C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/14 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61P 29/00 (2006.01) C07D 213/81 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/14 (2006.01)
Patent
CA 2453223
The invention relates to selective anthranilamide pyridine amides as inhibitors of VEGFR-2 and VEGFR-3 and to their production and use as medicaments for treating diseases that are caused by persistent angiogenesis. The inventive compounds can be used for example in cases of psoriasis, Kaposi's sarcoma, restenosis, such as e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukaemia, arthritis, such as rheumatoid arthritis, haemangioma, angiofibromatosis, in eye diseases such as diabetic retinopathy, neovascular glaucoma, in kidney diseases such as glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombic micro-angiopathic syndrome, transplant rejection and glomerulopathy, in fibrotic diseases such as hepatic cirrhosis, mesangial-cell proliferative diseases, arteriosclerosis, damage to the nerve tissue and inhibition of the re-occlusion of vessels after balloon catheter treatment, in vessel prosthetics or after the use of mechanical devices for keeping vessels open, e.g. stents, as immunosuppressants, to support wound healing without scars and in cases of age spots and contact dermatitis. The inventive compounds can also be used as inhibitors of VEGFR-3 in lymphangiogenesis for hyperplastic and dysplastic changes in the lymphatic system.
L'invention concerne des anthranylamides pyridine amides sélectives en tant qu'inhibateurs VEGFR-2 et VEGFR-3, leur préparation et leur utilisation sous forme de médicament pour soigner des maladies provoquées par des angiogenèses persistantes. Les composés faisant l'objet de l'invention peuvent être utilisés dans dans les cas suivants : psoriasis, sarcome de Kaposi, resténose comme la resténose induite par un stent, endométriose, maladie de Crohn, maladie de Hodgkin, leucémie, arthrite comme la polyarthrite rhumatoïde, hémangiome, angiofibrome, maladies oculaires comme la rétinopathie diabétique, glaucome néovasculaire, maladies rénales comme la glomérulonéphrite, néphropathie diabétique, néphrosclérose maligne, syndrome de microangiopathie thrombique, rejets de transplantations et glomérulopathie, maladies fibrotiques comme la cirrhose du foie, maladies de prolifération cellulaire mésangiale, arthériosclérose, endommagements du tissu nerveux et inhibition de la réocclusion de vaisseaux après traitement par cathéter à ballonnet, prothétique des vaisseaux ou après la pose de dispositifs mécaniques pour maintenir des vaisseaux ouverts comme des stents, comme immunosuppresseurs, comme support de subérification de blessure sans cicatrice, taches de vieillesse et dermite de contact. Les composés selon l'invention sont également utiles en tant qu'inhibiteurs VEGFR-3 en cas de lymphangiogenèse lors de modifications hyperplasiques et dysplasiques du système lymphatique.
Ernst Alexander
Haberey Martin
Huth Andreas
Krueger Martin
Menrad Andreas
Marks & Clerk
Schering Aktiengesellschaft
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