公开(公告)号：US06300316B1

公开(公告)日：2001-10-09

申请号：US09378886

申请日：1999-08-23

Applicant: Katherine E. Brighty ,  Takushi Kaneko ,  Robert G. Linde, II ,  Hiroko Masamune ,  Paul R. McGuirk ,  Wei-Guo Su ,  Yong-Jin Wu ,  Bingwei V. Yang

Inventor： Katherine E. Brighty ,  Takushi Kaneko ,  Robert G. Linde, II ,  Hiroko Masamune ,  Paul R. McGuirk ,  Wei-Guo Su ,  Yong-Jin Wu ,  Bingwei V. Yang

IPC: A61K3170

CPC classification number: C07D405/14 ,  C07D407/14 ,  C07D417/14 ,  C07D491/04 ,  C07D493/04 ,  C07H17/08

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract translation: 本发明涉及式的化合物及其药学上可接受的盐。 式1的化合物是可用于治疗与这种感染相关的各种细菌和原生动物感染和疾病的有效的抗细菌和抗原虫药。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

公开(公告)号：US06248719B1

公开(公告)日：2001-06-19

申请号：US09485965

申请日：2000-02-18

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The compounds of formula 1 are useful as antibiotic agents. The invention further relates to pharmaceutical compositions and methods of treating bacterial infection using such compounds, and to methods of making the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐，其中R 1 -R 7如本文所定义。 式1的化合物可用作抗生素。 本发明还涉及使用这些化合物治疗细菌感染的药物组合物和方法，以及制备式1化合物的方法。

公开(公告)号：US08637525B2

公开(公告)日：2014-01-28

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: A01N43/54 ,  A01N43/90 ,  A61K31/517 ,  A61K31/519 ,  A01N43/64 ,  A61K31/41

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 。

公开(公告)号：US20110212937A1

公开(公告)日：2011-09-01

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: A61K31/397 ,  C07D401/12 ,  A61K31/517 ,  C07D239/70 ,  C07D403/12 ,  C07D403/14 ,  C07D471/04 ,  A61K31/519 ,  C07D491/052 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/5386 ,  A61P25/28

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：US20110015175A1

公开(公告)日：2011-01-20

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: A61K31/55 ,  C07D487/04 ,  C07D417/12 ,  C07D491/20 ,  A61K31/437 ,  A61K31/428 ,  A61K31/4439 ,  A61P25/28 ,  A61P25/00 ,  A61P27/02 ,  A61P35/00

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：US20080194535A1

公开(公告)日：2008-08-14

申请号：US12019986

申请日：2008-01-25

Applicant: Lawrence R. Marcin ,  Andrew C. Good ,  Yong-Jin Wu ,  Dmitry S. Zuev ,  Richard E. Olson ,  Nenghui Wang

Inventor： Lawrence R. Marcin ,  Andrew C. Good ,  Yong-Jin Wu ,  Dmitry S. Zuev ,  Richard E. Olson ,  Nenghui Wang

IPC: A61K31/395 ,  C07D273/02 ,  A61P25/00

CPC classification number: C07D273/02 ,  C07D413/04 ,  C07D487/04

Abstract: There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L 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）的大环二氨基丙烷或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，m，n，W，X​​，Y，Z和 L，其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：US07087609B2

公开(公告)日：2006-08-08

申请号：US10719188

申请日：2003-11-21

Applicant: Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

Inventor： Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

IPC: A61K31/496 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D409/12 ,  C07D213/74 ,  C07D401/12

Abstract: The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and B are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said piperazinyl phenylethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain, and anxiety.

Abstract translation: 本发明提供具有通式I的哌嗪基苯乙基酰胺和相关衍生物，其中R 1，R 2，R 3，R 3， 4，R 5，R 6，A和B如说明书中所定义，或其无毒的药学上可接受的盐，溶剂合物或水合物，其为开放剂 或KCNQ钾通道的激活剂。 本发明还提供了包含所述哌嗪基苯乙基酰胺的药物组合物和治疗对KCNQ钾通道开放活性敏感的疾病如偏头痛或偏头痛发作，双相情感障碍，癫痫，急性和慢性疼痛和焦虑症的方法。

公开(公告)号：US06664238B1

公开(公告)日：2003-12-16

申请号：US09459116

申请日：1999-12-10

Applicant: Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

Inventor： Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: This invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R15, R16 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐和溶剂化物，其中X 1，X 2，R 2，R 15，R 16和R 6如本文所定义 。 式1的化合物是可用于治疗各种细菌和原生动物感染的抗细菌剂和抗原虫药，以及与这种感染有关的疾病。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

公开(公告)号：US06482801B2

公开(公告)日：2002-11-19

申请号：US09794381

申请日：2001-02-27

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of using said compounds of formula 1 in the treatment of infections, and methods of preparing said compounds of formula 1.

Abstract translation: 本发明涉及式的化合物及其药学上可接受的盐，其中R 1和R 2如本文所定义。 本发明还涉及含有式1化合物的药物组合物，使用式1化合物治疗感染的方法，以及制备所述式1化合物的方法。

公开(公告)号：US06291656B1

公开(公告)日：2001-09-18

申请号：US09341888

申请日：1999-07-15

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: C07H1708

CPC classification number: C07H17/08

Abstract: The invention relates to compounds of the formula I and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said compounds of formula I.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及含有式I化合物的药物组合物，使用式I化合物治疗感染的方法，以及制备所述式I化合物的方法。