| 主权项 |
1. A method for treating a disease selected from rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, a disease which is due to overexpression of tumor necrosis factor alpha (TNFα) or an increased concentration of TNFα selected from Crohn's disease and intestinal ulcers, and treatment of an acute or chronic rejection reaction on the part of the organ recipient against the transplanted organ, in a patient in need thereof, comprising administering to such patient a pharmaceutically effective amount of a compound according to formula (I): wherein:
X is N or CH;M is N or CH; R1 is hydrogen,
halogen chosen from F, Cl, I and Br,—(C1-C4)-alkyl,—CN,—CF3,—OR5, wherein R5 is hydrogen or —(C1-C4)-alkyl,—N(R5)—R6, wherein R5 and R6 are selected from hydrogen and —(C1-C4)-alkyl,—C(O)—R5, wherein R5 is hydrogen or —(C1-C4)-alkyl, or—S(O)x—R5, wherein x is the integer zero, 1 or 2, and wherein R5 is hydrogen or —(C1-C4)-alkyl; R2 is a heteroaryl radical, which is selected from 3-hydroxypyrro-2,4-dione, imidazole, imidazolidine, imidazoline, indazole, isothiazole, isothiazolidine, isoxazole, 2-isoxazolidine, isoxazolidine, isoxazolone, morpholine, oxazole, 1,3,4-oxadiazole, oxadiazolidinedione, oxadiazolone, 1,2,3,5-oxathiadiazole-2-oxide, 5-oxo-4,5-dihydro[1,3,4]oxadiazole, 5-oxo-1,2,4-thiadiazole, piperazine, pyrazine, pyrazole, pyrazoline, pyrazolidine, pyridazine, pyrimidine, tetrazole, thiadiazole, thiazole, thiomorpholine, triazole and triazolone, wherein the heteroaryl radical is optionally substituted one, two, or three times by —C(O)—R5, wherein R5 is selected from hydrogen and —(C1-C4)-alkyl, —(C1-C4)-alkyl, —O—R5, wherein R5 is selected from hydrogen and —(C1-C4)-alkyl, —N(R5)—R6, wherein R5 and R6 are each selected from hydrogen and —(C1-C4-alkyl), halogen, or a keto radical, —C(O)—OR5, wherein R5 is hydrogen or —(C1-C4-alkyl), or —C(O)—N(R7)—R8, wherein R7 and R8 are each selected from hydrogen, —(C1-C4)-alkyl-OH, —O—(C1-C4)-alkyl and —(C1-C4-alkyl); R3 is hydrogen or —(C1-C4-alkyl); R4 is a heteroaryl radical, which is selected from pyrrole, furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, isothiazole, tetrazole, 1,2,3,5-oxathiadiazole-2-oxides, triazolones, oxadiazolone, isoxazolone, oxadiazolidinedione, triazole, 3-hydroxypyrro-2,4-diones, 5-oxo-1,2,4-thiadiazoles, pyridine, pyrazine, pyrimidine, indole, isoindole, indazole, phthalazine, quinoline, isoquinoline, quinoxaline, quinazoline, cinnoline, β-carboline and benzofused cyclopenta derivatives or cyclohexa derivatives of the heteroaryl radical, wherein the heteroaryl radical is optionally substituted one, two or three times by —(C1-C5)-alkyl, —(C1-C5)-alkoxy, halogen, nitro, amino, trifluoromethyl, hydroxyl, hydroxy-(C1-C4)-alkyl, methylenedioxy, ethylenedioxy, formyl, acetyl, cyano, hydroxycarbonyl, aminocarbonyl or —(C1-C4)-alkoxycarbonyl, or an aryl radical which is selected from phenyl, naphthyl, 1-naphthyl, 2-naphthyl, biphenylyl, 2-biphenylyl, 3-biphenylyl and 4-biphenylyl, anthryl and fluorenyl, wherein the aryl radical is optionally substituted one, two, or three times by —(C1-C5)-alkyl, —(C1-C5)-alkoxy, halogen, nitro, amino, trifluoromethyl, hydroxyl, hydroxy-(C1-C4)-alkyl, methylenedioxy, ethylenedioxy, formyl, acetyl, cyano, hydroxycarbonyl, aminocarbonyl or —(C1-C4)-alkoxycarbonyl; and R11 is hydrogen,
halogen chosen from F, Cl, I and Br,—(C1-C4)-alkyl,—CN,—CF3,—OR5, wherein R5 is hydrogen or —(C1-C4)-alkyl,—N(R5)—R6, wherein R5 and R6 are selected from hydrogen and —(C1-C4)-alkyl,—C(O)—R5, wherein R5 is hydrogen or —(C1-C4)-alkyl, or—S(O)x—R5, wherein x is the integer zero, 1 or 2, and wherein R5 is hydrogen or —(C1-C4)-alkyl, or a stereoisomer or a mixture of stereoisomers in any ratio of the compound, or a pharmaceutically acceptable salt of the compound. |
