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 vitamin D derivatives of the formula (I), wherein Z is an optionally substituted carbocyclic or heterocyclic, optionally aromatic or heteroaromatic 5- or 6-membered ring or an optionally substituted condensed ring structure that consists of a 5-membered and a 6-membered ring or of two 6-membered rings, and Q, R1-R4, X1-X2 and Y1-Y3 have the meanings given in the description. The invention further relates to a method for their production, to the use of said derivatives in the preparation of medicaments, and to a method for producing compounds of the formula (Iia), wherein E represents any side chain, and R7, R8, Y2, Y3 and Y5 have the meanings given in the description. The invention also relates to the intermediates of both methods.
摘要:
The invention relates to novel vitamin D derivatives of general formula (I), a method for the production thereof, intermediate products of the method as well as the utilization thereof for producing medicaments.
摘要:
New 20-methyl-substituted vitamin D derivates have general formula (I), in which R1 is a hydrogen atom, a hydroxyl group or an alkanoyloxyl group with 1 to 12 carbon atoms or a benzoyloxyl group, R2 is a hydrogen atom or an alkanoyl group with 1 to 12 carbon atoms or a benzoyl group; and R3 is saturated or unsaturated, straight-chain or branched-chain hydrocarbon residue with up to 18 C atoms, possibly interrupted and/or substituted by one or several carbocyclic structures (C¿3-10?-cycloalkyl or cycloakenyl residues, the latter having up to 2 double bonds), possibly substituted by one or several hydroxyl, oxo, amino groups and/or by one or several halogen atoms, possibly having one or several oxygen, sulphur and/or nitrogen (as (a)) atoms as chaining members in the hydrocarbon residue. Also disclosed is a process for preparing the same. These new compounds have a strongly improved induction of cell differentiation (HL-60), with respect to calcitriol, and are suitable for preparing medicaments.
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 concerns 23-oxa derivatives of vitamins of the D-series, the derivatives having the formula (I), in which R?1, R2 and R4¿, independently of each other, may be a hydrogen atom or an acyl group with 1-9 carbon atoms; each R3 may be a hydrogen atom or a straight-chain or branched-chain alkyl group with 1-4 carbon atoms; and x is an alkylene residue-(CH¿2?)n-in which n =1, 2 or 3, neither of the R?3¿ groups being methyl or propyl when n = 1. The invention also concerns a method of preparing such derivatives. The compounds have a proliferation inhibiting and cell differentiating effect and are suitable for the production of medicaments.
摘要:
New 20-methyl-substituted vitamin D derivates have general formula (I), in which R1 is a hydrogen atom, a hydroxyl group or an alkanoyloxyl group with 1 to 12 carbon atoms or a benzoyloxyl group, R2 is a hydrogen atom or an alkanoyl group with 1 to 12 carbon atoms or a benzoyl group; and R3 is saturated or unsaturated, straight-chain or branched-chain hydrocarbon residue with up to 18 C atoms, possibly interrupted and/or substituted by one or several carbocyclic structures (C¿3-10?-cycloalkyl or cycloakenyl residues, the latter having up to 2 double bonds), possibly substituted by one or several hydroxyl, oxo, amino groups and/or by one or several halogen atoms, possibly having one or several oxygen, sulphur and/or nitrogen (as (a)) atoms as chaining members in the hydrocarbon residue. Also disclosed is a process for preparing the same. These new compounds have a strongly improved induction of cell differentiation (HL-60), with respect to calcitriol, and are suitable for preparing medicaments.