首页> 外国专利> Use of naphthalene derivatives for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolismus, diabetes mellitus, depression, metabolic syndromes and age-related cognitive decline

Use of naphthalene derivatives for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolismus, diabetes mellitus, depression, metabolic syndromes and age-related cognitive decline

机译:萘衍生物用于治疗醛固酮增多症,心力衰竭,心肌纤维化,皮质醇过多症,糖尿病,抑郁症,代谢综合征和与年龄有关的认知能力下降的用途

摘要

Use of naphthalene derivatives (I) or their salts for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolismus, diabetes mellitus, depression, metabolic syndromes and age-related cognitive decline. Use of naphthalene derivatives of formula (I) or their salts for the treatment of hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolismus, diabetes mellitus depression, metabolic syndromes and age-related cognitive decline. Y 1(=C(R 9) 2), (=N(R 10)), (=O) or (=S); T 1, U 1, V 1, W 1, X 1C or N; R 1, R 2H, halo, CN, OH, nitro, alkyl, alkoxy, alkyl carbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylaminosulfonyl, thioalkyl, alkylsulfinyl or alkyl sulfonyl; R 3nitrogenous mono- or bicyclic heteroaryl residue (where partially or completely saturated equivalents and substituted) and N atom which is not substituted; R 4-R 9H, halo, CN, OH, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyl, lower alkylcarbonyloxy, lower alkylaminocarbonyl, lower alkyaminosulfonyl, lower thioalkyl, lower alkylsulfinyl, lower alkylsulfonyl, arylalkyloxy, heteroarylalkyloxy; and n : 0-2. With provisos. Full definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Cardiant; Antiinflammatory; Antidiabetic; Antidepressant; Analgesic; Antianginal; Nootropic. MECHANISM OF ACTION : Mammalian-cytochrome-P450 (CYP)-oxygenase inhibitor; Human or mammalian-aldosterone synthase inhibitor; Steroid-11beta -hydroxylase inhibitor. The CYP11B2 inhibitory activity of (I) was tested in cell line using biological assays. The results showed that (I) exhibited a median inhibitory concentration value of 92%.
机译:萘衍生物(I)或它们的盐在治疗醛固酮过多症,心力衰竭,心肌纤维化,皮质醇过多,糖尿病,抑郁症,代谢综合征和与年龄有关的认知能力下降的方面的用途。式(I)的萘衍生物或其盐在治疗醛固酮增多症,心力衰竭,心肌纤维化,皮质醇过多,糖尿病抑郁症,代谢综合征和与年龄有关的认知能力下降中的用途。 Y 1>(= C(R 9>)2),(= N(R 10>)),(= O)或(= S); T 1>,U 1>,V 1>,W 1>,X 1> C或N; R 1>,R 2> H,卤素,CN,OH,硝基,烷基,烷氧基,烷基羰基,烷基羰氧基,烷基氨基羰基,烷基氨基磺酰基,硫代烷基,烷基亚磺酰基或烷基磺酰基; R 3>氮的单或双环杂芳基残基(部分或完全饱和的等同物并被取代)和未被取代的N原子; R 4> -R 9> H,卤素,CN,OH,硝基,低级烷基,低级烷氧基,低级烷基羰基,低级烷基羰基氧基,低级烷基氨基羰基,低级烷基氨基磺酰基,低级硫代烷基,低级烷基亚磺酰基,低级烷基磺酰基,芳基烷氧基,杂芳基烷氧基; n:0-2。附带条件。完整定义在“定义(完整定义)”字段中给出。活动:Cardiant;消炎(药;抗糖尿病抗抑郁药止痛药抗心绞痛促智。作用机理:哺乳动物细胞色素P450(CYP)加氧酶抑制剂;人或哺乳动物的醛固酮合酶抑制剂;类固醇11β-羟化酶抑制剂。使用生物测定法在细胞系中测试(I)的CYP11B2抑制活性。结果表明(I)显示出92%的中值抑制浓度值。

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