首页> 外国专利> In vitro screening/selecting chemical compounds derived from delphinidin activating estrogen receptor (ER) alpha, comprises obtaining fused heterocylic compound, testing whether the compound activates ER alpha and selecting compound

In vitro screening/selecting chemical compounds derived from delphinidin activating estrogen receptor (ER) alpha, comprises obtaining fused heterocylic compound, testing whether the compound activates ER alpha and selecting compound

机译:体外筛选/选择衍生自翠雀素激活雌激素受体(ER)α的化合物,包括获得融合的杂环化合物,测试该化合物是否激活ER alpha并选择化合物

摘要

In vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . In vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound of formula (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . R 1-R 11 : H, halo (preferably F, Br or I), OH, amino, nitroso, nitro, CN, azonium, (1-6C)alkyl, (2-6C)alkenyl, (2-6C) alkynyl, (1-6C) haloalkyl, (1-6C) alkoxy, (1-6C) thioalkoxy, (1-6C) haloalkoxy, di ((1-6C) alkyl) amino or alkylcarbonyl; and X : a heteroatom comprising O, N or S (optionally charged and optionally substituted with a group of (1-6C) alkyl, (2-6C) alkenyl, (2-6C) alkynyl, (1-6C) haloalkyl, (1-6C) alkoxy, (1-6C) thioalkoxy, (1-6C) haloalkoxy, di ((1-6C) alkyl) amino, or alkylcarbonyl). An independent claim is included for in vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . An independent claim is included for in vitro method for screening and selecting chemical compounds derived from delphinidin inducing the production of nitric oxide (NO) in endothelial cells, comprising: obtaining at least one compound (I); testing whether the compound induces the production of nitric oxide in endothelial cells with which it is contacted and selecting the compound if it induces the production of nitric oxide in endothelial cells with which it is contacted. [Image] ACTIVITY : Vasotropic; Cardiovascular-Gen.; Cytostatic; Cardiant; Antiarteriosclerotic; Hypotensive. MECHANISM OF ACTION : Estrogen receptor alpha activator; Nitric oxide production inducer.
机译:一种用于筛选和选择衍生自翠雀素的激活雌激素受体(ER)α的化合物的体外方法,包括:获得至少一种稠合的杂环化合物(I);测试化合物是否激活ERalpha;并选择激活雌激素受体ERalpha的化合物。筛选和选择衍生自翠雀素的激活雌激素受体(ER)α的化合物的体外方法,包括:获得至少一种式(I)的稠合杂环化合物;和测试化合物是否激活ERalpha;并选择激活雌激素受体ERalpha的化合物。 R 1 -R 11:H,卤素(优选F,Br或I),OH,氨基,亚硝基,硝基,CN,偶氮鎓,(1-6C)烷基,(2-6C)烯基,(2-6C)炔基,(1-6C)卤代烷基,(1-6C)烷氧基,(1-6C)硫代烷氧基,(1-6C)卤代烷氧基,二((1-6C)烷基)氨基或烷基羰基; X:杂原子,包含O,N或S(任选地被(1-6C)烷基,(2-6C)烯基,(2-6C)炔基,(1-6C)卤代烷基, 1-6C)烷氧基,(1-6C)硫代烷氧基,(1-6C)卤代烷氧基,二((1-6C)烷基)氨基或烷基羰基)。包括独立的权利要求的体外方法,用于筛选和选择衍生自激活了雌激素受体(ER)α的飞燕草碱的化合物,包括:获得至少一种稠合的杂环化合物(I);测试化合物是否激活ERalpha;并选择激活雌激素受体ERalpha的化合物。包括独立的权利要求,所述方法用于筛选和选择衍生自飞燕草碱的化合物,所述化合物诱导内皮细胞中一氧化氮(NO)的产生,包括:获得至少一种化合物(I);和测试该化合物是否在与其接触的内皮细胞中诱导一氧化氮的产生,并选择该化合物是否在与其接触的内皮细胞中诱导一氧化氮的产生。活动:垂直运动;心血管创细胞抑制卡迪恩抗动脉硬化;低血压。作用机理:雌激素受体α激活剂。一氧化氮产生诱导剂。

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