172 results about "Isoindoles" patented technology

This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.

The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.

The invention discloses a method for preparing lenalidomide (3-(7-amino-3-oxo-1H-isoindole-2-base) piperidine-2,6-diketone). Two intermediates of the lenalidomide are 2-halomethyl-3-nitro-benzoic acidmethyl ester and 3-aminopiperidine-2,6-diketone. The invention discloses methods for preparing the two intermediates and preparing the lenalidomide by using the two intermediates. The method has novel process, short procedures, high reaction yield, low production cost, and larger implementation value and social and economic benefits.

The invention relates to the field of extraction and separation of traditional Chinese medicines, in particular to an isoindole alkaloid compound which is extracted, separated and identified from purslane, and an extraction and separation method of the isoindole alkaloid compound. The new alkaloid compound has a molecular formula of C28H23NO8 and is named as Oleraisoindole. The invention also provides the extraction and separation method of the isoindole alkaloid compound; the method comprises the steps of sequentially extracting by means of water boiling, extracting by using ethyl acetate, carrying out silica gel column chromatography, purifying by using an octadecylsilyl medium-pressure column and Sephadex LH-20, and carrying out liquid phase separation. The isoindole alkaloid compound is identified by using ultraviolet (UV), infrared ray (IR), HR-ESI-TOF-MS, hydrogen-1 nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR) and a two-dimensional nuclear magnetic spectrum analysis method. The compound has potential anti-inflammatory activity, anti-tumor activity, and the like; the invention also provides the preparation method of the compound, thus providing a lead compound and a theoretical basis for development of new medicines and new components.

The invention discloses a novel synthetic process of hydrochloric acid trientine, and aims at providing the synthetic method of the hydrochloric acid trientine. The synthetic process can avoid using a highly-toxic material, namely potassium cyanide, and is temperate in reaction condition. A compound 2,2'-(2,2'-(ethane-1,2-diradical-bibenzyl-di (ethane-2,1-double radical)) bi isoindole-1,3-diketone is used as an initiator, after hydrazinolysis, an intermediate N1, N1'-(ethane-1,2-diradical) di(N1-nethyl ethane-1,2-diamine) is obtained. Through carbobenzoxy protection (Cbz protection), salt is generated,and dibenzyl 2,2'-(ethane-1,2-diradical-di (benzylamine-diradical)) di (ethane-2,1-diradical) dioctyl phthalatic acid aster hydrochloride is obtained so as to crystallize in ethanol through pressing catalytic hydrogenation deprotection to directly obtain the hydrochloric acid trientine. The synthetic process belongs to the organic synthetic technical field.

It is an object of the present invention to provide a luminescent polymer that is useful as a luminescent signal probe for labeling and detecting a target substance at high sensitivity in bioassay, and to provide the application of said luminescent polymer to bioassay. The luminescent polymer of the present invention comprises at least one biotin covalently attached to a polymer that includes monosaccharide or amino acid as a constituent monomer covalently attached to a luminescent substance. Preferably, two or more biotins are attached. Examples of the above-mentioned luminescent substance include cyanoisoindoles, luminols, and acridinium esters, and examples of the polymer include polysaccharides, polyamino acids, peptides, polypeptides, and proteins.

The invention relates to fluoro-boron diisoindole compounds and a preparation method thereof. Compared with the conventional fluoro-boron dipyrrole compounds, according to the fluoro-boron diisoindole compounds, pyrrole rings are directly replaced by isoindole rings, the conjugated range of pi bonds in a parent molecule is increased and thus the photochemical and physical properties of the compounds are changed, molecular absorption and emission wavelengths cause a 'red shift', the maximum ultraviolet absorption wavelength can reach 640nm-680nm and the maximum fluorescence emission wavelength is up to 670nm-713nm and the fluoro-boron diisoindole compounds are near-infrared fluorescent dyes.

The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.

The invention relates to the field of drug synthesis, and particularly relates to a preparation method of a lenalidomide intermediate and lenalidomide. The compound is a drug for treating multiple myeloma. The method comprises the steps of adopting 2-bromomethyl-3-nitrobenzoate and 3-amino-2,6-piperidione hydrochloride as reaction substrates and an inorganic base as an acid-binding agent and obtaining a white to almost white key intermediate 3-(4-nitro-1-oxo-1,3-dihydro-2H-isoindole-2-yl) piperidine-2,6-diketone of the lenalidomide through simple post-treatment; and adopting a mixed solvent of an organic solvent and water as a reaction solvent and carrying out catalytic hydrogenation in the presence of palladium on carbon to prepare the lenalidomide (II). The process route is low in production cost, and a product is high in purity and friendly to environment, and has relatively great implement value and social and economical benefits.

The invention relates to a near-infrared fluorine-boron dipyrrole fluorochrome and a preparation method thereof. According to the method, halogenated isoindole imine and a boric acid reagent Suzuki are coupled, and then the near-infrared fluorine-boron dipyrrole fluorochrome is synthesized through acid catalysis condensation, wherein the emission wavelengths of the fluorochrome in various solvents are greater than 669nm, and the emission spectrum of the fluorochrome and derivatives thereof can reach 748nm. The fluorochrome has relatively high fluorescence quantum yield (0.67-1) and excellent optical physicochemical properties, such as light stability, and has a good application prospect in fields like laser dye and bioanalysis.

