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Tetrahydropyridothiazole compounds, preparation method, drug compositions containing the same, and uses thereof

A technology of tetrahydropyridines and compounds, applied in the field of medicinal chemistry and pharmacotherapeutics, capable of solving limited and other problems

Inactive Publication Date: 2012-12-26
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it has been found that there are very limited compounds with good selectivity against HDAC class I, II, and III inhibitors, including natural products and synthetic compound sources.

Method used

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  • Tetrahydropyridothiazole compounds, preparation method, drug compositions containing the same, and uses thereof
  • Tetrahydropyridothiazole compounds, preparation method, drug compositions containing the same, and uses thereof
  • Tetrahydropyridothiazole compounds, preparation method, drug compositions containing the same, and uses thereof

Examples

Experimental program
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Embodiment 1

[0091]

[0092] a) Preparation of compound 3

[0093] Weigh compound 1 (210 mg, 0.89 mmol) and compound 2 (200 mg, 0.81 mmol) in a reaction tube, dissolve in 2 ml of N, N-dimethylformamide (DMF), add diisopropylethylamine ( DIPEA) (0.31mL, 1.77mmol), under nitrogen protection, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) (170mg, 0.89mmol) and 1-hydroxy - Benzo-triazole (HoBt) (120mg, 0.89mmol), stirred overnight at room temperature, the reaction solution was directly extracted with 30 ml of ethyl acetate, and the organic layer was washed successively with 1N hydrochloric acid, saturated sodium bicarbonate, water and saturated brine After one time, dry with anhydrous sodium sulfate, and evaporate the solvent under reduced pressure to obtain a crude product, which is separated and purified by column chromatography to obtain the product, and the elution condition is petroleum ether:ethyl acetate=5:1-3:1, Compound 3 was obtained as 293 mg of white amor...

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Abstract

The present invention relates to the field of pharmaceutical chemistry and drug treatment. Specifically the present invention relates to tetrahydropyridothiazole compounds represented by the following general formula I, a preparation method, drug compositions containing the same, and uses thereof. The compounds represented by the general formula I in the present invention are selective inhibitors acting on histonedeacetylase-6, and provide inhibition effects for deacetylation action of the histonedeacetylase, particularly for deacetylation action of the histonedeacetylase-6 so as to produce biological activities, such that the present invention further relates to applications of the compounds in preparation of drugs for treatment of histonedeacetylase-6 inhibitor mediated diseases, specifically in preparation of drugs for treatment of tumors, neurological diseases, and associated diseases.

Description

technical field [0001] The present invention relates to the fields of medicinal chemistry and pharmacotherapeutics. Specifically, the present invention relates to tetrahydropyridothiazole compounds, their preparation methods and pharmaceutical compositions containing the compounds; The application in medicines for diseases mediated by the invention, specifically relates to its application in the preparation of medicines for treating tumors, neurological diseases and related diseases. Background technique [0002] Cancer is one of the major diseases threatening human health. According to the World Health Organization, cancer is one of the leading causes of death in the world. In 2007, the number of cancer deaths reached 7.9 million, accounting for about 13% of all deaths. At present, the commonly used antineoplastic drugs in clinical practice are mainly cytotoxic drugs, which have unavoidable disadvantages such as poor selectivity, high toxicity and side effects, and easy d...

Claims

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Application Information

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IPC IPC(8): C07D513/04A61K31/437A61P35/02A61P35/00A61P9/00A61P9/04A61P29/00A61P7/06A61P37/02A61P25/28A61P25/16A61P25/00
Inventor 沈竞康李佳方光华苏明波熊兵马兰萍周宇波王昕薛梦竹
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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