公开(公告)号：US08637523B2

公开(公告)日：2014-01-28

申请号：US13180623

申请日：2011-07-12

Applicant: Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Yunhui Zhang

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Yunhui Zhang

IPC: A61P27/02 ,  A61P35/00 ,  C07D498/04 ,  A61P25/28

CPC classification number: C07D487/06 ,  A61K31/33 ,  C07D487/16 ,  C07D498/06 ,  C07D498/16

Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate β-amyloid peptide (β-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 提供式（I）化合物，包括其药学上可接受的盐：其调节β-淀粉样肽（β-AP）产生，并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽（β- AP）生产。

公开(公告)号：US20130030011A1

公开(公告)日：2013-01-31

申请号：US13358822

申请日：2012-01-26

Applicant: KENNETH M. BOY ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

Inventor： KENNETH M. BOY ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: A61K31/517 ,  C07D491/052 ,  A61P35/00 ,  A61P25/28 ,  A61P25/00 ,  A61P27/02 ,  C07D239/70 ,  C07D471/04

CPC classification number: C07D239/70 ,  A61K31/517 ,  A61K31/519 ,  C07D401/04 ,  C07D471/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/10

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

公开(公告)号：US20120184565A1

公开(公告)日：2012-07-19

申请号：US13180623

申请日：2011-07-12

Applicant: Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Yunhui Zhang

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Yunhui Zhang

IPC: A61K31/519 ,  C07D498/14 ,  A61P29/00 ,  A61P25/00 ,  A61P27/02 ,  A61P35/00 ,  C07D498/04 ,  A61P25/28

CPC classification number: C07D487/06 ,  A61K31/33 ,  C07D487/16 ,  C07D498/06 ,  C07D498/16

Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate β-amyloid peptide (β-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 提供式（I）化合物，包括其药学上可接受的盐：其调节和淀粉样蛋白肽（＆bgr; -AP）产生，并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽 （＆bgr; -AP）生产。

公开(公告)号：US08349880B2

公开(公告)日：2013-01-08

申请号：US12683791

申请日：2010-01-07

Applicant: Lawrence R. Marcin ,  Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jason M. Guernon ,  Mendi A. Higgins ,  Jianliang Shi ,  Yong-Jin Wu ,  Yunhui Zhang ,  John E. Macor

Inventor： Lawrence R. Marcin ,  Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jason M. Guernon ,  Mendi A. Higgins ,  Jianliang Shi ,  Yong-Jin Wu ,  Yunhui Zhang ,  John E. Macor

IPC: A61K31/41 ,  A61K31/425 ,  C07D249/00 ,  C07D277/82

CPC classification number: C07D487/04 ,  C07D417/12 ,  C07D471/04 ,  C07D513/10

Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 本公开提供了一系列式（I）的化合物，其减少β-淀粉状蛋白肽（＆bgr--AP）产生，并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽（＆bgr; -AP）生产。

公开(公告)号：US20120028994A1

公开(公告)日：2012-02-02

申请号：US13013373

申请日：2011-01-25

Applicant: Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: A61K31/517 ,  C07D401/14 ,  A61P35/00 ,  A61P25/28 ,  A61P25/00 ,  A61P27/02 ,  C07D403/12 ,  C07D401/12

CPC classification number: A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/052 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 本公开提供了一系列式（I）的化合物，其调节和淀粉样蛋白肽（＆bgr; -AP）产生，并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽（＆bgr; -AP）生产。

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。

公开(公告)号：US07273866B2

公开(公告)日：2007-09-25

申请号：US10731854

申请日：2003-12-09

Applicant: Kenneth M. Boy ,  Yong-Jin Wu ,  Jason M. Guernon

Inventor： Kenneth M. Boy ,  Yong-Jin Wu ,  Jason M. Guernon

IPC: A61K31/5375 ,  A61K31/427 ,  A61K31/426 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07D277/56 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

Abstract: Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraine

Abstract translation: 描述了式I的新型2-芳基噻唑衍生物，其是KCNQ钾通道的开放剂，并且可用于治疗对KCNQ钾通道开放有响应的病症，包括疼痛和偏头痛

公开(公告)号：US07179920B2

公开(公告)日：2007-02-20

申请号：US10964489

申请日：2004-10-13

Applicant: Kenneth M. Boy ,  Piyasena Hewawasam ,  Sing-Yuen Sit

Inventor： Kenneth M. Boy ,  Piyasena Hewawasam ,  Sing-Yuen Sit

IPC: C07D215/38 ,  C07D215/44

CPC classification number: C07D215/36

Abstract: This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including erectile dysfunction and irritable bowel syndrome

Abstract translation: 本发明描述了作为钾通道调节剂的式（I）化合物，可用于治疗受钾通道活动异常影响的病症，包括勃起功能障碍和肠易激综合征

公开(公告)号：US07049309B2

公开(公告)日：2006-05-23

申请号：US10964079

申请日：2004-10-13

Applicant: Kenneth M. Boy ,  Piyasena Hewawasam ,  Sing-Yuen Sit ,  Kai Xie

Inventor： Kenneth M. Boy ,  Piyasena Hewawasam ,  Sing-Yuen Sit ,  Kai Xie

IPC: A61K31/551 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/54

CPC classification number: C04B35/632 ,  C07D215/36 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including erectile dysfunction and irritable bowel syndrome.

Abstract translation: 本发明描述了作为钾通道调节剂的式（I）化合物，并且可用于治疗受异常钾通道活性（包括勃起功能障碍和肠易激综合征）影响的病症。

公开(公告)号：US08486952B2

公开(公告)日：2013-07-16

申请号：US12845045

申请日：2010-07-28

Applicant: Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: A01N43/54 ,  A01N43/90 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/497 ,  A61K31/00 ,  A61K31/535 ,  C07D239/70 ,  C07D491/00 ,  C07D495/00 ,  C07D471/00 ,  C07D413/00

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 本公开提供了一系列调节β-淀粉样肽（β-AP）产生的式（I）化合物，并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽（β-AP）产生影响的病症 。