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    • 11. 发明申请
    • 1-ADAMANTYLAZETIDIN-2-ONE DERIVATIVES AND DRUGS CONTAINING SAME
    • 1-ADAMANTYLAZETIDIN-2-ONE衍生物和含有其的药物
    • US20100075943A1
    • 2010-03-25
    • US12550206
    • 2009-08-28
    • Hisashi NakashimaTakahiro MoriTakaaki ArakiTakahisa OgaminoKazutoyo AbeTadaaki OhgiyaRyoko Mori
    • Hisashi NakashimaTakahiro MoriTakaaki ArakiTakahisa OgaminoKazutoyo AbeTadaaki OhgiyaRyoko Mori
    • A61K31/397C07D205/04A61P3/00
    • C07D205/08A61K31/397C07D401/04C07D401/08C07D405/04
    • It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate. [wherein A ring represents C6-10 aryl group, 5- to 14-membered heteroaryl group, R1 is a hydrogen atom, halogen atom, C1-6 alkoxycarbonyl group, hydroxyl group, carboxyl group or carbamoyl group; R2 and R3 are the same or different and are a C1-6 alkyl group; R4, R5, and R6 are same or different, and are a hydrogen atom, halogen atom, C1-6 alkyl group, C1-6 alkoxy group, C6-10 aryl group, or R4 and R5, or R5 and R6 may together form a C1-3 alkylenedioxy group, R7 and R8 are the same of different and represent a hydrogen atom or C1-6 alkyl group, or may together form a C3-6 cyclic hydrocarbon group, n represents an integer of 0 or 1]
    • 提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1,特别是糖尿病,胰岛素抵抗,糖尿病并发症,肥胖,血脂异常,高血压,脂肪肝或代谢综合征的疾病的新化合物。 它是由以下通式(1)表示的1-金刚烷基氮杂环丁-2-酮衍生物或其盐或其溶剂合物。 [其中A环表示C6-10芳基,5〜14元杂芳基,R1表示氢原子,卤素原子,C1-6烷氧基羰基,羟基,羧基或氨基甲酰基。 R2和R3相同或不同,为C1-6烷基; R 4,R 5和R 6相同或不同,为氢原子,卤素原子,C 1-6烷基,C 1-6烷氧基,C 6-10芳基或R 4和R 5,或者R 5和R 6可以一起形成 C 1-3亚烷基二氧基,R 7和R 8相同,表示氢原子或C 1-6烷基,或一起形成C 3-6环烃基,n表示0或1的整数]