摘要:
Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y = SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要:
The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
摘要:
The invention relates to ortho-substituted anthranilic acid amides and to their use as medicaments for treating medical disorders, which are triggered by persistent angiogenesis.
摘要:
The invention relates to ortho-substituted anthranilic acid amides and to their use as medicaments for treating medical disorders, which are triggered by persistent angiogenesis.
摘要:
The invention relates to selected anthranylamide pyridones that inhibit VEGFR-2 and VEGFR-3 and to their use as medicaments for treating diseases that are triggered by persistent angiogenesis.
摘要:
The invention relates to substituted N-oxide anthranylamide derivatives, to the production thereof and to their use as medicaments for treating diseases that are triggered by persistent angiogenesis. The inventive compounds can be used in the case of psoriasis, Kaposi's sarcoma, restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia, arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma, eye diseases, such as diabetic retinopathy, neovascular glaucoma, renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombotic microangiopathic syndromes, transplant rejections and glomerulopathy, fibrotic diseases such as cirrhosis of the liver, mesangial cell-proliferative diseases, arteriosclerosis, injuries of the nerve tissue, and for inhibiting the reocclusion of vessels after balloon catheter treatment, for use in vascular prosthetics or after inserting mechanical devices for holding vessels open such as, e.g. stents, as immunosuppressants, as an aid in scar-free wound healing, and for treating age spots and contact dermatitis. The inventive compounds can also be used as VEGFR-3 inhibitors in lymphangiogenesis.
摘要:
The invention relates to substituted cyanoanthranilamide derivatives, to the production and use thereof as medicaments for the treatment of diseases triggered by persistent angiogenesis. The inventive compounds can be used, for instance in psoriasis, Kaposis sarcoma, restenosis, e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia, arthritis, e.g. rheumatoid arthritis, hemangioma, angiofribroma, eye diseases, e.g. diabetic retinopathy, neovascular glaucoma, kidney diseases, e.g. glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombotic microangiopatic syndrome, transplantation rejections and glomerulopathy, fibrotic diseases such as liver cirrhosis, mesangial cell proliferative diseases, arteriosclerosis, injuries of nerve tissue and inhibition of reocclusion of blood vessels after balloon catheter treatment, in vascular prosthetics or after implantation of mechanical devices for keeping blood vessels open, e.g. stents, as immunosuppressants, as aid in scarless wound healing, age spots and contact dermatitis. The inventive compounds can also be used as VEGFR-3 inhibitors in lymphangiogenesis. The invention further relates to compounds of general formula (I), wherein A represents group -N(R7)-; Y1 to Y5 represent a nitrogen atom or group -CY6; Y6 represents cyano, halogen, C¿1?-C6-alkyl, C1-C6-alkoxy, amino or hydroxy, wherein at least one nitrogen atom is contained in the ring and at least one cyano radical is contained in the ring.
摘要:
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.
摘要:
The invention relates to substituted cyanoanthranilamide derivatives, to the production and use thereof as medicaments for the treatment of diseases triggered by persistent angiogenesis. The inventive compounds can be used, for instance in psoriasis, Kaposis sarcoma, restenosis, e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia, arthritis, e.g. rheumatoid arthritis, hemangioma, angiofribroma, eye diseases, e.g. diabetic retinopathy, neovascular glaucoma, kidney diseases, e.g. glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombotic microangiopatic syndrome, transplantation rejections and glomerulopathy, fibrotic diseases such as liver cirrhosis, mesangial cell proliferative diseases, arteriosclerosis, injuries of nerve tissue and inhibition of reocclusion of blood vessels after balloon catheter treatment, in vascular prosthetics or after implantation of mechanical devices for keeping blood vessels open, e.g. stents, as immunosuppressants, as aid in scarless wound healing, age spots and contact dermatitis. The inventive compounds can also be used as VEGFR-3 inhibitors in lymphangiogenesis. The invention further relates to compounds of general formula (I), wherein A represents group -N(R7)-; Y1 to Y5 represent a nitrogen atom or group -CY6; Y6 represents cyano, halogen, C¿1?-C6-alkyl, C1-C6-alkoxy, amino or hydroxy, wherein at least one nitrogen atom is contained in the ring and at least one cyano radical is contained in the ring.