Pyrimido [4,5-b] indole derivatives

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01) C07D 209/00 (2006.01) C07D 239/00 (2006.01)

Patent

CA 2464934

The present invention relates to pyrimido[4,5-b]indoles which are useful as an active ingredient of pharmaceutical preparations. The pyrimido[4,5-b]indoles of the present invention have MKK7 and MKK4 inhibitory activity, and can be used for the prophylaxis and treatment of diseases associated with MKK7 and MKK4 activity. Such diseases include, inflammatory and immunoregulatory disorders and diseases such as asthma, atopic dermatitis, rhinitis, allergic rhinitis, allergic diseases, COPD, septic shock, arthritis, joint diseases and myocardial injuries, as well as autoimmune pathologies such as rheumatoid arthritis, Grave's disease, and atherosclerosis. The compounds of the present invention are also useful for treatment of ischemia, myocardial injury, pulmonary hypertension, renal failure, Huntington's chorea and cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and focal ischemia.

L'invention porte sur des pyrimido[4,5-b]indoles utiles en tant que principe actif de compositions pharmaceutiques. Les pyrimido[4,5-b]indoles de la présente invention ont une activité inhibitrice sur MKK7 et MKK4 et peuvent s'utiliser dans la prévention et le traitement des maladies associées à l'activité des MKK7 et MKK4. Ces maladies comprennent des troubles inflammatoires et immunorégulateurs et des maladies telles que l'asthme, la dermatite atopique, la rhinite, la rhinite allergique, les maladies allergiques, la BPCO, le choc septique, l'arthrite, les maladies des articulations et les accidents du myocarde ainsi que des pathologies auto-immunes telles que la polyarthrite rhumatoïde, la maladie de Graves et l'athérosclérose. Les composés de la présente invention sont aussi utiles dans le traitement de l'ischémie, de la lésion myocardique, de l'hypertension pulmonaire, de l'insuffisance rénale, de la chorée de Huntington et de l'hypertrophie cardiaque ainsi que de maladies neurodégénératives telles que la maladie de Parkinson, la maladie d'Alzheimer et l'ischémie focale.

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