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Pyridyl thiazole amines compound, as well as medical composite and application thereof

A technology of pyridylthiazolamides and compounds, which can be applied in drug combination, organic chemistry, antineoplastic drugs, etc., and can solve the problems of narrow clinical application range and drug-induced drug resistance gene mutations, etc.

Active Publication Date: 2012-03-21
东莞粤港澳干细胞生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In fact, most of the current protein tyrosine kinase inhibitor anti-tumor drugs have drug-induced drug-resistant gene mutations, and face problems such as narrow clinical application and

Method used

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  • Pyridyl thiazole amines compound, as well as medical composite and application thereof
  • Pyridyl thiazole amines compound, as well as medical composite and application thereof
  • Pyridyl thiazole amines compound, as well as medical composite and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] N-(5-(4-methyl-1H-imidazole-1-substituted)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridine-3-substituted-thiazole -2-substituted amino)-benzamide (D573)

[0141] (N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino) -benzamide)

[0142]

[0143] Step 1. 3-(3-acetylthioureido)-4-methylbenzoate (Methyl3-(3-acetylthioureido)-4-methylbenzoate)

[0144]

[0145] Ammonium thiocyanate (3.8 g, 50 mmol) was dissolved in 50 mL of acetone, and a solution of acetyl chloride (3.90 g, 50 mmol) in 10 mL of acetone was added dropwise at 40°C, stirred for 1 h, then cooled to room temperature, and 3-amino- 75 mL of acetone solution of methyl 4-methylbenzoate (8.25 g, 50 mmol) was reacted at room temperature for 5 h, 100 mL of water was added, stirring was continued for 1 h, the precipitate was filtered, washed three times with water and three times with n-hexane, and dried under vacuum to obtain a white solid 11.3 grams (8...

Embodiment 2

[0165] N-(5-(1H-imidazole-1-substituted)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridine-3-substituted-thiazole-2-substituted amino )-Benzamide (D574)

[0166] (N-(5-(1H-imidazol-1-yl)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-benzamide)

[0167]

[0168] The synthesis method is as in Example 1.

[0169] 1 HNMR (400 MHz, d-DMSO), δ 10.71(s, 1H), 9.64(s, 1H), 9.15(s, 1H), 8.89(s, 1H), 8.46(d, J=4.0 Hz, 1H ), 8.34(m, 2H), 8.24(m, 2H), 7.81(s, 1H), 7.77(s, 1H), 7.68, (d, J=8.0 Hz, 1H), 7.53(s, 1H), 7.44(d, J=8.0 Hz, 1H), 7.39(m, 1H), 7.17(s, 1H), 2.40(s, 3H).

[0170] MS (ESI), m / z: 521 (M + +H + ).

Embodiment 3

[0172] N-(5-(1H-1,2,4-triazole-1-substituted)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridine-3- Substituted-thiazole-2-substituted amino)-benzamides (D593)

[0173] (N-(5-(1H-1,2,4-triazole-1-yl)-3-(trifluoromethyl)-phenyl)-4-methyl-3-(4-pyridin-3-yl-thiazol-2- ylamino)-benzamide)

[0174]

[0175] The synthesis method is as in Example 1.

[0176] 1 HNMR (400MHz, d-DMSO), δ10.74(s, 1H), 9.61(s, 1H), 9.44(s, 1H), 9.10(s, 1H), 8.84(s, 1H), 8.68(s, 1H), 8.45(d, J=4.0Hz, 1H), 8.29(s, 1H), 8.27(s, 1H), 8.21(d, J=8.0Hz, 2H), 8.00(s, 1H), 7.68, (d, J=8.0Hz, 1H), 7.52(s, 1H), 7.43(d, J=8.0Hz, 1H), 7.36, (m, 1H), 2.39(s, 3H).

[0177] MS (ESI), m / z: 522 (M + +H + ).

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Abstract

The invention discloses a pyridyl thiazole amines compound with the general formula (I), as well as a medical composite and application thereof. The compound and pharmaceutically acceptable salts or stereoisomers thereof can be applied to the preparation of medicines for treating or preventing tumors. The compound can effectively overcome drug resistance induced by Gleevec. The detailed definition of each group in the formula is shown in specifications.

Description

technical field [0001] The present invention belongs to the field of chemical medicine, in particular to pyridyl thiazole amine compounds with structural characteristics of formula (I) or pharmaceutically acceptable salts or stereoisomers and prodrug molecules thereof, and pharmaceutical combinations containing such compounds Compounds and the application of these compounds or compositions in the preparation of medicaments. Background of the invention [0002] Tumor is currently the number one killer of human health and life, and its incidence rate is second only to cardiovascular diseases. And with the impact of environmental pollution or other factors, the incidence of malignant tumors is rapidly increasing. According to the data released by the World Health Organization in 2003, there were 10 million malignant tumor patients in the world in 2000, and 6.2 million deaths due to malignant tumors, accounting for 12% to 25% of the total deaths. It is expected that by 2020, t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/14A61K31/4439A61K31/506A61P35/00
Inventor 丁克王德平裴端卿潘景轩张章冯玉冰罗坤甘继荣庄晓曦段磊
Owner 东莞粤港澳干细胞生物科技有限公司
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