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    REFOLDED RECOMBINANT ALPHA SECRETASE CRYSTALS AND METHODS FOR PREPARING AND USING THE SAME
    22.
    发明申请
    REFOLDED RECOMBINANT ALPHA SECRETASE CRYSTALS AND METHODS FOR PREPARING AND USING THE SAME 有权
    重建的重组ALPHA分泌物晶体及其制备和使用方法

    公开(公告)号：US20100203616A1

    公开(公告)日：2010-08-12

    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: C12N9/50

    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
    23.
    发明申请
    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors 失效
    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：US20100093695A1

    公开(公告)日：2010-04-15

    申请号：US12633311

    申请日：2009-12-08

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

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

    IPC: A61K31/438 ,  C07D413/14 ,  A61K31/5377 ,  C07D413/12 ,  C07D487/04 ,  A61K31/55 ,  A61K31/551

    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 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.

    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-NR 8 R 9，-N（R 6） - （CH 2）b -NR 8 R 9，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。

    Inhalation device
    25.
    发明授权
    Inhalation device 失效
    吸入装置

    公开(公告)号：US4291688A

    公开(公告)日：1981-09-29

    申请号：US104610

    申请日：1979-12-17

    Applicant: Frederic E. Kistler

    Inventor： Frederic E. Kistler

    IPC: A61M15/00

    CPC classification number: A61M15/0086 ,  A61M15/009 ,  A61M2205/43 ,  A61M2205/581

    Abstract: An inhalation device of the type adapted to receive and locate an aerosol container designed to administer a multiplicity of metered doses, said aerosol container having a composition under pressure therein and having metering valve means including a valve stem and associated metering means, the valve stem having an axial discharge tube extending therethrough for discharge of a metered dose upon actuation of said metering valve means by depression of said valve stem, said inhalation device comprising a body having a skirt adapted to receive and locate said aerosol container in a first end thereof and a head-piece connected to a second end of said skirt, a mouth-piece extending from said head-piece and in communication therewith, and an audible signal generating means, said head-piece having actuating means for said metering valve means and a discharge passageway leading to a discharge orifice directed towards said mouth-piece, said actuating means being engageable with the valve stem upon location of the container within the skirt and operable to actuate the metering valve means whereby a metered dose is discharged through the valve stem discharge tube and the discharge passageway and discharge orifice into the mouth-piece, wherein said audible signal generating means is located in said air-passageway within the body upstream of said discharge orifice and surrounds the actuating means for the metering valve means, and is actuatable upon inhalation through said mouth-piece when said inhalation device is in engagement with said container.

    Abstract translation: 一种适于接收和定位被设计成施用多个计量剂量的气溶胶容器的吸入装置，所述气溶胶容器具有在其内的压力下的组成，并具有包括阀杆和相关联的计量装置的计量阀装置，所述阀杆具有 延伸穿过其中的轴向排出管，用于通过按压所述阀杆来致动所述计量阀装置来排出计量剂量，所述吸入装置包括具有适于在其第一端接收和定位所述气溶胶容器的裙部的主体， 与所述裙部的第二端连接的头部件，从所述头部件延伸并与之连通的口部件和可听见的信号发生装置，所述头部件具有用于所述计量阀装置的致动装置和排出通道 导致朝向所述口件的排放孔，所述致动装置可与阀杆u接合 所述容器在所述裙部内的位置可操作以致动所述计量阀装置，由此计量剂量通过所述阀杆排出管和所述排出通道和排出孔排出到所述口件中，其中所述可听信号发生装置位于 所述空气通道位于所述排放孔的上游，并且围绕所述计量阀装置的致动装置，并且当所述吸入装置与所述容器接合时可以通过所述口件吸入而被致动。

    1-polyfluoroalkyl benzodiazepines
    26.
    发明授权
    1-polyfluoroalkyl benzodiazepines 失效
    1-多氟烷基苯甲酸酯

    公开(公告)号：US3723414A

    公开(公告)日：1973-03-27

    申请号：US3723414D

    申请日：1970-02-13

    Applicant: SCHERING CORP

    Inventor： STEINMAN M

    IPC: A61K31/55 ,  C07D243/16 ,  C07D53/06

    CPC classification number: C07D243/16 ,  A61K31/55

    Abstract: Disclosed herein are 1-(polyfluoroalkyl)-2,3-dihydro-5-aryl-1H1,4-benzodiazepines and compounds useful as intermediates for preparing these benzodiazepines. These benzodiazepines are particularly useful as anti-anxiety agents.

    Abstract translation: 本文公开了1-（多氟烷基）-2,3-二氢-5-芳基-1H-1,4-苯并二氮杂和用作制备这些苯并二氮杂的中间体的化合物。 这些苯二氮卓类特别可用作抗焦虑剂。

    Laminated tablets
    27.
    发明授权
    Laminated tablets 失效
    层压片

    公开(公告)号：US3696188A

    公开(公告)日：1972-10-03

    申请号：US3696188D

    申请日：1971-06-16

    Applicant: SCHERING CORP

    Inventor： FERNANDEZ RAUL O ,  CANNITO VINCENT F ,  OLSEN OSCAR

    IPC: A61J3/00 ,  A61J3/06

    CPC classification number: A61J3/005

    Abstract: Laminated, pan-coated tablets are described wherein the various medicament layers are separated by a layer containing 10-50 percent of a silica gel having a specified pore size. This silica gel layer not only substantially reduces the processing time but also aids in preventing migration of the ingredients and in accelerating dissolution.

    Abstract translation: 描述了层压的包覆片剂，其中各种药物层被含有10-50％具有特定孔径的硅胶的层分离。 该硅胶层不仅大大减少了处理时间，而且有助于防止成分的迁移和加速溶解。

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