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    Esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    6.
    发明授权
    Esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
    取代的8-羟基-1-苯基-2,3,4,5-四氢-1H-3-苯并吖庚因的酯

    公开(公告)号：US4477378A

    公开(公告)日：1984-10-16

    申请号：US416513

    申请日：1982-09-09

    Applicant: Elijah H. Gold ,  Wei K. Chang

    Inventor： Elijah H. Gold ,  Wei K. Chang

    IPC: C07D223/16 ,  A61K31/55

    CPC classification number: C07D223/16 ,  Y10S514/96

    Abstract: Disclosed are esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1-H-3-benzazepines represented by the general formula I ##STR1## wherein X is chloro, bromo or trifluoromethyl; R.sub.1 is alkyl, aralkyl, aryl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, cycloalkylalkyl, alkoxycarbonylalkyl, cycloalkyl, 1-adamantyl, cycloalkoxyalkyl, alkoxy, aralkoxy, cycloalkoxy or aryloxy; and the pharmaceutically acceptable acid addition salts thereof. The compounds show neuroleptic, antidepressive and antiaggressive activity.

    Abstract translation: 公开了由通式I表示的取代的8-羟基-1-苯基-2,3,4,5-四氢-1H-3-苯并吖庚因的酯，其中X是氯，溴或三氟甲基; R1是烷基，芳烷基，芳基，烷氧基烷基，芳氧基烷基，芳烷氧基烷基，环烷基烷基，烷氧基羰基烷基，环烷基，1-金刚烷基，环烷氧基烷基，烷氧基，芳烷氧基，环烷氧基或芳氧基; 及其药学上可接受的酸加成盐。 这些化合物显示出抗精神病药，抗抑郁药和抗过敏活性。

    Refolded recombinant β-secretase crystals and methods for preparing and using the same
    7.
    发明授权
    Refolded recombinant β-secretase crystals and methods for preparing and using the same 有权
    重折叠重组和分泌酶晶体及其制备和使用方法

    公开(公告)号：US08063185B2

    公开(公告)日：2011-11-22

    申请号：US12434897

    申请日：2009-05-04

    Applicant: Brian M. Beyer ,  Bruce A. Malcolm ,  Corey O. Strickland ,  Wenyan Wang ,  Eileen Wilson

    Inventor： Brian M. Beyer ,  Bruce A. Malcolm ,  Corey O. Strickland ,  Wenyan Wang ,  Eileen Wilson

    IPC: C12N1/12

    CPC classification number: C12N9/6421 ,  C07K2299/00

    Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

    Abstract translation: 本申请涉及用于生长未络合和复合形式的分泌型（BACE）多肽的晶体的方法。 本申请还涉及未结合的BACE的晶体形式和由晶体确定的BACE的三维结构。 此外，本申请涉及BACE的结晶形式用于鉴定与BACE结合并优选抑制BACE的酶活性的配体，优选抑制剂（拮抗剂）。 此外，本申请涉及编码BACE多肽的核酸序列和与以前的方法相比制备BACE的方法，导致更有效的结晶。

    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors
    9.
    发明申请
    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors 审中-公开
    取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂

    公开(公告)号：US20100087425A1

    公开(公告)日：2010-04-08

    申请号：US12633286

    申请日：2009-12-08

    Applicant: Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitaki ,  Zhiqiang Zhao

    Inventor： Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitaki ,  Zhiqiang Zhao

    IPC: A61K31/5377 ,  C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/541 ,  A61P25/00 ,  A61P25/28

    CPC classification number: C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    Abstract: 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 aryl heterocycloalkyl; 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.

    Abstract translation: 本发明公开了下式的新型γ-分泌酶抑制剂：其中：L是-O - ， - N（R6） - ， - S - ， - S（O） - 或-S（O 2） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-X-C（O）-Y， - 亚烷基-X-C（O）-Y， - 亚烷基-C（O）-Y， - 亚烷基 - 亚环烷基-X-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚烷基-C（O） （O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-X-C（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-NR8R9，-N（R6） - （CH2）b-NR8R9，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。

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