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Kinase inhibitors

A C1-C4, alkyl technology, applied in the field of kinase inhibitors, can solve the problems of high preparation cost, limited in vivo effect and therapeutic bioavailability and absorption

Inactive Publication Date: 2008-10-29
ELI LILLY & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

p38 kinase inhibitors or cytokine inhibitors are expensive to manufacture and can have bioavailability and absorption issues that limit in vivo efficacy and therapeutic use

Method used

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  • Kinase inhibitors
  • Kinase inhibitors
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Examples

Experimental program
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Effect test

preparation example 1

preparation example 2

preparation example 3

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Abstract

The present invention provides kinase inhibitors of Formula (I). Wherein R<1>, R<2>, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.

Description

Background of the invention p38 kinase is a mitogen-activated protein (MAP) kinase that belongs to the superfamily of serine-threonine kinases. This kinase is activated by extracellular stress such as heat, UV light and osmotic stress, and by inflammatory stimuli such as lipopolysaccharide. When activated, p38 kinase phosphorylates intracellular protein substrates that regulate the biosynthesis of the proinflammatory cytokines tumor necrosis factor alpha (TNFα) and interleukin-1β (IL-1β). These cytokines are involved in the pathology of many of the following disorders: Chronic inflammatory disorders (Lee, and others Ann.N.Y.Acad.Sci. , 696, 149-170 (1993); Muller-Ladner, Curr. Opin. Rheumatol. , 8, 210-220(1996)), cardiovascular and central nervous system disorders (Salituro, et al. Current Medicinal Chemistry , 6, 807-823 (1999)), and autoimmune disorders (Pargellis, et al. Nature Structural Biology , 9(4), 268-272(2002)). Furthermore, the phosphorylated form of mi...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61K31/44A61K31/497
Inventor J·A·巴斯蒂安J·A·布拉斯德布拉斯A·德迪奥斯K·J·胡奇亚克李铁朝B·罗佩斯德乌拉尔德－加门迪亚M·M·梅德M·R·迈尔斯M·A·波班斯石全仲伯禹
Owner ELI LILLY & CO