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    • 2. 发明申请
    • Novel gamma secretase inhibitors
    • 新型γ分泌酶抑制剂
    • US20060004004A1
    • 2006-01-05
    • US11098745
    • 2005-04-04
    • Theodros AsberomJohn CladerHubert JosienMark McBriarDmitri PissarnitskiZhiqiang Zhao
    • Theodros AsberomJohn CladerHubert JosienMark McBriarDmitri PissarnitskiZhiqiang Zhao
    • A61K31/5377A61K31/496A61K31/4545C07D413/14C07D41/14
    • C07D451/04C07D211/96C07D401/06C07D401/12C07D413/06C07D413/14C07D451/06C07D471/04C07D471/10C07D487/04C07D487/08
    • Gamma-secretase inhibitors of the formula: are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes —C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-C(O)—Y, —S(O)—Y, -alkylene-S(O)—Y, -alkylene-cycloalkylene-S(O)—Y, -cycloalkylene-alkylene-S(O)—Y, -alkylene-cycloalkylene-alkylene-S(O)—Y, -cycloalkylene-S(O)—Y, —S(O2)—Y, -alkylene-S(O2)—Y, -alkylene-cycloalkylene-S(O2)—Y, -cycloalkylene-alkylene-S(O2)—Y, -alkylene-cycloalkylene-alkylene-S(O2)—Y, and -cycloalkylene-S(O2)—Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, —O-alkyl, —OH, —N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, —C(O)—; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.
    • 下式的γ-分泌酶抑制剂:可用于治疗各种神经变性疾病,其中例如:R 1包括未取代或取代的芳基或杂芳基; R 2包括-C(O)-Y, - 亚烷基-C(O)-Y-亚烷基 - 亚环烷基-C(O)-Y-亚烷基 - 亚烷基-C(O) - Y, - 亚烷基 - 亚环烷基 - 亚烷基-C(O)-Y-环亚烷基-C(O)-Y,-S(O)-Y-亚烷基-S(O)-Y-亚烷基 - 亚环烷基-S (O)-Y-亚烷基 - 亚烷基-S(O)-Y-亚烷基 - 亚环烷基 - 亚烷基-S(O)-Y-亚烷基-S(O)-Y,-S(O) - 亚烷基-S(O)2 - 亚烷基 - 亚环烷基-S(O)2 - 亚烷基-S(O 2) -S(O)2 - 亚烷基 - 亚环烷基 - 亚烷基-S(O)2 - 和 - 亚环烷基-S(O 2) / Y,其中Y如本文所定义,并且所述亚烷基或亚环烷基中的每一个可以是未经取代的或如本文所提供的取代的; 每个R 3独立地包括H,烷基,-O-烷基,-OH,-N(R 9)2,酰基和 芳酰基 或其部分(R 3)2和连接在式I中的环碳原子一起定义为羰基,-C(O) - ; 每个R 3A和R 3B独立地包括H或烷基; R 11包括芳基,杂芳基,烷基,环烷基,芳基烷基,芳基环烷基,杂芳基烷基,杂芳基环烷基,芳基杂环烷基或烷氧基烷基。 一种或多种式I化合物或其药学上可接受的盐,溶剂化物和/或酯或其组合物可用于治疗,例如阿尔茨海默氏病。