169 results about "Indole Compound" patented technology

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

The invention belongs to the field of organic synthetic chemistry, and relates to a preparation method of melatonin and meerythrine indole derivatives and compounds. Specifically, the indole derivative is efficiently synthesized by taking arylamine and carboxylic acid as raw materials through a one-pot two-step reaction in the presence of catalysis of ferric chloride hexahydrate (FeCl3. 6H2O), a ligand, a diazotization reagent, an additive and a solvent under the conditions of visible light irradiation, inert atmosphere and room temperature. According to the method, visible light induced iron-based LMCT catalysis and iron lewis acid catalysis functions are integrated, and efficient integration of diazotization, decarboxylation, free radical coupling and cyclization reaction is achieved. The method has the advantages that raw materials are cheap and easy to obtain, reaction conditions are mild, substrate applicability is wide, functional group compatibility is good, operation is easy, convenient and safe, and environment friendliness is achieved, gram-level scale preparation can be achieved, and a green and efficient synthesis path is provided for indole compounds with biological activity such as melatonin and meerythrine.

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

Provided herein are indole compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

The application relates to the field of agricultural disease control technology, and particularly relates to the use of indole compounds and pharmaceutically acceptable salts, solvates, crystal forms, prodrugs, stereoisomers and tautomers thereof for preparing a medicine for inhibiting pathogenic key protein kinase CgSlt2 of pathogenic fungi. The application first proposes a new type of CgSlt2-targeted inhibitor, specifically, indole compounds ((S)-N-(1-(1H-indol-3-yl)-4-(methylamino)-4-oxobutan-2-yl)-8-bromo-1,6-naphthyridine-2-carboxamide) and ((S)-N-(2-((1H-indol-3-yl)-1-(methylamino)-1-oxopropyl)-8-bromo-1,6-naphthyridine-2-carboxamide) are used as CgSlt2 inhibitors, have the characteristics of high target specificity and high activity, and exhibit excellent pathogenicity inhibition of a strain of the complex group of Colletotrichum gloeosporioides.

The application belongs to the field of organic synthesis and particularly relates to a synthesis method of polysubstituted indole propionate derivatives. Aryl acetate compounds and sulfonyl indole compounds are used as raw materials, and the reaction is carried out through an isothiourea organic small molecule catalyst. The reaction raw materials are simple and easy to obtain, the reaction conditions are mild, the operation is simple, the reaction time is short, the reaction has good diastereoselectivity and high yield, the synthesis method of the polysubstituted indole propionate derivatives overcomes the defects and deficiencies of the existing synthesis method, and has the characteristics of high efficiency, simplicity and wide universality.

The application discloses an indole compound, a preparation method and application thereof. Specifically, the application provides a compound as shown in formula I, a pharmaceutically acceptable salt or an enantiomer thereof, and the compound can effectively shorten sleep latency, prolong sleep time, and has a better sleep promoting effect.

The invention provides an indole compound and a solar cell. The indole compound has a structural formula as shown in a formula (I). At least one of R1-R7 has a structure as shown in a formula (Hy1): L1 is any one of substituted or unsubstituted C6-C30 arylene, substituted or unsubstituted C3-C30 heteroarylene, substituted or unsubstituted C1-C30 alkylene, substituted or unsubstituted C1-C30 alkyleneoxy and substituted or unsubstituted C1-C30 alkylenesulfenyl, and R8 is any one of a phosphate group, a carboxylic acid group and a sulfonic acid group; when R1-R7 do not represent the structure represented by formula (Hy1), R1-R7 represent the structure represented by formula (Hy1); a substituted or unsubstituted C1-C30 alkyl group, a substituted or unsubstituted C1-C30 alkoxy group, a substituted or unsubstituted C1-C30 alkylthio group, a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C6-C30 arylamino group, a substituted or unsubstituted C3-C30 heteroaryl group, a substituted or unsubstituted C3-C30 heteroarylamino group, a substituted or unsubstituted C3-, each independently selected from hydrogen, halogen, nitro, hydroxyl, substituted or unsubstituted C1-C30 alkyl group, substituted or unsubstituted C1-C30 alkoxy group, substituted or unsubstituted C1-C30 alkylthio group, substituted or unsubstituted C6-C30 aryl group, substituted or unsubstituted C3-C30 heteroarylamino group, substituted or unsubstituted C3- and C12 cycloalkyl is selected from any one of C12 cycloalkyl.

