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BENZIMIDAZOLE DERIVATIVE, HUMAN CHYMASE INHIBITOR, THERAPEUTIC AGENT AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF

机译：基于苯并咪唑衍生物，人类化学酶抑制剂，治疗剂和基于其的药物组合物

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FIELD: organic chemistry, medicine, pharmacy.;SUBSTANCE: invention relates to benzimidazole derivatives or their salts useful in medicine of the general formula (1): wherein R¹ and R² can comprise similar or different values and represent independently of one another hydrogen atom, halogen atom, cyano-group, hydroxyl group, alkyl group comprising 1-4 carbon atoms, alkoxy-group comprising 1-4 carbon atoms, trifluoromethyl group; A represents unsubstituted, linear alkylene group comprising 1-7 carbon atoms; E represents group -COOR³ comprising 1-6 carbon atoms; G represents unsubstituted, linear alkylene group comprising 1-6 carbon atoms; M represents a simple bond or -S(O)_m- wherein m represents a whole number in the range 0, 1 or 2; J represents substituted or unsubstituted heterocyclic group comprising 4-10 carbon atoms and one heteroatom in ring taken among the group consisting of nitrogen atom or sulfur atom excluding unsubstituted pyridine ring; a substitute in indicated aromatic heterocyclic group is taken among halogen atom, cyano-group, linear alkyl group comprising 1-6 carbon atoms, linear alkoxy-group comprising 1-6 carbon atoms, trifluoromethyl group and trifluoromethoxy-group wherein one or more indicated substituted can be replaced by random positions in ring; X represents methane group (-CH=). Also, invention relates to a pharmaceutical composition used in inhibition of human chymase activity based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof in aims for prophylaxis and/or treatment of inflammatory disease, cardiovascular disease, allergic disease, respiratory disease or osseous either cartilaginous metabolic disease.;EFFECT: valuable medicinal properties of compounds and composition.;14 cl, 3 tbl, 20 ex

机译：技术领域本发明涉及可用于通式（1）的药物中的苯并咪唑衍生物或其盐：<图像文件=“ 00000002.GIF” he =“ 33” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 75” />其中R ^{1 和R ^{2 可以包含相似或不同的值，并且彼此独立地表示氢原子，卤素原子，氰基，羟基，具有1-4个碳原子的烷基，具有1-4个碳原子的烷氧基，三氟甲基; A代表包含1-7个碳原子的未取代的直链亚烷基; E表示含1-6个碳原子的-COOR ^{3 基团; G代表包含1-6个碳原子的未取代的直链亚烷基; M表示单键或-S（O）_{m -，其中m表示0、1或2范围内的整数; J表示取代基中的氮原子或硫原子中的4〜10个碳原子和环中的1个杂原子的取代或未取代的杂环基。在所示的芳族杂环基中的取代基选自卤素原子，氰基，包含1-6个碳原子的直链烷基，包含1-6个碳原子的直链烷氧基，三氟甲基和三氟甲氧基，其中一个或多个所示取代可以被戒指中的随机位置取代; X代表甲烷基团（-CH ＝）。本发明还涉及基于这些化合物用于抑制人糜酶活性的药物组合物。本发明提供了制备新的化合物和基于其的药物组合物，其目的是预防和/或治疗炎性疾病，心血管疾病，过敏性疾病，呼吸系统疾病或骨性或软骨性代谢性疾病。效果：化合物和组合物的有价值的医学特性。 14 cl，3 tbl，20前}}}}

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公开/公告号RU2263674C2

专利类型
公开/公告日2005-11-10

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申请/专利号RU20020122105
发明设计人 TSUTIJA NAOKI (JP);MATSUMOTO ESIJUKI (JP);SAJTOU KHIROSI (JP);MIZUNO TSUESI (JP);
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申请日2001-01-17
分类号C07D403/06;C07D409/06;A61K31/4184;A61P9/00;A61P11/00;A61P37/08;A61P29/00;A61P3/14;
国家 RU
入库时间 2022-08-21 22:01:53

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