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19 条记录 (耗时 0.03 秒)

    Indole acetic acid acyl guanidines as β-secretase inhibitors
    8.
    发明授权
    Indole acetic acid acyl guanidines as β-secretase inhibitors 有权
    吲哚乙酸酰基胍作为β-分泌酶抑制剂

    公开(公告)号：US07601751B2

    公开(公告)日：2009-10-13

    申请号：US11508481

    申请日：2006-08-23

    申请人： Lorin A. Thompson, III ,  Jianliang Shi ,  F. Christopher Zusi ,  Michael F. Dee ,  John E. Macor

    发明人： Lorin A. Thompson, III ,  Jianliang Shi ,  F. Christopher Zusi ,  Michael F. Dee ,  John E. Macor

    IPC分类号： A61K31/404 ,  A61K31/5377 ,  C07D209/04 ,  C07D413/12 ,  C07D241/04

    CPC分类号： C07D209/18

    摘要： There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 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： 提供一系列式（I）的取代酰基胍或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8，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。

    Compound and method for treating skin for acne or psoriasis
    9.
    发明授权
    Compound and method for treating skin for acne or psoriasis 失效
    用于治疗皮肤或皮肤病的化合物和方法

    公开(公告)号：US5086060A

    公开(公告)日：1992-02-04

    申请号：US552726

    申请日：1990-07-16

    申请人： Neil F. Haley ,  Xina Nair ,  Gerard J. Gendimenico ,  F. Christopher Zusi ,  R. Thomas Swann

    发明人： Neil F. Haley ,  Xina Nair ,  Gerard J. Gendimenico ,  F. Christopher Zusi ,  R. Thomas Swann

    IPC分类号： A61K8/00 ,  A61K8/30 ,  A61K8/49 ,  A61K31/23 ,  A61Q19/00 ,  C07C20060101 ,  C07C69/608 ,  C07C69/96 ,  C07C219/34 ,  C07C233/25 ,  C07C235/46 ,  C07C235/60 ,  C07C255/55 ,  C07C271/28 ,  C07C271/44 ,  C07C403/20 ,  C07C403/22 ,  C07D277/66 ,  C07D417/04 ,  C07D455/03 ,  C07D455/04 ,  C07F15/02

    CPC分类号： C07C403/20 ,  C07C219/34 ,  C07C233/25 ,  C07C235/46 ,  C07C235/60 ,  C07C255/55 ,  C07C271/28 ,  C07C271/44 ,  C07D277/66 ,  C07D455/04 ,  C07F15/02 ,  C07C2101/16 ,  Y10S514/859 ,  Y10S514/863

    摘要： The effects of acne and psoriasis are relived by applying either topically or by oral adminstration, a compound having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of H, Cl, straight or branched alkyl of 1 to 10 carbon atoms, NO.sub.2, COOR.sub.6, CN, OR.sub.6, NR.sub.6 R.sub.7, NR.sub.6 C(.dbd.S)NR.sub.7 R.sub.8, NF.sub.6 COR.sub.7, SO.sub.2 NR.sub.6 R.sub.7, CH(CH.sub.3)COOH, CONR.sub.6 R.sub.7, COR.sub.6, OCONR.sub.6 R.sub.7, NR.sub.6 COONR.sub.7, R.sub.9 OR.sub.6, NR.sub.6 SO.sub.2 R.sub.7, Si(CH.sub.3).sub.3, and NR.sub.6 CONR.sub.7 R.sub.8,R.sub.3 together with R.sub.4 forms a benzo ring or taken together with R.sub.2 forms a benzo or tetrahydrobenzo ring or together with R.sub.2 and R.sub.1 forms a: ##STR2## moiety or together with R.sub.2 forms a ##STR3## moiety or R.sub.2 together with R.sub.1 forms a benzo ring or R.sub.2 together with R.sub.3 forms a ##STR4## moiety, or R.sub.1 is independently selected from the group consisting of ##STR5## moiety, R.sub.6, R.sub.7 and R.sub.8 are indenpendently selected from the group consisting of straight or branched alkyl containing from 1 to 10 carbon atoms, aryl and containing from 6 to 10 carbon atoms and hydrogen, andR.sub.9 is alkylene or 1 to 6 carbon atoms,and iron carbonyl complexes thereof,to an area of the human skin in an amount effective to repair damage due to acne or psoriasis.This treatment is not accompanied by substantial discomfort or dermatological irritation.

    摘要翻译： 痤疮和牛皮癣的作用通过局部施用或口服施用来重现，具有以下结构的化合物：其中R 1，R 2，R 3，R 4和R 5独立地选自H，Cl，直链或 1〜10个碳原子的支链烷基，NO2，COOR6，CN，OR6，NR6R7，NR6C（= S）NR7R8，NF6COR7，SO2NR6R7，CH（CH3）COOH，CONR6R7，COR6，OCONR6R7，NR6COONR7，R9OR6，NR6SO2R7，Si CH 3）3和NR 6 CONR 7 R 8，R 3与R 4一起形成苯并环或与R 2一起形成苯并或四氢苯并环或与R 2和R 1一起形成：部分或与R 2一起形成一个或多个 R 2与R 1一起形成苯并环或R 2与R 3一起形成一个“部分”，或者R 1独立地选自下列基团，R 6，R 7和R 8独立地选自直链或 含有1至10个碳原子的支链烷基，芳基和含有6至10个碳原子的氢， 并且R9是亚烷基或1至6个碳原子，以及它们的羰基羰基络合物，可以有效修复由于痤疮或牛皮癣引起的损伤的量的人皮肤区域。 这种治疗不伴有明显的不适或皮肤病刺激。