246 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.

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.

The invention relates to the technical field of 2-arylindole compounds, in particular to a green method for synthesizing a 2-arylindole compound through catalyst-free light driving. In the prior art, the conventional synthesis method of the 2-aryl indole compound has harsh reaction conditions, and generally, an expensive transition metal catalyst is also required to be added as a catalyst. In order to solve the technical problems, the invention provides the green catalyst-free light-driven synthesis method of the 2-arylindole compound, which comprises the following steps: by taking an indole compound and a diaryl iodonium salt compound as initial reaction raw materials, carrying out blue light irradiation reaction in a reaction solvent at room temperature, and after the reaction is finished, obtaining the 2-arylindole compound. According to the method, reaction raw materials are easy to obtain, reaction steps are simple, conditions are mild, the method is environmentally friendly, no catalyst or chemical additive needs to be added in the reaction process, and the method has good application prospects.

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 invention belongs to the technical field of organic synthesis, and discloses a preparation method of a 3-alkylindole compound, which comprises the following steps: in an inert atmosphere, reacting a reaction solution mixed with an indole compound, an allyl alcohol compound, a catalyst Mn-1 and alkali at 110-150 DEG C for 12-24 hours to obtain the 3-alkylindole compound. Mn (CO) 5Br is used as a transition metal and complexed with a PNP pincerlike manganese complex to obtain the Mn-1 catalyst, the 3-alkylindole compound is obtained under the catalysis of the catalyst, allyl alcohol can be aryl allyl alcohol or aliphatic allyl alcohol, a substituent group on an indole ring can be an electron withdrawing group, the application range of a substrate is wide, meanwhile, the selection range of alkali or a solvent is wide, and the 3-alkylindole compound is suitable for industrial production. The method has the advantages of high atom economy, environment friendliness, high safety and the like.

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.

Some aspects of the disclosure relate to compositions comprising fermentates of bacterial strains capable of producing indole-containing compounds such as ILA and lAld. Some aspects relate to nutritional supplements, and food products containing such fermentates, and methods of use thereof.

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%.

The invention belongs to the technical field of biological medicines, and discloses a carbazole / benzo [cd] indole compound as well as a preparation method and application thereof. The carbazole / benzo [cd] indole compound has a structure as shown in a general formula I: # imgabs0 #, wherein R is one of NO2, NH2, Br and N (Ph) 2. The carbazole / benzo [cd] indole compound can generate active oxygen molecules after illumination, including superoxide anions and hydroxyl radicals, and can be applied to preparation of drugs for photodynamic therapy.

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 present invention discloses a method for synthesizing indoline, which is characterized in that: under the co-catalysis of yttrium bis(trimethylsilylamide) and tris(pentafluorophenyl)borane, an additive, a hydrogen source, and an indole compound are used as raw materials to react in a solvent to obtain an indoline compound; the structural formula of the indole compound is the structural formula of the indoline compound. The raw materials of the method of the present invention are widely sourced or easy to prepare, with simple operation, controllable selectivity, high yield, mild conditions, and wide generality.

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 discloses a synthesis method of N-protected 2-benzoyl-3-aryl azo indole, which is characterized in that CuNPs (at) HKUST-1 is used as a catalyst, the use of noble metal is abandoned, the use amount is extremely small, and the economical efficiency and the greenness are improved; the synthesis of the 2-aroyl indole compound is efficiently and highly regioselectively realized by using the guiding advantage of the azo substrate of the 2-aroyl indole compound under the nitrogen atmosphere with an equivalent amount of oxidizing agent. The N-protected aryl azo indole which is wide in source and extremely high in research value is used as a raw material, the benzoylformic acid which is rich in reserve is used as an acyl source, and synthesis of the 2-aroyl indole compound is achieved. The raw materials used in the invention are all industrial commodities, and the raw materials are simple to prepare, wide in source, low in price and stable in structure; reaction pollution is small, environmental protection is achieved, and operation is easy.

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.