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Use of thiazolidinone derivatives as antiangiogenic agents

A technology of thiazolidine and application, applied in the field of thiazolidinone compounds, can solve the problem that the mechanism of action is not completely clear and the like

Inactive Publication Date: 2007-12-05
欧洲细胞治疗责任有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mechanism of action of this compound is not fully understood (29)

Method used

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  • Use of thiazolidinone derivatives as antiangiogenic agents
  • Use of thiazolidinone derivatives as antiangiogenic agents
  • Use of thiazolidinone derivatives as antiangiogenic agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0086] Example - 4-(5-formyl-furan-2-yl)-benzoic acid methyl ester

[0087] 5-Bromofural (2.43g, 13.9mmole), 4-(methoxycarbonyl)phenylboronic acid (2.50g, 13.9mmole), tris(dibenzylideneacetone)palladium (0) (192mg, 0.2 mmole) and potassium fluoride (2.42 g, 41.7 mmole) in 1,4-dioxane (100 ml) was added to a solution of tri-tert-butylphosphine in hexane (10% by weight, 101 mg, 0.5 mmole). After heating at 65-70°C for 4 hours, the mixture was cooled to room temperature and treated with dichloromethane (150ml). After stirring for 10 minutes, the mixture was filtered through celite, and the filtrate was concentrated under reduced pressure. The residue was purified by flash chromatography on silica gel, eluting with ethyl acetate-hexane mixture (1:1), to give 4-(5-formyl-furan-2-yl)-benzoic acid methyl ester (2.6 g, 81 %Yield).

[0088] 1 H NMR (300MHz, CDCl 3 ): δ9.70(s, 1H), 8.10(d, 2H), 7.90(d, 2H), 7.35(d, 1H), 6.95(d, 1H), 3.98(s, 3H).

[0089] General Process B

[0...

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Abstract

The invention relates to the use of compounds of general formula (I), in which R1, R2 and X are as defined in the description for the preparation of pharmaceutical compositions for the treatment of pathologies in which inhibition of the interaction between HIF-1a and p300 is beneficial, in particular as antiangiogenic medicaments for the therapy of solid tumors.

Description

field of invention [0001] The present invention relates to thiazolidinone compounds capable of inhibiting the interaction between HIF-1α transcription factor and its coactivator p300 and preventing the production of vascular endothelial cell growth factor. Background of the invention [0002] Vascular endothelial growth factor plays a key role in physiological and physiopathological angiogenesis. Numerous mechanisms have been implicated in the regulation of the VEGF gene, with an essential role played by tissue oxygen tension, as evidenced by reversible increases in VEGF mRNA levels under hypoxic conditions in vivo and in vitro. The increased expression of VEGF mRNA is mainly mediated by the transcription factor HIF-1 (hypoxia-inducible factor-1), which binds to the binding site of the promoter region of the VEGF gene. [0003] A large number of experimental data show that: HIF-1 is an overall regulator of oxygen homeostasis, and the impairment of HIF-1 activity promotes th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61K31/5377C07D417/06C07D417/14A61P35/00A61P19/02A61P17/06A61P17/00A61P27/02A61P27/06
CPCC07D417/06C07D417/14A61K31/5377A61K31/427A61P1/02A61P1/04A61P11/00A61P13/08A61P15/00A61P17/00A61P17/06A61P19/02A61P25/00A61P27/02A61P27/06A61P35/00A61P43/00
Inventor M·卡辛G·科莱拉S·德穆纳里M·格鲁尼
Owner 欧洲细胞治疗责任有限公司
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