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    Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
    6.
    发明申请
    Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 失效
    具有负激素和/或拮抗剂活性的类视黄醇化合物的合成和用途

    公开(公告)号：US20020156054A1

    公开(公告)日：2002-10-24

    申请号：US09821673

    申请日：2001-03-28

    发明人： Elliott S. Klein ,  Alan T. Johnson ,  Andrew M. Standeven ,  Richard L. Beard ,  Samuel J. Gillett ,  Tien T. Duong ,  Sunil Nagpal ,  Vidyasagar Vuligonda ,  Min Teng ,  Roshantha A. Chandraratna

    IPC分类号： A61K031/655 ,  A61K031/47 ,  A61K031/382 ,  A61K031/353 ,  A61K031/216 ,  A61K031/165

    CPC分类号： C07D335/06 ,  C07C57/50 ,  C07C63/33 ,  C07C63/49 ,  C07C63/66 ,  C07C63/72 ,  C07C63/74 ,  C07C65/19 ,  C07C65/28 ,  C07C65/38 ,  C07C69/618 ,  C07C69/76 ,  C07C69/90 ,  C07C69/94 ,  C07C233/81 ,  C07C245/10 ,  C07C327/48 ,  C07C2602/10 ,  C07D213/55 ,  C07D277/30 ,  C07D307/54 ,  C07D333/24 ,  C07D409/04 ,  C07D417/04 ,  C07F7/081

    摘要： Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

    摘要翻译： 芳基取代的和芳基和（3-氧代-1-丙烯基）取代的苯并吡喃，苯并噻喃，1,2-二氢喹啉和5,6-二氢萘衍生物具有类视黄醇阴性激素和/或拮抗剂样生物活性。 本发明的RAR拮抗剂可以施用于包括人在内的哺乳动物，以预防或减少RAR激动剂在结合受体位点上的作用。 具体来说，RAR激动剂与类视黄醇药物一起施用或共同施用以预防或改善由类维生素A或维生素A或维生素A前体引起的毒性或副作用。 类视黄醇阴性激素可用于增强其他类维生素A和核受体激动剂的活性。 例如，称为AGN 193109的类视黄醇阴性激素有效地增加了体外反式激活测定中其他类维生素A和类固醇激素的有效性。 另外，反式激活测定可用于鉴定具有负激素活性的化合物。 这些测定是基于负激素下调修饰的具有组成型转录激活子结构域的嵌合维甲酸受体的活性的能力。