96 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.

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 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.

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 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 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.

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.

The application belongs to the technical field of organic synthesis, and particularly relates to a method for catalytically synthesizing N-substituted-3-methyl indole compounds by using aza carbene oxazoline ring palladium compound. The application aims to provide a new synthesis method for N-substituted-3-methyl indole compounds, specifically, a high-catalytic-activity aza carbene oxazoline ring palladium compound is used as a catalyst to catalyze a direct coupling cyclization reaction of o-dichlorobenzene or o-bromochlorobenzene compounds and allyl arylamine, so as to obtain N-substituted-3-methyl indole compounds. The catalyst used in the application has high catalytic activity, the reaction has good product and functional group compatibility, in addition, the catalyst itself is easy to synthesize, and aryl chlorides used in the synthesis route are cheap and easy to obtain. Therefore, the synthesis route provided in the application has great competitive advantages and industrial production utilization value.

The invention belongs to the technical field of compounds, and provides a Schiff base bridged coumarin indole compound as well as a preparation method and application thereof. The coumarin indole compound bridged by the Schiff base or the pharmaceutically acceptable salt of the coumarin indole compound provided by the invention has a structure as shown in a formula I. In-vitro antimicrobial activity evaluation shows that the coumarin indole compound has a good inhibition effect on gram-positive bacteria and gram-negative bacteria, and particularly has a good antibacterial effect on staphylococcus aureus; compared with the prior art, the derivative disclosed by the invention has the advantages that the drug resistance is not easy to generate, so that the derivative or the pharmaceutically acceptable salt thereof can be used for preparing antibacterial active drugs, more efficient and safe candidate drug molecules are provided for clinical treatment, and the clinical treatment problems of increasingly serious drug resistance, stubborn germs, newly appearing harmful microorganisms and the like are favorably solved.

A method and compositions of matter for treating or preventing an auto-immune disorder or immune response in a patient, that includes providing a therapeutic dose to the patient of a substituted indole compound having at least one substitution, wherein the substituted indole compound has only one thiol group, and wherein the ring the thiol group is attached to only contains one N or O atom.

The invention discloses a method for synthesizing an indole fused ring compound through light-induced continuous flow, which comprises the following steps: dissolving a compound shown as a formula I and a compound shown as a formula II in an organic solvent to obtain a homogeneous solution; and pumping the obtained homogeneous solution into a micro-channel reaction device provided with a light source, and reacting to obtain the indole fused ring compound as shown in the formula III. The novel condensed ring indole compound is obtained by taking nitro-aromatic hydrocarbon as a photosensitizer, absorbing energy through ultraviolet irradiation, attacking double bonds on N-Boc indole by the excited nitro-aromatic hydrocarbon to generate triple double free radicals, and carrying out cyclization reaction after electron transition. Compared with the prior art, the light-induced continuous flow reaction device is innovatively applied, the method is green, efficient, free of metal residues and mild in reaction condition, and the synthesized novel product, namely the fused heterocycle indole, has a wide application prospect in the aspect of synthesizing medical products.

This invention discloses a 2-p-methylphenyl-3-trifluoroethylindole compound with the structure shown in formula (A), its crystal form, preparation method, and applications. This invention provides crystal form I of the compound of formula (A), which is monoclinic with space group P21 / c and cell parameters α = 90°, β = 91.884(10)°, and γ = 90°. This invention also provides a method for preparing crystal form A, successfully preparing a 2-p-methylphenyl-3-trifluoroethylindole compound and its crystal form. Furthermore, the compound or its crystal form exhibits certain antibacterial activity and good stability, greatly facilitating subsequent product transportation, storage, or formulation processes.

The present application relates to the technical fields of medical and pharmaceutical chemical synthesis, and particularly relates to a synthesis method of 3-thiocyanatospiro cyclobutyl oxindole compounds, which comprises the following steps: in a reactor, compound 1, compound 2, a catalyst, an additive and a solvent are stirred for 30 minutes at room temperature, after the reaction is completed, the crude product is obtained by reduced pressure distillation, and the 3-thiocyanatospiro cyclobutyl oxindole compound is obtained by column chromatography and thin layer chromatography purification. N The present application takes phenyl bicyclo[1.1.0]butane-1-formamide compounds and thiocyanate as raw materials, and promotes the synthesis of 3-thiocyanatospiro cyclobutyl oxindole compounds by an oxidant. The present application has the advantages of simple synthesis steps, mild conditions, safe operation, good functional group compatibility, high reaction conversion, low cost and the like, and is conducive to industrial production.

