首页> 外国专利> Derivatives of 5, 6, 7, 8 - tetrahidroimidazo 1,5a pyridine with aldosterone synthase Inhibitory activity, Pharmaceutical compositions containing them and their use in the preparation of drugs for the treatment of hiperaldosterismo and Cushing's Syndrome.

Derivatives of 5, 6, 7, 8 - tetrahidroimidazo 1,5a pyridine with aldosterone synthase Inhibitory activity, Pharmaceutical compositions containing them and their use in the preparation of drugs for the treatment of hiperaldosterismo and Cushing's Syndrome.

机译:具有醛固酮合酶抑制作用的5、6、7、8-四氢咪唑基1,5a []吡啶衍生物,含有它们的药物组合物及其在制备治疗类风湿性关节炎和库欣氏综合症的药物中的用途。

摘要

Pharmaceutical compositions containing them and their use in the manufacture of Medicines with Inhibitory activity of aldosterone synthase for the treatment and Prevention of Cushing's Syndrome, hypokalemia, hypertension, Primary and Secondary hiperaldosterismo and related diseases.Claim 1: a compound of General formula (1), in which X is n; c; Z is a link); R is H or alkyl); b is C1 C1 - 8 8 -, alkoxy, halogen or trifluoromethyl; r1 is alkyl alquenilo C1 - C2 - 8, 8, alquinilo C2 - 8 - alkyl, aryl or heterociclil C0 C0 - 4 - 4 unsaturated, whose Radicals are not s Ustituidos or are substituted by alkoxy C1 1 - 4 - 8 - alkoxy alkyl 8carbonilo C1, C1 - 8Alquilcarbonilo C0 - C1 - 8 8 alquilsulfonilo, aryl alkoxy C0 - 4 - aryl carbonyl, halogen, heterociclilo, cyano, trifluoromethyl, Oxo, trifluoromethoxy, or tri silyl c1-4 alkyl; R2 is H); or (b) is 8 C1 - C3 alkyl, cycloalkyl - 8, halogen, carboxy c1-4 alkyl, alcoxicarbonilo c1-4 alkyl, c1-4 alkyd Ilcarbonilo C0 - 4 alkyl, aryl or alkyl heterociclil C0 - C1 - 4 - 4 unsaturated.The Radicals are not replaced or substituted by alkoxy C1 1 - 4 - 8 - 8carbonilo C1 alkyl, alkoxy, alquilcarbonilo C0 - C1 - 8, 8, 8 alquilsulfonilo C1 -, aryl alkoxy C0 - 4 - aryl carbonyl, halogen, heterociclilo, cyano, trifluoromethyl, Oxo, trifluoromethoxy, or tri alkyl c1-4 silyl; n is u N Number 0, 1 or 2; and its SaltProdrug or compound in which one or more Atoms are replaced by their non Radioactive Stable Isotopes, in particular Salt useful from the point of view of Pharmaceuticals, where R2 is H, R1 is not naphthyl or carbazolyl.
机译:含有它们的药物组合物及其在制备具有醛固酮合酶抑制活性的药物中的用途,该药物用于治疗和预防库欣氏综合症,低血钾,高血压,原发性和继发性类风湿性关节炎及相关疾病。索赔1:一种通式(1)的化合物,其中X是n; C; Z是一个链接); R是H或烷基); b为C 1 -C 8-8-,烷氧基,卤素或三氟甲基; r1是烷基alquenilo C1-C2-8、8,alquinilo C2-8-烷基,芳基或杂环基C0 C0-4-4不饱和,其基团不是脲基或被烷氧基C11-4-8烷氧基烷基取代8carbonilo C1,C1-8Alquilcarbonilo C0-C1-8 8 alquilsulfonilo,芳基烷氧基C0-4-芳基羰基,卤素,杂环基,氰基,三氟甲基,氧代,三氟甲氧基或三甲硅烷基c1-4烷基; R2是H);或(b)是8个C1-C3烷基,环烷基-8,卤素,羧基c1-4烷基,alcoxicarbonilo c1-4烷基,c1-4醇酸Ilcarbonilo C0-4烷基,芳基或烷基杂取代基C0-C1-4-4自由基不被烷氧基C1 1-4-8-8碳基C1烷基,烷氧基,alquilcarbonilo C0-C1-8、8、8烷磺酰基C1-,芳基烷氧基C0-4芳基羰基,卤素,杂环基取代或取代,氰基,三氟甲基,氧代,三氟甲氧基或三烷基c1-4甲硅烷基; n是u N数字0、1或2;以及其盐前药或其中一个或多个原子被其非放射性稳定同位素取代的化合物,特别是从药学角度出发有用的盐,其中R2是H,R1不是萘基或咔唑基。

著录项

  • 公开/公告号AR049126A1

    专利类型

  • 公开/公告日2006-06-28

    原文格式PDF

  • 申请/专利权人 SPEEDEL EXPERIMENTA AG;

    申请/专利号AR2005P102199

  • 发明设计人

    申请日2005-05-27

  • 分类号C07D471/04;A61K31/437;A61K31/4188;A61P9/00;C07D471/04;C07D221/00;C07D235/00;

  • 国家 AR

  • 入库时间 2022-08-21 21:40:26

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