Disclosed are substituted indole compounds and compositions. The substituted indole compounds and compositions can be used for treating or preventing acute renal failure in a subject. The compounds and compositions can also be used for treating an infectious disease or cancer.

The application discloses an iridium complex, a preparation method thereof and application of the iridium complex in synthesis of chiral piperidines, and the preparation method of the iridium complex comprises the following steps: adding an indole compound, an iridium compound and an alkali into a first solvent, heating and stirring at 40-80 DEG C, lowering to room temperature after reaction, filtering, reducing pressure distillation, and separating by silica gel column chromatography to obtain the iridium complex; under the cooperation of the iridium complex as a catalyst and chiral phosphoric acid, 1,5-diol compounds and amine compounds can be directly reacted to obtain a series of chiral piperidine compounds, the method has the advantages of high reaction efficiency, simplicity and high yield, and the enantiomeric excess value of the chiral piperidine prepared by using the iridium catalyst is not less than 83%.

Disclosed herein are solid forms (e.g., crystalline forms) of 4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-9H-pyrido[2,3-b]indole (Compound 1), as well as compositions, pharmaceutical compositions, kits, methods, and uses thereof. The compounds disclosed herein are inhibitors of atypical protein kinase C (aPKC), and therefore, their solid forms are useful for treating and / or preventing basal cell carcinoma.

This invention relates to the pharmaceutical field, specifically to a heteroindole derivative, its synthesis method, and its applications. The heteroindole compound derivative has the structure shown in general formula (I), wherein R1 is selected from any one of N-Boc-trans-1,4-cyclohexanediamine, N-Boc-piperazinyl, trans-1,4-cyclohexanediamine, piperazinyl, and N-methylpiperazinyl; R2 is selected from H or a halogen atom; and X, Y, and Z are all selected from CH or N. This invention demonstrates through experiments that the heteroindole derivative possesses good CDK9 inhibitory activity and selectivity, providing a theoretical basis for the treatment of diseases related to the activity or expression level of the cell cycle-dependent kinase CDK9, and exhibits good pharmaceutical potential.

The invention relates to an azaindole compound as well as a preparation method and application thereof. The compound has a structure as shown in a formula I. The invention also relates to a preparation method of the compound with the structure shown in the formula I and a pharmaceutical composition. The invention also provides application of the compound in preparation of drugs for reducing uric acid.

The present application relates to a kind of RANKL / NLRP3 dual-target inhibitor and its preparation method and application, belong to the field of pharmaceutical chemistry and biomedical technology.The indole compound, its optical isomer, pharmaceutically acceptable salt and hydrate provided by the present application have RANKL and NLRP3 dual-target inhibition activity, can be inhibited by inhibiting RANKL-RANK interaction, and inhibit inflammasome NLRP3 activity, regulate RANKL activity in osteoclast precursor cell, inhibit the formation of osteoclast, thereby reduce bone resorption, and improve the inflammatory response caused by rheumatoid arthritis, is expected to play the prevention and treatment of bone metabolic disease.

The invention relates to the technical field of biological medicines, and particularly discloses an azaindole compound as well as a preparation method and application thereof. The azaindole compound provided by the invention is a compound as shown in a general formula I or pharmaceutically acceptable salt, isomer, solvate, hydrate, prodrug or isotope derivative of the compound, the structural formula of the general formula I is shown in the specification. The azaindole compound provided by the invention shows good inhibitory activity on BCR-ABL-T315I and BCR-ABL-WT transfected Ba / F3 cells, so that the azaindole compound can be used as a BCR-ABL inhibitor and is expected to be developed into a medicine for treating and / or preventing BCR-ABL related diseases.

