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Thiadiazole derivative

A compound and pharmaceutical technology, applied in the field of medicine, can solve problems such as injury, side effects, and low cure rate

Inactive Publication Date: 2013-07-17
天津天诚新药评价有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy is faster, but the cure rate is very low
At the same time, it is clinically found that many anticancer drugs have obvious damage and side effects on the normal body, such as mutagenesis and genotoxicity

Method used

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  • Thiadiazole derivative
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 2-(6,7-Dihydrothieno[3,2-c]pyridin-5(4H)-yl)-N-(5-(ethylthio)-1,3,4-thiadiazole-2 -base) the preparation of acetamide (compound I-1)

[0061]

[0062] Add 23.7g of intermediate III-1, 100mL of acetonitrile, 20.2g of triethylamine, and 17.5g of 4,5,6,7-tetrahydrothiophene [3,2] into a reaction flask equipped with stirring, condenser, and thermometer. -c] Pyridine hydrochloride, stirred at room temperature for 5 hours, washed the reaction solution with 3×50mL saturated brine, extracted with ethyl acetate, fully dried with anhydrous sodium sulfate, filtered, and evaporated to exhaust the ethyl acetate under reduced pressure, that is, Reddish-brown oil, separated by column [mobile phase: v (petroleum ether): v (ethyl acetate) = 3: 2], Rf = 0.51, and a white solid (HPLC: 99.4%) was obtained. 1 H NMR (CDCl 3 , 400MHz) δ: 1.311-1.347 (t, 3H, -CH 3 ), 2.481-2.499 (m, 2H, -CH 2 CH 2 -), 2.819-2.888 (m, 2H, -CH 2 CH 2 -), 3.184-3.239 (q, 2H, -CH 2 CO-), 3.546(s, 2H, -C...

Embodiment 2

[0068] Formation of compound 1 into hydrochloride: take 2.0 g of the white solid product of compound 1 and dissolve it in 10 mL of anhydrous ether. Cool in an ice-water bath to 0°C, add dropwise 25% diethyl ether solution of hydrochloric acid until the pH is 2, and continue to stir for about 1 h under an ice-water bath. Filter to obtain a white solid.

[0069] In order to more fully illustrate the pharmaceutical composition of the thiadiazole derivatives of the present invention, the following formulation examples are provided below, and the examples are for illustration only, and are not intended to limit the scope of the present invention.

Embodiment 3

[0071] Prepare hard gelatin capsules with the following ingredients:

[0072]

[0073] Preparation process: pre-dry the raw and auxiliary materials, and pass through a 100-mesh sieve for later use. The above ingredients are mixed according to the prescription amount and filled into hard gelatin capsules.

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PUM

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Abstract

The invention belongs to the technical field of anti-tumor medicaments, and provides a thiadiazole derivative with a structure of a formula I. In the formula I, R<1> is hydrogen, methyl and ethyl, and R<2> is the hydrogen, chlorine, bromine, the methyl, methylmercapto, ethylthio, methoxy carbonyl, carbethoxy, methoxyphenyl, bromophenyl and phenoxymethyl. The invention also relates to a preparation method for the compound, and discloses a medicinal composition in which a compound or a pharmaceutically-acceptable salt thereof are taken as active ingredients and application of the compound or the pharmaceutically-acceptable salt of the compound which serve as the anti-tumor medicaments.

Description

technical field [0001] The invention belongs to the technical field of medicine, more specifically, relates to a class of compounds with anti-tumor effect and their preparation method and application. Background technique [0002] Cancer has become a major chronic disease that seriously endangers human health. According to statistics, there are 9 million people who suffer from cancer every year in the world, and 6 million patients die from cancer. Almost one cancer patient dies every second. The annual incidence of cancer in my country is about 1.2 million, the number of cancer deaths is as high as more than 900,000, and the number of patients waiting for treatment exceeds 1.5 million, and there is an increasing trend year by year. Therefore, cancer has become the second largest killer after cardiovascular disease. Clinically, tumors are treated in three major ways: surgery, radiotherapy, and chemotherapy. Although the chemotherapy method is quicker, the cure rate is very...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61K31/4365A61P35/00
Inventor 黄淑云李兴伟支爽王平保刘登科
Owner 天津天诚新药评价有限公司