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    Oxime-Containing Acyl Guanidines as Beta-Secretase Inhibitors
    4.
    发明申请
    Oxime-Containing Acyl Guanidines as Beta-Secretase Inhibitors 有权
    含肟的酰基胍作为β-分泌酶抑制剂

    公开(公告)号：US20070232581A1

    公开(公告)日：2007-10-04

    申请号：US11693026

    申请日：2007-03-29

    申请人： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

    发明人： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

    IPC分类号： A61K31/55 ,  A61K31/445 ,  A61K31/40 ,  A61K31/397 ,  A61K31/396 ,  A61K31/165 ,  C07D211/26 ,  C07D207/30 ,  C07D223/04 ,  C07D203/04

    CPC分类号： C07D209/20 ,  C07C257/20 ,  C07C279/22

    摘要： There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

    摘要翻译： 提供了一系列式（I）的取代的含肟基的酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中R 1，R 2，R 3，R 4，R R 5，R 6和R 7如本文所定义，其药物组合物和使用方法。 这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

    Optically active aziridine-2-carboxylate derivatives and a process for preparing them
    6.
    发明授权
    Optically active aziridine-2-carboxylate derivatives and a process for preparing them 失效
    光学活性氮丙啶-2-羧酸酯衍生物及其制备方法

    公开(公告)号：US07268228B2

    公开(公告)日：2007-09-11

    申请号：US10344225

    申请日：2001-08-10

    申请人： Won Koo Lee ,  Chan Sun Park ,  Yeon Hwa Lim ,  Hyun J on Ha

    发明人： Won Koo Lee ,  Chan Sun Park ,  Yeon Hwa Lim ,  Hyun J on Ha

    IPC分类号： C07D251/16 ,  C07D203/16 ,  C07D203/04

    CPC分类号： C07D203/08

    摘要： This invention relates to compounds of Formula I having an aziridine-2-carboxylic group and a menthol group, a process for preparing such compounds, a method for obtaining optically active aziridine-2-carboxylate derivatives by optical resolution of such compounds, and optically active aziridine-2-carboxylate derivatives obtained by the same method: wherein R1 is hydrogen; alkyl; cycloalkyl; 4-chlorophenyl; 4-methoxyphenyl; s-triazinyl or pyridinyl acyl; benzyl; hydrocarbon residue which may be substituted with a substituent selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl and 4-methoxyphenyl; 2,4-dimethoxyphenyl; substituted phenyl including (1R)-phenylethyl or (1S)-phenylethyl. Preferences are given to (1R)-phenylethyl and (1S)-phenylethyl. Menthol is selected from the group consisting of (+)-menthol and (−)-menthol.

    摘要翻译： 本发明涉及具有氮丙啶-2-羧酸基和薄荷醇基团的式I化合物，制备这些化合物的方法，通过这种化合物的光学拆分获得光学活性氮丙啶-2-羧酸酯衍生物的方法和光学活性 通过相同方法得到的氮丙啶-2-羧酸酯衍生物：其中R 1是氢; 烷基; 环烷基 4-氯苯基; 4-甲氧基苯基; s-三嗪基或吡啶基酰基; 苄基; 可以被选自羟基，烷氧基，二烷基氨基，苯基，4-氯苯基和4-甲氧基苯基的取代基取代的烃残基; 2,4-二甲氧基苯基; 包括（1R） - 苯基乙基或（1S） - 苯基乙基的取代的苯基。 给予（1R） - 苯基乙基和（1S） - 苯基乙基。 薄荷醇选自（+） - 薄荷醇和（ - ） - 薄荷醇组成的组。

    Cross-linked hyaluronate compounds
    9.
    发明申请
    Cross-linked hyaluronate compounds 审中-公开
    交联透明质酸盐化合物

    公开(公告)号：US20050222081A1

    公开(公告)日：2005-10-06

    申请号：US10511373

    申请日：2003-04-17

    申请人： Diego Gianolio ,  Pericles Calias ,  Robert Miller

    发明人： Diego Gianolio ,  Pericles Calias ,  Robert Miller

    IPC分类号： A61K31/728 ,  C07D203/04 ,  C08B37/00 ,  C08B37/08

    CPC分类号： C07D203/04 ,  C08B37/0072

    摘要： There is disclosed a cross-linked hyaluronate compound obtained by reacting a sodium hyaluronate compound with a polfunctional aziridine compound as a cross-linking agent. The polyfunctional aziridine compound was added to hyaluronan of various molecular weights in an equivalent ratio of HA/AZ of 1:1 to 1:10, preferably, 1:3 to 1:10, more preferably, 1:3 to 1:5; most preferably 1:4 to 1:5. The polymeric hydrogel compounds obtained are useful to prevent the formation of post-operative adhesions, designing tissue engineering applications, and the like.

    摘要翻译： 公开了通过使透明质酸钠化合物与作为交联剂的官能氮丙啶化合物反应得到的交联的透明质酸盐化合物。 将多官能氮丙啶化合物以等于1：1至1:10，优选1:3至1:10，更优选1:3至1:5的HA / AZ比例加入各种分子量的透明质酸中; 最优选1:4至1:5。 获得的聚合物水凝胶化合物可用于防止术后粘连的形成，设计组织工程应用等。