly less than 0.2% by weight of an alkali salt of thiosulfuric acid and / or its solvates such as hydrates, or totally free from alkali salt of thiosulfuric acid and / or its solvates such as hydrates.

Disclosed herein are dosage and dosage regimens for N-(3-cyano-5-(cyclohexylmethyl)-6,6- dimethyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)-2-(4-sulfamoylphenyl)acetamide (Compound (1)), or a pharmaceutically acceptable salt thereof, for the treatment or prevention of a dengue virus disease or disorder. In addition, the invention provides using such dosage and dosage regimens in methods for the treatment or prevention of a dengue virus disease or disorder: Compound (1).

The invention discloses a hetero-diad compound taking indanone-tetrahydrothieno [3, 2-c] pyridine as a parent body and a preparation method and application thereof, the hetero-diad compound taking indanone-tetrahydrothieno [3, 2-c] pyridine as the parent body is selected from the compounds shown in the following general formulas (I), (II) and (III), the compound takes indanone of donepezil as a parent nucleus, and the compound is selected from the compounds shown in the general formulas (I), (II) and (III). And the compound is combined with an anti-platelet functional group tetrahydrothieno [3, 2-c] pyridine through a linking group. The compound has multiple action mechanisms (inhibiting AChE, resisting Abeta aggregation, resisting platelet aggregation and improving learning and memory impairment) and high blood-brain barrier permeability, and is suitable for preventing and treating vascular dementia.

The present invention relates to a composition, in particular a cosmetic or dermatological composition, comprising at least one aqueous phase, at least one water-soluble organic UV-screening agent and at least one thiopyridinone compound of given formula, and / or the optical isomers or geometric isomers thereof and also the organic or mineral acid or base salts thereof, and / or solvates thereof, such as hydrates.

Disclosed are a method for synthesizing a thieno[3,2-b]pyridine-5(4H)-one derivative by using a gold catalyst and a use of the derivative compound, wherein the novel thieno[3,2-b]pyridine-5(4H)-one derivative of the present disclosure, which is a compound synthesized using gold as a catalyst, has fluorescence characteristics with a wide range of emission wavelengths and thus can be helpfully used in various industrial fields, such as physics, chemistry, and biomedicine research.

The application discloses a novel 3-urea-substituted thieno[2,3-b]pyridine compound, a preparation method and application thereof. The preparation method is that 5-bromothieno[2,3-b]pyridine-3-amine is subjected to nucleophilic substitution reaction with phenyl chloroformate or phenyl thiophosphonic chloride to generate an intermediate, the intermediate is subjected to nucleophilic substitution reaction with a substituted amine to generate a key intermediate, then the key intermediate is subjected to palladium-catalyzed Suzuki coupling reaction or Buchwald-Hartwig coupling reaction under alkaline conditions with a substituted aryl boronic acid or borate or a substituted arylamine to obtain a target product, namely the 3-urea-substituted thieno[2,3-b]pyridine compound. The 3-urea-substituted thieno[2,3-b]pyridine compound has a certain prospect as a DRAK2 inhibitor in the development of metabolic syndrome treatment drugs.

The present invention relates to a composition, notably a cosmetic or dermatological composition, comprising palmitoyl tripeptide-1, palmitoyl tetrapeptide-7, and at least one compound of formula (I) or (I'), as described hereinbelow, and / or optical isomers thereof, geometrical isomers thereof, and also organic or mineral acid or base salts thereof, and / or solvates thereof such as hydrates.

The present invention relates to a composition, in particular a cosmetic or dermatological composition, comprising at least one amino-substituted 2-hydroxybenzophenone compound, and at least one compound of formula (I) or (I'), as described hereinbelow, and / or optical isomers thereof, geometrical isomers thereof, and also organic or mineral acid or base salts thereof, and / or solvates thereof such as hydrates.

The present invention relates to a composition comprising: (a) at least one thiopyridinone compound; and (b) at least one compound selected from ergothioneine and derivatives thereof. The present invention can provide a composition including (a) thiopyridinone compound(s) with increased stability of the (a) thiopyridinone compound(s) over time, in particular even when the composition is maintained for a relatively long period of time under elevated temperature.

Provided herein are compounds of formula (I) or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt, hydrate, or solvate of any of the foregoing, wherein R1, R2, Ring A, L, R6, R7, and R8 are as defined elsewhere herein. Also provided are methods of preparing compounds of formula (I). Also provided herein are methods of modulating TDP-43 and methods of treating a disease or condition mediated by TDP-43 in an individual in need thereof.

The present invention relates to a composition, preferably a transdermally or topically administrable composition, comprising as active ingredient a thienopyridine compound of chemical formula 1 or a pharmaceutically acceptable salt thereof. The composition of the present invention contains menthol, preferably L-menthol, and can thereby promote the penetration of the thienopyridine compound into the skin and additionally synergistically enhance the anti-inflammatory and / or antipruritic effect of the thienopyridine compound.