1-methyl-2-carboxyl-3-acetanilide indole compounds and applications thereof. The compounds can block the interaction between NLRP3 and NEK7, effectively inhibit the activation and assembly of NLRP3 inflammasome, and have good prevention and treatment effect on NLRP3 inflammasome related inflammatory diseases such as Alzheimer's disease and Parkinson's disease. Thus, the compounds can be used for preparing drugs for treating and / or preventing NLRP3 inflammasome related inflammatory diseases, and provide a new choice for the development of NLRP3 inflammasome small molecule inhibitors.

The invention relates to a polysubstituted indole compound as well as a preparation method and application thereof. Specifically, the invention discloses a compound as shown in a formula (I), or a pharmaceutically acceptable salt thereof, or a prodrug thereof, the compound is a complement factor B inhibitor, has a significant inhibitory effect on complement factor B, and is high in bioavailability and excellent in pharmacokinetics.

The invention provides an indole compound as well as a preparation method and application thereof. The structural formula of the compound is shown as a formula (I), a formula (II) or a formula (III). The compound provided by the invention is used as an ATP (adenosine triphosphate) competitive sphingosine kinase 1 (SphK1) or 2 (SphK2) inhibitor, and shows strong enzyme inhibition activity and an effect of resisting tumor cell proliferation. Experiments prove that the indole compound provided by the invention has the potential to be developed into an anti-tumor therapeutic drug and an anti-pulmonary arterial hypertension therapeutic drug, and a new direction is provided for the field of anti-cancer therapeutic drugs. The preparation method of the compound is simple, low in cost, free of dangerous reagents and suitable for industrial production.

The application belongs to the technical field of organic hydrogen storage material preparation, and particularly relates to a preparation method of a pyrrolo[2,3-e]indole hydrogen storage material. The preparation method comprises the following steps: in a reactor, benzene diamine and o-diol, catalyst alpha and catalyst beta are put in, then reaction is carried out at 25-250 DEG C for 0.1-48 hours, and pyrrolo[2,3-e]indole compounds are obtained; the catalyst alpha is a catalyst with hydrogen activation ability and dehydrogenation ability; the catalyst beta is an acid with Hammett acidity function H0 < 0. The application provides a method for preparing the hydrogen storage material pyrrolo[2,3-e]indole compounds, benzene diamine and diol are used for reaction, two catalysts are used, and a one-step closed double ring is realized, and the atom economy is high. The starting material of the application is cheap and easy to obtain, and is easy to be industrialized, and helps hydrogen energy industry. The method of the application has high universality and high substrate tolerance.

The invention belongs to the technical field of biological medicines, and discloses 5-(benzyl carbamoyl)-indole compounds and application thereof in preparation of medicines for preventing and / or treating diabetic cardiomyopathy. In-vivo and in-vitro experiments prove that the 5-(benzyl carbamoyl)-indole compound disclosed by the invention can effectively reduce blood sugar and improve myocardial cell injury induced by high glucose and high fat, does not cause body weight increase, has a remarkable curative effect of improving diabetic cardiomyopathy, is small in side effect, and can be used for preparing medicines for treating diabetic cardiomyopathy. And the pharmaceutical composition has a remarkable effect at a low dosage, has a more excellent effect compared with a high-dosage positive drug, and provides a new drug for treating diabetic cardiomyopathy, so that the pharmaceutical composition has a wide application prospect.

The invention relates to the technical field of organic synthetic chemistry, in particular to a selenylation preparation method of aniline and an indole compound, which comprises the following steps: A1, reacting the indole compound or the aniline compound with potassium selenide and N-chloro-N-fluorobenzenesulfonamide in an organic solvent at the temperature of 0 DEG C to room temperature; and A2, after the reaction is finished, carrying out extraction, concentration and column chromatography purification to obtain the selenium cyanate indole or aniline derivative, wherein the reaction operation comprises the following steps: dissolving the indole or aniline compound and KSeCN in an organic solvent, slowly dropwise adding CFBSA while stirring at the temperature of 0 DEG C, heating to room temperature after dropwise adding, and continuously stirring for reaction. According to the method, the CFBSA reagent is taken as an oxidizing agent, relatively cheap potassium selenide is taken as a selenium cyano group source, selenylation of aniline, indole and part of aromatic rings is realized at room temperature under a mild oxidation condition, and corresponding products are obtained at medium to excellent yield.

The invention discloses an application of an oxoindole compound in preparation of a drug for resisting vesicular stomatitis virus. The oxoindole compound disclosed by the invention can be used for efficiently inhibiting proliferation of vesicular stomatitis virus (VSV) and has relatively low cytotoxicity. The oxoindole compound provided by the invention has a wide application prospect in preparation of anti-vesicular stomatitis virus drugs and drugs for treating vesicular stomatitis virus infection related diseases. The invention provides a new application of the oxoindole compound in anti-VSV drugs.