164 results about "Isoindole" patented technology

The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-alpha in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.

The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-alpha in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.

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

The present application describes 2-(2′,6′-dioxo-3′-deutero-piperidin-3′-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

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 invention relates to novel conjugated polymers containing one or more [1,2,5]Thiadiazolo[3,4-e]isoindole-5,7-dione (TID) repeating units, to methods for their preparation and educts or intermediates used therein, to polymer blends, mixtures and formulations containing them, to the use of the polymers, polymer blends, mixtures and formulations as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising, or being prepared from, these polymers, polymer blends, mixtures or formulations.

The invention discloses a crystal IV of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl) piperidine-2,6-diketone. 2theta expressed by degrees has diffraction peaks between 7.7+/-0.2 and 11.9+/-0.2 in the X-ray diffraction pattern of the crystal. Moreover, the invention also discloses a preparation method and a medicinal composite of the crystal.

Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is -CH2-, -SO-, -O-, -SO2-, or -S-; compositions comprising the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.

The invention discloses a 1,3,4-thiadiazole fluorouracil compound as well as a preparation method and application thereof. The compound has a general formula I, wherein R is substituted phenyl, aromatic heterocycle or aryloxy alkyl; the substituent group R1 in tri-substituted phenyl is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl, R2 is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl, and R3 is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl; and the aromatic heterocycle is pyridine, thiofuran, furan, indole or isoindole. The invention has less compound consumption, good insecticidal effect, simple process method, low cost and wide market prospect.

The invention provides a preparation method of lurasidone. On the basis of the existing preparation method of lurasidone, a one-pot method is adopted to replace the method including multiple steps and obtain a target product once. The preparation method comprises the following steps: adding 3-(1-piperazinyl)-1,2-benzisothiazole in toluene, stirring to dissolve; adding (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and an inorganic alkali, heating and carrying out reflux reaction for 12-36 hours; adding (3alpha R,4S,7R,7alpha S)4,7-methano-1H-isoindole-1,3(2H)-dione; heating and refluxing; recycling toluene at reduced pressure; adding ethyl acetate in the residue, stirring to dissolve, washing for 2-3 times with 5% hydrochloric acid, separating out the organic layers, drying for 20-120 minutes, filtering to remove the drying agent, concentrating the obtained ethyl acetate solution, dropwise adding concentrated hydrochloric acid, precipitating the solid, and performing suction filtration to obtain crude lurasidone; and refining crude lurasidone to obtain pure lurasidone. By adopting the preparation method of lurasidone, the solvent can be recycled conveniently and the method is simple in operation.

the invention relates to a pachysandra terminalis alkaloid compound for resisting tumor metastasis (as shown in the figure), which comprises 9-dimethylamino-4,7-megastigmadien-3-one (1), E-salignone (2), Z-salignone (3), 3beta-(3'alpha-isopropyl)-lactam-5alpha-pregn-4-one (4), pachystermine A (5), 3-spiro-(3'-oxo-isoindole)-5alpha-pregn-20-one (6) and 3beta-(methylsenecioylamino)-5alpha-pregn-20-one(7). The invention has a strong effect on resisting the chemotaxis migration of breast cancer cells, and can be used for preparing medicaments for resisting tumor metastasis.

The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II):

(wherein R¹ and R² each independently represents a C_1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I):

(wherein R¹ and R² have the same meanings as R¹ and R² in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

The invention relates to a fluorescent molecular probe for detecting Cu<2+> in the field of fine chemical engineering, in particular to a preparation method of a Cu<2+> fluorescent molecular probe based on rhodamine dyes and an application of the fluorescent molecular probe to biocellular imaging and water system copper ion detection. A preparation method of a compound I includes the steps: adding 1 part of (E)-2-((3', 6'-bis (diethylamino)-3-oxaspiro [isoindazole-1, 9'-xanthene]-2-alkene) imine) ethylal and 6 parts of hydrazine hydrate into a reaction vessel, heating and stirring mixture, performing rotary evaporation to remove ethyl alcohol after reaction, and adding 50 parts of methylene dichloride and 150 parts of saturated sodium chloride solution; separating mixture by the aid of a separating funnel, drying a organic phase by the aid of anhydrous sodium sulfate, performing spin drying on solvents, and separating coarse products by a column chromatography to obtain the compound I. The preparation method is mild in reaction condition, less in synthesis step and high in product yield, and raw materials are low in cost and easily acquired.

The invention relates to the technical field of pH fluorescent probes and particularly relates to a lysosome targeted pH fluorescent probe for monitoring cell autophagy as well as preparation and application of the lysosome targeted pH fluorescent probe. The preparation method comprises the following steps of dissolving 2-(2-aminoethyl)-3',6'-bis(diethylamino) spiro [isoindole-1,9'-xanthan]-3-ketone and 2-(2-methoxyethoxy)4-methyl benzene sulfonic acid ethyl ester in N, N-dimethylformamide, and carrying out heating reflux to obtain a crude product; and removing a solvent from the crude product, and separating through a silica gel column to obtain a pure product. Cytotoxicity tests show that the probe has almost no toxic or side effect on cells, a cell co-localization experiment determinesthat the probe can specifically target a cell lysosome, and a laser confocal microimaging experiment shows that the probe has good cell membrane permeability and can perform high-sensitivity detectionon pH change in the lysosome. The probe provided by the invention can monitor the autophagy process of the cells by detecting the change of pH in the lysosome.

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.