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    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    1.
    发明申请
    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 有权
    用于还原β-淀粉样生成的化合物

    公开(公告)号：US20130131051A1

    公开(公告)日：2013-05-23

    申请号：US13477143

    申请日：2012-05-22

    Applicant: LORIN A. THOMPSON, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

    Inventor： LORIN A. THOMPSON, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

    IPC: C07D279/08 ,  C07D513/04 ,  C07D417/10

    CPC classification number: C07D279/08 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D513/04

    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.

    Abstract translation: 包括其药学上可接受的盐的式（I）化合物在本文中阐述：其中X选自CH 2，O和NR 2; m = 0或1; 每个实例的R 1选自卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是键，-NHCO-，-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素，卤代C 1-4烷氧基，4-甲氧基苯基，羟基，氨基，C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基， C 1-4烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢，苄基，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，乙酰基和甲磺酰基; 并且R 3，R 4和R 5独立地选自氢或C 1-4烷基。

    Substituted tetrahydroisoquinolines as β-secretase inhibitors
    4.
    发明授权
    Substituted tetrahydroisoquinolines as β-secretase inhibitors 有权
    取代的四氢异喹啉作为分泌酶抑制剂

    公开(公告)号：US07902218B2

    公开(公告)日：2011-03-08

    申请号：US11951516

    申请日：2007-12-06

    Applicant: Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    Inventor： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    IPC: C07D217/00 ,  A61K31/47

    CPC classification number: C07K5/06139 ,  C07D471/04

    Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 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.

    Abstract translation: 提供一系列式（I）的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐，其中R，R 8和R 9如本文所定义，其药物组合物和使用方法。 这些化合物通过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的生成。 本公开涉及可用于治疗与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。

    Indole acetic acid acyl guanidines as β-secretase inhibitors
    5.
    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

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

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

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

    CPC classification number: C07D209/18

    Abstract: 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.

    Abstract translation: 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。

    Lactams as inhibitors of A-&bgr; protein production
    6.
    发明授权
    Lactams as inhibitors of A-&bgr; protein production 有权
    内酰胺类作为A-β蛋白生产的抑制剂

    公开(公告)号：US06495540B2

    公开(公告)日：2002-12-17

    申请号：US09817957

    申请日：2001-03-27

    Applicant: Lorin A. Thompson

    Inventor： Lorin A. Thompson

    IPC: A61K3155

    CPC classification number: C07D223/12 ,  A61K31/55

    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

    Abstract translation: 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

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