Abstract: The present invention relates to novel compounds selected from 2-aminoaryloxazoles of formula I 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, FGFR3 and/or Flt-3 inhibitors.

Abstract: The present invention relates to a method for treating type II diabetes, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from non-toxic, selective and potent c-kit inhibitors.

Abstract: The present invention relates to a method for whitening human skin and treating melanocyte dysfunction associated diseases comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a screening method allowing the identification and selection of compounds targeting the transphosphorylase (also called phosphotransferase) domain of c-kit, more particularly compounds selected to be potent inhibitors of constitutively activated c-kit, while being unable to inhibit other activation pathways as for example the pathways leading to death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: Novel compounds selected from 2-(3-aminoaryl) amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions 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 inhibitors.

Abstract: The present invention relates to a method for treating CNS disorders, more particularly selected from the group consisting of depression, schizophrenia, anxiety, migraine, memory loss, pain and neurodegenerative diseases, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating substance use disorders, more particularly drug addiction, drug habituation, drug dependence, withdrawal syndrome and overdose, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating autoimmune diseases, more particularly selected from the group consisting of multiple sclerosis, ulcerative colitis, Chron's disease, rheumatoid arthritis and polyarthritis, scleroderma, lupus erythematosus, dermatomyositis, pemphigus, polymyositis, vasculitis, as well as graft-versus host diseases, comprising administering a compound capable of depleting mast cells to a mammal in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly on-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a screening method allowing the identification and selection of compounds capable of depleting mast cells, wherein said compounds do not show significant toxicity for other hematopeitic cells that are not mast cells or related cell or cell lines, such as SCF independent expanded human normal CD34+ cells.

Abstract: The present invention relates to a method for treating inflammatory diseases such as rheumatoid arthritis (RA), comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating mastocytosis comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor, wherein said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3. The invention also contemplates a composition for topical application comprising said inhibitor for treating category I mastocytosis.

Abstract: The present invention relates to a method for inhibiting tumor angiogenesis comprising administering a c-kit inhibitor to a human in need of such treatment, more particularly a non toxic, potent and selective c-kit inhibitor, wherein said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating bone loss such as osteoporsis comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferbly, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating inflammatory bowel diseases (IBD), such as crohn's disease, comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating allergic diseases such as asthma, comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating Multiple Sclerosis (MS) comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating interstitial cystitis, comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, potent and selective c-kit inhibitor, wherein said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to a method for treating bacterial infections, preferably infections caused by FimH expressing bacteria, comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non toxic, potent and selective c-kit inhibitor, wherein said inhibitor is unable to promote detah of IL-3 dependent cells cultured to presence of IL-3.

Abstract: The present invention relates to a method for promoting hair growth, preventing or minimizing hair loss comprising administering a tyrosine kinase inhibitor to a human in a need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

Abstract: The present invention relates to novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles 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 inhibitors.