Triazole derivatives

A technology of derivatives and drugs, applied in the field of triazole derivatives, can solve the problems of tissue damage, treatment-dependent activation and harmfulness

Inactive Publication Date: 2009-01-14
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tumor cell tolerance to TGF-β has been shown to counteract multiple cytotoxic effects of radiotherapy and chemotherapy, and treatment-dependent activation of TGF-β in the stroma may be more deleterious because TGF-β makes the microenvironment more favorable for tumor growth, May produce tissue damage leading to fibrosis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0201] (R,S)-8-Hydroxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraazabenzene And [e] the preparation of azulene ("A1") was carried out in a scheme similar to the following scheme:

[0202]

[0203] 1.1 Preparation of 5-methoxy-2-nitroaniline

[0204] Dissolve 10 g of 5-chloro-2-nitroaniline in 100 ml of methanol, and add 32.3 g of sodium methoxide. The reaction mixture was refluxed for 18 hours under boiling. After cooling, the mixture was evaporated to dryness, 500 ml of water were added and the crude product was isolated by filtration. After drying, 9.15 g of 5-methoxy-2-nitroaniline are obtained.

[0205] 1.2 Preparation of (R, S)-3-(5-methoxy-2-nitrophenylamino)-2-methyl-propionic acid

[0206] 9.15 g of 5-methoxy-2-nitroaniline were dissolved in 60 ml of THF, 6.5 ml of 2-methacrylonitrile and 1.35 ml of a 40% solution of benzyltrimethylammonium hydroxide in methanol were added. The reaction mixture was heated at the boil for about 20 hours and...

Embodiment A

[0244] Example A: Injection Vials

[0245] A solution of 100 g of the active ingredient of formula I and 5 g of disodium hydrogen phosphate in 3 L of double-distilled water was adjusted to pH 6.5 with 2N hydrochloric acid, sterile filtered, transferred to injection vials, lyophilized under sterile conditions and sterilized. condition sealed. Each injection vial contains 5 mg of active ingredient.

Embodiment B

[0246] Example B: Suppositories

[0247] A mixture of 20 g of the active ingredient of formula I with 100 g of soy lecithin and 1400 g of cocoa butter was melted, poured into moulds and allowed to cool. Each suppository contains 20 mg of active ingredient.

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Abstract

Novel triazole derivatives are inhibitors of TGF-beta receptor I kinase, for the treatment of tumours.

Description

Background of the invention [0001] The object of the present invention was to find new compounds having valuable properties, in particular new compounds which can be used for the preparation of medicaments. [0002] The present invention relates to compounds and the use of compounds in which the inhibition, regulation and / or regulation of signal transduction of kinases, in particular TGF-beta receptor kinases, plays a role, and to compounds comprising these The pharmaceutical composition of and the use of said compound for treating diseases induced by kinases. [0003] Transforming growth factor β is the prototype of the TGF-β superfamily, a family of highly conserved multifunctional growth factors that have important functions in both embryonic development and adult organisms. In mammals, three subtypes of TGF-β have been identified (TGF-β1, 2 and 3), with TGF-β1 being the most common subtype (Kingsley (1994) Genes Dev 8:133-146). TGF-β3 is expressed only in, for example, m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D513/04A61K31/55A61K31/38A61P35/00
CPCC07D513/04C07D471/14C07D487/04A61P17/02A61P25/28A61P31/18A61P35/00A61P35/02A61P35/04A61P9/00A61P9/10A61K31/38A61K31/55
Inventor B·塞尚C·阿门特H·格雷纳尔U·格拉德勒G·赫尔策曼
Owner MERCK PATENT GMBH
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