This invention discloses an α-indolylpyrrolo[1,2-a]indole derivative and its preparation method. The derivative is a levorotatory or dextrorotatory optically active form or racemate with the following structural formula: The preparation involves using α-indolylpropynyl alcohols and indole compounds as raw materials, and 3,5-bis(trifluoromethyl)phenylbinaphthylphosphonic acid as a catalyst, reacting in an organic solvent to obtain the α-indolylpyrrolo[1,2-a]indole derivative. This invention utilizes an organophosphate-catalyzed tandem reaction of two components to synthesize the α-indolylpyrrolo[1,2-a]indole derivative. The reaction conditions are mild, the process is simple, and the operation is convenient. The obtained product is the core skeleton of the indole bases of the natural products isoborreverine and dimethyl isoborreverine, which is of great significance for the synthesis of analogs of these natural products.

The invention discloses a 2, 3, 4, 9-tetrahydro-1H-pyridine [3, 4-b] indole compound as well as a preparation method and application of the 2, 3, 4, 9-tetrahydro-1H-pyridine [3, 4-b] indole compound. According to the preparation method, 3-hydroxy-4-methoxybenzaldehyde and 1-(chloromethyl)-2, 6-difluorobenzene are taken as initial raw materials, and 1-(3-((2, 6-difluorophenyl) oxo)-4-methoxyphenyl)-2, 3, 4, 9-tetrahydro-1H-pyridine [3, 4-b] indole is prepared through a two-step reaction. The 1-(3-((2, 6-difluorophenyl) oxo)-4-methoxyphenyl)-2, 3, 4, 9-tetrahydro-1H-pyridine [3, 4-b] indole provided by the invention has a remarkable inhibition effect on osteoclast differentiation induced by RANKL, has no obvious cytotoxicity, can be used as a candidate drug which is novel in structure and is used for inhibiting osteoclast differentiation, and has a broad application prospect. The method is used for targeting osteoclast to treat bone mass loss related diseases.

The present application relates to the technical field of biological medicines, and particularly discloses an azaindole compound, a preparation method therefor, and a use thereof. The azaindole compound provided by the present application is a compound represented by general formula I or a pharmaceutically acceptable salt, an isomer, a solvate, a hydrate, a prodrug or an isotope derivative thereof; and the structural formula of general formula I is: formula I. The azaindole compound provided by the present application exhibits good inhibitory activity against Ba / F3 cells transfected with BCR-ABL-T315I and BCR-ABL-WT. Therefore, the azaindole compound can be used as a BCR-ABL inhibitor, and is expected to be developed into a drug for treating and / or preventing BCR-ABL related diseases.

The application discloses a 2-aryl-3-trifluoroethyl indole compound with a structure as shown in formula A and a preparation method and application thereof. 3 The target object A is obtained through the reaction of the aromatic aldehyde, the azacyclic carbene (NHC) and the o-amino styrene, 3,3-dimethyl-1-(trifluoromethyl)-1,3-dihydro-1 lambda The 2-aryl-3-trifluoroethyl indole compound disclosed by the application has excellent antibacterial activity, is a novel material with a novel structure, raw materials are easy to obtain, reaction conditions are mild, green and environment-friendly, and operation is simple.

The invention discloses a bisindole compound as well as a synthesis method and anti-tumor application thereof. The molecular structure of the bisindole compound is shown in the specification. The bisindole compound XQ-010 has the remarkable effects that the bisindole compound XQ-010 can be used as an IL-6 / STAT3 signal channel regulator for tumor treatment, particularly has unique advantages in the aspect of inhibiting tumor growth and metastasis based on the inhibiting effect of the bisindole compound XQ-010 on CD133 + and CD44 + tumor stem cells, and has important clinical application value and development prospect.

The invention discloses a method for synthesizing benzofuran and indole compounds through molybdenum-catalyzed intermolecular deoxygenation cycloaddition reaction, which comprises the following steps: by taking an o-hydroxyphenylacetylene compound or an o-aminophenylacetylene compound as a substrate A and a 1, 3-dicarbonyl compound as a substrate B, reacting under the action of a molybdenum catalyst, a ligand and an additive, thereby obtaining the benzofuran and indole compounds. And carrying out an intermolecular deoxygenation cycloaddition reaction in an organic solvent to generate a corresponding benzofuran or indole compound. The invention provides a method for synthesizing benzofuran and indole compounds through molybdenum-catalyzed intermolecular deoxygenation cycloaddition reaction, the method takes a molybdenum compound as a catalyst, the reaction condition is mild, the atom economy is high, the functional group compatibility is good, and various substituted benzofuran and indole compounds can be efficiently constructed; and a new path is provided for synthesis of the important heterocyclic compounds.