The invention discloses a method for normal-pressure efficient synthesis of 6H-isoindole [2,1-a] indole-6-ketone compounds. The technical scheme of the invention has the key points that by taking 2-(2-bromoaryl)-1H-indole compounds and CO as starting materials, under the effects of transition metal palladium catalysts, ligands and alkali, heating and stirring reaction is carried out at 100-140 DEG C in an organic solvent so as to obtain target products, namely the 6H-isoindole [2,1-a] indole-6-ketone compounds. The method disclosed by the invention has the advantages that reaction conditions are mild, the starting materials are simple and easy to prepare, substrates are wide in range of application, and the operation is simple.

Reaction of a dialdehyde, particularly phthaldialdehyde (I), with R-Z where Z is a nucleophilic group (preferably SH) and R is polymerisable (e.g. allyl) gives a reactive thioacetal (V) which can react with an amine ligand L-NH2 to produce an isoindole (IV) which may be fluorescent. At some stage, generally before interaction with L-NH2, the R groups are polymerised, possibly leading to self-assembly of the polymer on a metal or SH-bearing surface. Such a coated surface is useful as a transducer in assays or as a binding medium e.g. for chromatography.

The invention relates to a series of compounds represented as the formula (I), or pharmaceutically acceptable salts thereof, which can be used as new-generation Wee1 selective inhibitor. Compared withexisting Wee1 inhibitor, the compound has a higher selectivity on Wee1 kinase, so that the compound is safer and is higher in treatment index, and also has higher blood brain barrier permeability. The compound has better safety and a larger applicable range, and can be applied to treatment on various tumors, including brain tumor.

The invention relates to a preparation method of 3-methylene isoindole-1-one derivatives. The preparation method comprises the following steps: an N-substituted 2-chlorobenzamide derivative in formula (1), alkyne-terminated compounds in formula (2) and nitrogen-containing ligands react in an organic solvent at 80-100 DEG C in the presence of potassium carbonate and a copper salt catalyst, and the 3-methylene isoindole-1-one derivatives in formula (3) are obtained. The equation is shown in the specification, wherein R<1>, R<2>, R<3> and R<4> are hydrogen; R<5> is C1-C6 alkyl or aromatic, and aromatic is phenyl, benzyl or substituted benzyl; R<6> is phenyl, C2-C6 alkyl, acetoxy methylene or p-tolyloxy methylene. High-yield 3-methylene isoindole-1-one derivatives can be obtained with the method; reaction conditions are mild, reaction operation and a post-processing process are simple, and the method is suitable for large-scale production.

The present invention relates to a lurasidone key intermediate preparation method, and belongs to the technical field of compound synthesis. According to the method, when 4,-(1,2-benzisothiazol-3-yl)-(3aR,7aR)-octahydrospiro(2H-isoindole-2,1-piperazine)methanesulfonate is generated, 4-(1,2-benzisothiazol-3-yl)-1-piperazine is adopted as a raw material, the 4-(1,2-benzisothiazol-3-yl)-1-piperazine, (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and potassium carbonate are subjected to a reaction in a solvent toluene, and a cyclodextrin phase transfer catalyst is added to the reaction system. According to the present invention, by using the cyclodextrin as the phase transfer catalyst, the incomplete reaction problem is solved, and the yield is substantially improved.

The invention discloses an integrated system for storing energy and generating power by using an organic hydrogen storage material. Power is generated by renewable sea energy, generated electric energy is used for supplying power for sea water desalting equipment, water electrolysis hydrogen preparation equipment and a power supply of a hydrogen energy base station, after sea water is filtered into fresh water, hydrogen is prepared by water electrolysis, renewable water resources are converted into hydrogen energy, obtained high-energy-density hydrogen is stored in the organic hydrogen storage material, the power supply of the hydrogen energy base station supplies power for organic hydrogen storage equipment, an obtained hydrogenation organic hydrogen storage material can be conveyed to any places through pipes, the organic hydrogen storage material consists of isoindole, purrocoline, 7,8-benzoquinoline and N-ethylindole, hydrogen separated from an organic hydrogen storage device is directly used for fuel cells, and the hydrogen energy is converted into electric energy or is directly used for heating through the hydrogen fuel cells. Compared with traditional ocean power generation, the integrated system for storing energy and generating power by using the organic hydrogen storage material overcomes geographical limitations of utilization of the sea energy, loss of the electric energy in a conveying process is avoided, and economy of utilization of energy is improved.

The invention relates to a novel crystalline form of mitiglinide drug for treating diabetes, composite comprising same and its preparation process. Mitiglinide is a medicine for treating Type-11 diabetes, and its chemical name is (-)-2(s)-benzyl-4-oxy-4-(cis-perhydro iso indole -2-yl) calcium butyrate dihydrate. The novel crystalline form has high stability.