Substituted oxazole derivatives and their use as tyrosine kinase inhibitors

Abstract

The present invention relates to novel compounds selected from substituted oxazole derivatives that selectively modulate, regulate, and / or inhibit signal transduction mediated by certain native and / or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.

Description

technical field [0001] The present invention relates to substituted oxazole derivatives which selectively modulate, modulate and / or inhibit signal transduction mediated by certain native and / or mutant tyrosine kinases present in various human and animal diseases, such as cell proliferation, metabolism, allergies and genetic diseases. Notably, these compounds are potent and selective inhibitors of c-kit, bcr-abl and Flt-3. Background technique [0002] Tyrosine kinases are receptor-type or non-receptor-type proteins that transfer the terminal phosphate group of ATP to protein tyrosine residues, thereby activating or inactivating signal transduction pathways. These proteins are thought to be involved in a variety of cellular mechanisms that, when disrupted, cause abnormal cell proliferation, migration, and inflammation. [0003] So far, there are about 58 receptor tyrosine kinases. Including the well-known VEGF receptor (Kim et al. Nature 362, pp.841-844, 1993), PDGF recept...

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Problems solved by technology

[0011] None of the above compounds have been reported as potent and selective inhibitors of c-kit or the c-kit pathway

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