Novel cyanopyridine derivatives useful in the treatment of cancer and other disorders

A cyano- and pyridyl-based technology, which is applied in the field of treatment of hyperproliferative and angiogenic diseases, and can solve problems such as hyperproliferative blood vessels and blindness

Inactive Publication Date: 2006-09-27
BAYER HEALTHCARE LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] For example, under extreme hypoxia, overexpression of VEGF can cause intraocular angiogenesis, resulting in hyperproliferation of blood vessels, and eventually blindness

Method used

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  • Novel cyanopyridine derivatives useful in the treatment of cancer and other disorders
  • Novel cyanopyridine derivatives useful in the treatment of cancer and other disorders
  • Novel cyanopyridine derivatives useful in the treatment of cancer and other disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0421] Unless otherwise stated, all reaction conditions, methods, abbreviations and reagents are as follows. All temperatures are in degrees Celsius (° C.) and all parts and percentages are by weight. Technical grade reagents and solvents were used without further purification.

[0422] Abbreviations used in this manual

[0423] DBU 1,8-diazabicyclo[5.4.0]undec-7-ene

[0424] DMF N,N-Dimethylformamide

[0425] DCM dichloromethane

[0426] DCE 1,2-Dichloroethane

[0427] DMSO Dimethyl Sulfoxide

[0428] HPLC high pressure liquid chromatography

[0429] MPLC Medium Pressure Liquid Chromatography

[0430] LC-MS Liquid Chromatography-Mass Spectrometry

[0431] RT retention time

[0432] MP melting point

[0433] NMR nuclear resonance spectrum

[0434] TLC thin layer chromatography

[0435] ES Electrospray

[0436] DMAC N,N-Dimethylacetamide

[0437] HRMS High Resolution Mass Spectrometry

[0438] CDI 1,1'-carbonyldiimidazole

[0439] HOBT 1-Hydroxybenzotriazole

[0...

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PUM

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Abstract

This invention relates to novel diaryl ureas of Formula (I), pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyperproliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Description

[0001] related application [0002] This application claims priority to applications 60 / 450,323, filed February 28, 2003, 60 / 450,324, filed February 28, 2003, and 60 / 450,348, filed February 28, 2003. technical field [0003] The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and the use of these compounds or compositions as single active agents or in combination with other active ingredients such as cytotoxic treatments for the treatment of hyperproliferative and angiogenic disorders. Background of the invention [0004] Activation of the Ras signaling pathway represents a cascade of events with profound effects on cell proliferation, differentiation and transformation. Raf kinases, as downstream effectors of Ras, are considered to be key transmitters of these signals from cell surface receptors to the nucleus (Lowy, D.R.; Willumsen, B.M. Ann. Rev. Biochem. 1993, 62, 851; Bos, J.L. Cancer Res .1989, 49, 4682). It has bee...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D405/12C07D213/79C07D417/12A61K31/443A61K31/444A61K31/4433A61K31/4436A61P35/00A61K31/35C07D213/00C07D251/00
CPCC07D401/12C07D213/00A61K31/35C07D251/00Y02A50/30C07D405/14A61P35/00A61K31/53A61K45/06A61K2300/00
Inventor 威廉·J·斯科特雅克·迪马斯蒂芬·博耶尔温迪·李陈元伟巴顿·菲利普斯沙拉德·维尔马陈健青陈智樊建梅布赖恩·劳登布什阿尼科·雷德曼易林朱清明
Owner BAYER HEALTHCARE LLC
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