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    NOVEL GAMMA SECRETASE INHIBITORS
    3.
    发明申请
    NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
    新的GAMMA SECRETASE抑制剂

    公开(公告)号：WO2005097768A3

    公开(公告)日：2005-12-15

    申请号：PCT/US2005011456

    申请日：2005-04-04

    Applicant: SCHERING CORP ,  ASBEROM THEODROS ,  CLADER JOHN W ,  JOSIEN HUBERT B ,  PISSARNITSKI DMITRI A ,  ZHAO ZHIQIANG ,  MCBRIAR MARK D

    Inventor： ASBEROM THEODROS ,  CLADER JOHN W ,  JOSIEN HUBERT B ,  PISSARNITSKI DMITRI A ,  ZHAO ZHIQIANG ,  MCBRIAR MARK D

    IPC: A61K31/44 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  A61P25/28

    CPC classification number: C07D451/04 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

    Abstract: 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.

    Abstract translation: 化学式的γ-分泌酶抑制剂应插入此处，因为它以摘要形式出现在纸上。 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; R2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，亚烷基-S（O）-Y，亚烷基 - 亚环烷基-S（O）-Y，亚环烷基 - 亚烷基-S（O）-Y （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）-Y，亚环烷基亚烷基 S（O 2）-Y，亚烷基亚环烷基 - 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未被取代或如所提供的被取代 本文; 每个R3独立地包括H，烷基，O烷基，OH，N（R9）2，酰基和芳酰基; 或部分（R 3）2与式I所示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; 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/或酯或包含其的组合物可用于治疗例如阿尔茨海默氏病。

    NOVEL GAMMA SECRETASE INHIBITORS
    9.
    发明申请
    NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
    新的GAMMA秘密抑制剂

    公开(公告)号：WO2005097768A2

    公开(公告)日：2005-10-20

    申请号：PCT/US2005/011456

    申请日：2005-04-04

    Applicant: SCHERING CORPORATION ,  ASBEROM, Theodros ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  PISSARNITSKI, Dmitri, A. ,  ZHAO, Zhiqiang ,  MCBRIAR, Mark, D.

    Inventor： ASBEROM, Theodros ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  PISSARNITSKI, Dmitri, A. ,  ZHAO, Zhiqiang ,  MCBRIAR, Mark, D.

    IPC: C07D295/00

    CPC classification number: C07D451/04 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

    Abstract: 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.

    Abstract translation: 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。

    4,5-CYCLOALKANO-3-BENZAZEPIN-7-OL-DERIVATIVES AND THEIR USE
    10.
    发明申请
    4,5-CYCLOALKANO-3-BENZAZEPIN-7-OL-DERIVATIVES AND THEIR USE 审中-公开
    4,5-环辛基-3-苯并恶嗪-7-醇衍生物及其用途

    公开(公告)号：WO1991011437A1

    公开(公告)日：1991-08-08

    申请号：PCT/US1991000503

    申请日：1991-01-31

    Applicant: SCHERING CORPORATION ,  ASBEROM, Theodros ,  O'CONNOR, Edward ,  BERGER, Joel, Gilbert ,  CLADER, John, Welch

    Inventor： SCHERING CORPORATION

    IPC: C07D223/18

    CPC classification number: C07D223/18 ,  C07D223/32

    Abstract: Novel benzazepines of formula (I), or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl ou (II); A represents -[CR R ]n-; n represents 3 or 4; R and R may be the same or different and each independently represents H, OH, alkyl, alkoxy, phenyl or substituted phenyl, with the proviso that R and R on the same carbon atom are not both OH, or R and R on the same carbon atom together represent =O; G represents H, R (CO)- or ArNHCO-; R represents H, alkyl, alkoxy, phenyl or substituted phenyl; Ar represents phenyl or substituted phenyl; and Y and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or haloalkyl; the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.

    Abstract translation: 式（I）的新的苯并氮杂或其药学上可接受的盐，其中R表示H，烷基，烯丙基ou（II）; A表示 - [CR 1 R 2] n - n表示3或4; R 1和R 2可以相同或不同，并且各自独立地表示H，OH，烷基，烷氧基，苯基或取代的苯基，条件是相同碳原子上的R 1和R 2 不同于OH，或同一碳原子上的R 1和R 2一起代表= O; G表示H，R 3（CO） - 或ArNHCO-; R 3表示H，烷基，烷氧基，苯基或取代的苯基; Ar表示苯基或取代的苯基; 并且Y和Z可以相同或不同，并且各自独立地选自H，卤素，烷基，烷氧基或卤代烷基; 其药学上可接受的盐及其药物组合物; 有用于治疗精神病药物依赖，D1依赖性神经障碍或疼痛。

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