The invention discloses a method for selectively preparing an indole compound or a carbazole compound by alkali salt regulation and manganese catalysis, which comprises the following steps of: selectively synthesizing the indole compound or the carbazole compound by taking 2-aryl indole or substituted 2-aryl indole and alpha-chloro aryl ethyl ketone or substituted alpha-chloro aryl ethyl ketone as initial raw materials; conditions are mild, selectivity, yield and safety are high, and industrial production is facilitated; according to the invention, 2-aryl indole or substituted 2-aryl indole and alpha-chloro-aryl ethyl ketone or substituted alpha-chloro-aryl ethyl ketone are used as initial raw materials for the first time, and alkali salt is regulated to regulate the reaction so as to selectively prepare indole compounds or carbazole compounds.

The application provides a preparation method and application of a metallocene polypropylene catalyst. The first aspect of the application provides a preparation method of a metallocene polypropylene catalyst, comprising the following steps: subjecting a carrier to a thermal activation treatment to obtain a thermally activated carrier; loading a first cocatalyst on the thermally activated carrier to obtain a thermally activated carrier after loading of the first cocatalyst; preparing a catalyst precursor by using a second cocatalyst, a metallocene compound and an indole compound; and reacting the thermally activated carrier after loading of the first cocatalyst with the catalyst precursor to obtain the metallocene polypropylene catalyst. The preparation method of the metallocene polypropylene catalyst can effectively improve the activity and stereoregularity of the metallocene polypropylene catalyst by adding an electron donor of the indole compound to modify an active center in the preparation process of the metallocene polypropylene catalyst; and meanwhile, the preparation process is simple, and the types of chemical reagents used are few.

The present application relates to a solid form of an indole compound, a preparation method therefor and a use thereof. Specifically, the present application relates to a solid form of a compound of Formula (1), a method of preparing same, a pharmaceutical composition comprising same, and a use thereof in treating a disease.

The invention relates to the technical field of chemical synthesis, in particular to a preparation method of a 3-hydroxyl oxoindole compound. The method specifically comprises the following steps: adding indole with different functional groups and derivatives thereof into a solvent at room temperature, then adding NCS and an oxidizing agent, and reacting while stirring; after extraction, adding a 1N NaOH solution, and continuously stirring to complete the reaction; and removing the solvent in vacuum, and purifying residues through a rapid column chromatography to obtain the 3-hydroxyl oxoindole compound. The invention provides the simple and efficient preparation method of the 3-hydroxyl oxoindole compound, a series of 3-hydroxyl oxoindole compounds substituted by different functional groups can be prepared by the method provided by the invention, and the method is mild in reaction condition, low in synthesis cost, high in product yield and suitable for industrial production. Technical support is provided for application of the 3-hydroxyl oxoindole compound in the fields of organic synthesis, fine chemical engineering and pharmacy.

This invention relates to a method for the trivalent rhodium-catalyzed synthesis of 2-cyanenylindole compounds, belonging to the field of organic chemistry. The method uses [Cp*RhCl2]2 as a catalyst and N-pyrimidine indole compounds and alkynyl-N-cyano-N-phenyl-p-toluenesulfonamide compounds as raw materials. The reaction is carried out in an organic solvent at 60°C with lithium chloride assistance, and the 2-cyanenylindole compounds are obtained after separation and purification. This invention utilizes a cyano group migration strategy to achieve a tandem reaction of indole C-H alkenylation and cyano group introduction, constructing C-C and C-CN bonds in one step, with a target product yield of 31%–82%. Compared with existing technologies, this invention uses a non-toxic cyanide source instead of traditional highly toxic cyaniding reagents, and has advantages such as simple operation, mild reaction conditions, wide substrate applicability, and high atom economy.