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Novel coumarin derivative having antitumor activity

A compound, methyl technology, applied in the field of novel coumarin derivatives

Active Publication Date: 2011-10-19
CHUGAI PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Thus, although some coumarin derivatives having antitumor activity are known, there are few compounds showing antitumor activity as high as a practical level as an anticancer agent.

Method used

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  • Novel coumarin derivative having antitumor activity
  • Novel coumarin derivative having antitumor activity
  • Novel coumarin derivative having antitumor activity

Examples

Experimental program
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Effect test

manufacture example

[0659] In the following production examples (synthesis examples), NMR analysis was performed using JNM-EX270 (270 MHz) manufactured by JEOL Corporation, JNM-GSX400 (400 MHz) manufactured by JEOL Corporation, or ARX-300 (300 MHz) manufactured by Bruka Corporation, and the NMR data were expressed in ppm (parts permillion, δ) are shown, referenced to the deuterium lock signal from the sample solvent.

[0660] In addition, mass spectrum data were obtained using JMS-DX303 manufactured by JEOL, JMS-SX / SX102A manufactured by JEOL, or a micro mass spectrometer (Navigator manufactured by Finningan) equipped with Agilent 1100 gradient high performance liquid chromatography manufactured by Agilent Technologies.

[0661] In the case of using a commercially available reagent, it was directly used for the reaction without performing pretreatments such as distillation and recrystallization. As a reaction solvent, when a commercially available solvent is used, an anhydrous solvent is used.

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PUM

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Abstract

The present invention provides a compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof. Because of having a sufficiently high antitumor activity, this compound or its salt is useful as a remedy for cell proliferative diseases, in particular, cancer. It is also intended to provide a medicinal composition which contains the above-described compound or its salt as the active ingredient. [Chemical formula 1] (1) wherein X is selected from heteroaryl, etc.; Y<1> and Y<2> are selected from -N=, etc.; Y<3> and Y<4> are selected from -CH=, etc.; A is selected from sulfamide, etc.; R<1> is selected from hydrogen, etc.; and R<2> is selected from C1-6 alkyl, etc.

Description

technical field [0001] The invention relates to a novel coumarin derivative with anti-tumor activity and a pharmaceutical composition using it as an active ingredient, especially a therapeutic agent for cell proliferation diseases. Background technique [0002] It is known that coumarin derivatives, that is, compounds derivatized at various positions using a coumarin skeleton as a core, have various pharmacological effects depending on the position of chemical modification (Non-Patent Document 31). For example, warfarin having an antithrombotic effect is widely known as a drug having a coumarin skeleton (Non-Patent Document 1). In addition, coumarin derivatives that act on various target proteins and have anti-tumor activity, or inhibit proteins related to anti-tumor activity, can be obtained by chemically modifying different positions of the mother nucleus. [0003] In addition, coumarin derivatives exhibiting antitumor activity by inhibiting steroid sulfatase have been re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/18A61K31/352A61K31/427A61K31/443A61K31/506A61P35/00C07D401/06C07D405/12C07D405/14C07D417/12C07D491/052
CPCC07D311/18C07D405/12C07D417/12A61P35/00C07D491/052A61K31/352C07D405/14
Inventor 饭仓仁兵藤郁美青木纪裕古市纪之松下正行渡边史郎小泽佐和子堺谷政弘扈泌秀富井靖志高梨贤二原田直树
Owner CHUGAI PHARMA CO LTD
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