公开(公告)号：US07981913B2

公开(公告)日：2011-07-19

申请号：US12779986

申请日：2010-05-14

Applicant: Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

Inventor： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

IPC: A61K31/42 ,  C07D263/30

CPC classification number: C07D265/30 ,  C07D207/09 ,  C07D207/12 ,  C07D207/27 ,  C07D265/32 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel 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: 提供了一系列取代的式（I）的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐，其中如本文所定义的W，R 3，R 5和R 6，其药物组合物和使用方法。 这些新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。

公开(公告)号：US20100222581A1

公开(公告)日：2010-09-02

申请号：US12779986

申请日：2010-05-14

Applicant: Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

Inventor： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

IPC: C07D413/14 ,  C07D403/12 ,  C07D207/12 ,  C07D265/30 ,  C07D207/09 ,  C07D413/12 ,  C07D207/27

CPC classification number: C07D265/30 ,  C07D207/09 ,  C07D207/12 ,  C07D207/27 ,  C07D265/32 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel 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: 提供了一系列取代的式（I）的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐，其中如本文所定义的W，R 3，R 5和R 6，其药物组合物和使用方法。 这些新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。

公开(公告)号：US07408071B2

公开(公告)日：2008-08-05

申请号：US11693034

申请日：2007-03-29

Applicant: Kenneth M. Boy ,  Shirong Zhu ,  John E. Macor ,  Shuhao Shi ,  Samuel Gerritz

Inventor： Kenneth M. Boy ,  Shirong Zhu ,  John E. Macor ,  Shuhao Shi ,  Samuel Gerritz

IPC: C07D207/04 ,  C07D207/00 ,  A01N43/64 ,  A01N43/36

CPC classification number: C07D207/16 ,  C07D209/52

Abstract: There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p 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）的取代的N-芳基吡咯烷衍生物或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4， 它们的药物组合物和方法，如本文所定义的，其中R 5，R 5，R 6，R 7， 的使用。 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。

公开(公告)号：US20080153868A1

公开(公告)日：2008-06-26

申请号：US11951516

申请日：2007-12-06

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

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

IPC: A61K31/437 ,  C07D217/00 ,  A61K31/47 ,  A61P25/00 ,  A61P25/28 ,  C07D221/02

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 8 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。

公开(公告)号：US07388007B2

公开(公告)日：2008-06-17

申请号：US11206441

申请日：2005-08-18

Applicant: Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

Inventor： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

IPC: A61K31/4025 ,  A61K31/5377 ,  C07D207/04 ,  C07D413/12

CPC classification number: C07D277/42 ,  C07D417/12 ,  C07K5/06139

Abstract: There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel 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）的新型取代的γ-内酰胺或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 4，R 5和R 5， 它们的药物组合物和使用方法。 这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白（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。

公开(公告)号：US20070232679A1

公开(公告)日：2007-10-04

申请号：US11693034

申请日：2007-03-29

Applicant: Kenneth M. Boy ,  Shirong Zhu ,  John E. Macor ,  Shuhao Shi ,  Samuel Gerritz

Inventor： Kenneth M. Boy ,  Shirong Zhu ,  John E. Macor ,  Shuhao Shi ,  Samuel Gerritz

IPC: A61K31/403 ,  A61K31/4025 ,  A61K31/401

CPC classification number: C07D207/16 ,  C07D209/52

Abstract: There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p 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）的取代的N-芳基吡咯烷衍生物或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4， 它们的药物组合物和方法，如本文所定义的，其中R 5，R 5，R 6，R 7， 的使用。 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。