发明名称 2,6-substituted-4-monosubstituted amino-pyrimidine as prostaglandin D2 receptor antagonists
摘要 Disclosed are the compounds 1-{ 6-[2-(2,4-Dicbloro-phenyl)-ethylamino]-2-methyl-pyrimidin-4-yl} -pyrrolidine-3-carboxylic acid, 2-(1-{ 2-Methoxy-6-[2-(4-trifluorometboxy-phenyl)-ethylamino]-pyrimidin-4-yl} -piperidin-3-yl)-2methyl- propionic acid, 2-[3-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -5-(l-hydroxy-1-methylethyl)-phenyl]-propan-2-ol, [6-(3-Amino-piperidin-l-yl)-2-methoxy-pyrimidin-4-yl]-[2-(2,4-dichloro-phenyI)-ethyl]-amine, [6-(4-amino-piperidin-l-yl)-2-methoxy-pyrimidin-4-yI]-[2-(2,4-dichloro-phenyl)-ethyl]-amine, N-(1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidin-4-yl)-acetamide, S-{ 6-[2-(2,4-0ichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -1-methyl-2,3-dihydro-1H-indole-2-carboxylic acid, 2-Methyl-propane-2-sulfonic acid [2-(3-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxypyrimidin-4-yl} -phenyI)-2-methyl-propionyl]-amide, 10 N,N-dimethylamide-2-sulfonic acid [2-(3- { 6-[2-(2,4-dich1oro-phenyl)-ethylamino]-2-methoxypyrimidin-4-yl} -phenyl)-2-methyl-propionyl]-amide, 2-(3-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -phenyl)-2-methyl-1-thiomorpholin-4-yl-propan-1-one, 2-(3-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -phenyl)isobutyramide, 2-(3-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -phenyl)-N,N dimethylisobutyramide, (1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidin-3-yl)-acetic acid, 1-{ 2-Methoxy-6-[2-(4-tritluoromethoxy-phenyl)-ethylamino]-pyrimidin-4-yl} -piperidine-3-carboxylic acid, N-(1-{ 2-Methoxy-6-[2-(4-trifluoromethoxy-phenyl)-ethylamino]-pyrimidin-4-yl} -piperidine-3-carbonyl)-methanesulfonamide,s-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -1-methyl-2,3-dihydro-IH-indole-2-carboxylic acid ethyl ester, (1-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidin-3-yl)-acetic acid ethyl ester, N-(1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidine-3-carbonyl)methanesulfonamide Ethanesulfonic acid (1-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} piperidine-3-carbonyl)-amide, 2-Methyl-propane-2-sulfonic acid (1-{ 6-[2-(2,4-dichlorophenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidine-3-earbonyl)-amide, N-(1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidine-3-carbonyl), trifluoro-methanesulfonamide, 1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrlmidin-4-yl} -piperidine-3-carboxylic acid(IH-tetrazol-5-yl)-amide, 1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrlmidin-4-yl} -piperidine-3-carboxylic acid amide, 1-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -piperidine-3-carboxylic acid dimethylamide, N,N-Dimethylamide-2-sulfonic acid 1-{ 6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxypyrimidin-4-yl} -piperidine-3-carboxamide, 5-{ 2-Methoxy-6-[2-(4-tritluoromethoxy-phenyl)-ethylamino]-pyrimidin-4-yl} thiophene-2-carboxylic acid, or 5-{ 6-[2-(2,4-Dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl} -2,3-dihydrobenzofuran-2-carboxylic acid, or a pharmaceutically acceptable salt, hydrate, or solvate thereof. Also Use of the compound or a pharmaceutically acceptable salt, hydrate or solvate thereof according in the manufacture of a medicament for treating an allergic disease, systemic mastocytosis. a disorder accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, a disease accompanied by itch, a disease which is generated secondarily as a result of behaviour accompanied by itch, inflammation.,chronic obsttuctive pulmonary diseases, ischemic reperfusion injury cerebrovascular accident, chronic rheumatoid arthritism, pleurisy or ulcerative colitis.
申请公布号 NZ571793(A) 申请公布日期 2011.08.26
申请号 NZ20070571793 申请日期 2007.04.12
申请人 SANOFI-AVENTIS 发明人 STEFANY, DAVID;HARRIS, KEITH JOHN;GILLESPY, TIMOTHY ALAN;GARDNER, CHARLES J;AGUIAR, JOACY C
分类号 C07D403/04;A61K31/505;A61P11/00;C07D239/46;C07D409/04 主分类号 C07D403/04
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