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    • 2. 发明申请
    • NOVEL GAMMA SECRETASE INHIBITORS
    • 新的GAMMA秘密抑制剂
    • WO2005097768A2
    • 2005-10-20
    • PCT/US2005/011456
    • 2005-04-04
    • SCHERING CORPORATIONASBEROM, TheodrosCLADER, John, W.JOSIEN, Hubert, B.PISSARNITSKI, Dmitri, A.ZHAO, ZhiqiangMCBRIAR, Mark, D.
    • ASBEROM, TheodrosCLADER, John, W.JOSIEN, Hubert, B.PISSARNITSKI, Dmitri, A.ZHAO, ZhiqiangMCBRIAR, Mark, D.
    • C07D295/00
    • C07D451/04C07D211/96C07D401/06C07D401/12C07D413/06C07D413/14C07D451/06C07D471/04C07D471/10C07D487/04C07D487/08
    • Gamma-secretase inhibitors of the formula: Chemical formula should be inserted here as it appears on the abstract in paper form. 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.
    • Gamma-secretase抑制剂的配方:化学式应该插在这里,它以纸质形式出现在抽象上。 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,亚环烷基亚烷基-C(O)-Y,亚烷基亚环烷基 - 亚烷基-C(O) -Y,亚环烷基-C(O)-Y,-S(O)-Y,亚烷基-S(O)-Y,亚烷基 - 亚环烷基-S(O)-Y,亚环烷基 - 亚烷基-S(O) 亚烷基亚环烷基亚烷基-S(O)-Y,亚环烷基-S(O)-Y,-S(O 2)-Y,亚烷基-S(O 2)-Y,亚烷基亚环烷基S(O 2) S(O 2)-Y,亚烷基亚烷基亚烷基 - 亚烷基-S(O 2)-Y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取代的或如所提供的取代 本文; 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(R3)2部分与式I中所示的环碳原子一起定义为羰基-C(O) - ; 每个R3A和R3B独立地包括H或烷基; R11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。