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    • 6. 发明申请
    • Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
    • 取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂
    • US20060040936A1
    • 2006-02-23
    • US11168797
    • 2005-06-28
    • Hubert JosienJohn CladerThomas BaraRuo XuHongmei LiDmitri PissarnitskiZhiqiang Zhao
    • Hubert JosienJohn CladerThomas BaraRuo XuHongmei LiDmitri PissarnitskiZhiqiang Zhao
    • A61K31/5377A61K31/498A61K31/496A61K31/46C07D43/02C07D413/02C07D487/04
    • C07D265/30C07D413/12C07D451/02C07D487/08
    • This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    • 本发明公开了下式的新型γ分泌酶抑制剂:其中:L是-O-,-N(R 6) - , - S - , - S(O) - 或-S(O - ; R 1选自芳基和杂芳基; R 2选自烷基,-C(O)-Y,-XC(O)-Y, - 亚烷基-XC(O)-Y, - 亚烷基-C(O )-Y-亚烷基 - 亚环烷基-OC(O)-Y-亚烷基 - 亚环烷基-C(O)-Y-亚烷基 - 亚烷基-OC(O)-Y-亚烷基 - 亚烷基-C(O) Y( - )亚环烷基-C(O)-Y-亚烷基-C(O)-Y-亚烷基 - 亚环烷基亚烷基-XC(O)-Y-亚烷基 - 亚环烷基 - 亚烷基-C(O)-Y, 芳基和杂芳基; R 3选自芳基,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,芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9,-N(R 6) - (CH 2) 芳基,杂芳基,烷基,环烷基,芳基烷基,芳基环烷基,杂芳基烷基,杂芳基环烷基和芳基杂环烷基 ; 或Y选自:一种或多种式I化合物或包含该化合物的制剂可用于,例如, 治疗阿尔茨海默病。