公开(公告)号：US07045551B2

公开(公告)日：2006-05-16

申请号：US10719465

申请日：2003-11-21

Applicant: Yong-Jin Wu ,  Li-Qiang Sun ,  Huan He ,  Alexandre L'Heureux

Inventor： Yong-Jin Wu ,  Li-Qiang Sun ,  Huan He ,  Alexandre L'Heureux

IPC: A61K31/165 ,  A61K31/34 ,  A61K31/535 ,  C07D265/30 ,  C07D307/78

CPC classification number: C07D295/135 ,  C07C233/19 ,  C07C233/22 ,  C07C233/60 ,  C07C233/73 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/40 ,  C07D307/54 ,  C07D333/24

Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A 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 aryl hydroxyethyl 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: 本发明提供了具有通式I的新型芳基羟乙基酰胺和相关衍生物，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7和A如说明书中所定义，或无毒的药学上可接受的 盐，溶剂合物或水合物，它们是KCNQ钾通道的开放剂或活化剂。 本发明还提供包含所述芳基羟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的方法。

公开(公告)号：US20060020011A1

公开(公告)日：2006-01-26

申请号：US11183702

申请日：2005-07-18

Applicant: Yong-Jin Wu ,  Huan He ,  Joanne Bronson

Inventor： Yong-Jin Wu ,  Huan He ,  Joanne Bronson

IPC: A61K31/4439 ,  A61K31/416 ,  A61K31/405 ,  A61K31/4025 ,  C07D403/02 ,  C07D405/02 ,  C07D409/02

CPC classification number: C07D207/08 ,  C07D403/04

Abstract: The present disclosure relates to chemical compounds and their use in treatment of human diseases. A particular embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salts or solvates thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Abstract translation: 本公开涉及化学化合物及其在治疗人类疾病中的用途。 一个具体实施方案涉及式（I）化合物或其异构体，其药学上可接受的盐或溶剂合物或包含所述化合物的药学上可接受的制剂可用于治疗或预防由速激肽介导的病症和/或选择性抑制5-羟色胺再摄取 转运蛋白。 该化合物作为双重NK-1拮抗剂和选择性5-羟色胺再摄取抑制剂。

公开(公告)号：US20060019944A1

公开(公告)日：2006-01-26

申请号：US11183700

申请日：2005-07-18

Applicant: Yong-Jin Wu ,  Huan He

Inventor： Yong-Jin Wu ,  Huan He

IPC: A61K31/55 ,  A61K31/495 ,  A61K31/445 ,  A61K31/40

CPC classification number: C07C217/52 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14

Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Abstract translation: 本公开涉及化学化合物及其在人类治疗中的用途。 本公开的具体实施方案涉及式（I）的化合物; 或其异构体，药学上可接受的盐或溶剂合物或包含所述化合物的药学上可接受的制剂可用于治疗或预防由速激肽介导的病症和/或选择性抑制5-羟色胺再摄取转运蛋白。 该化合物作为双重NK-1拮抗剂和选择性5-羟色胺再摄取抑制剂。

公开(公告)号：US20060019943A1

公开(公告)日：2006-01-26

申请号：US11183691

申请日：2005-07-18

Applicant: Yong-Jin Wu ,  Huan He

Inventor： Yong-Jin Wu ,  Huan He

IPC: A61K31/55 ,  C07D223/04

CPC classification number: C07D223/04

Abstract: The present disclosure relates to chemical compounds and their use in human therapy. In a specific embodiment, compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

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。

公开(公告)号：US08710061B2

公开(公告)日：2014-04-29

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: A61K31/497 ,  A01N43/54 ,  A01N43/90

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.

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：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：US20130131049A1

公开(公告)日：2013-05-23

申请号：US13478238

申请日：2012-05-23

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1, R2, R3, R4, R5, and R6 are independently hydrogen, C1-C6 alkyl or C1-C6 cycloalkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group, wherein each Y and Z group can be optionally substituted with from 0-3 substituents selected from halogen, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, OH, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is either a bond or is —NHCO—; L and Z together can be absent; and m is 1, 2 or 3.

Abstract translation: 式（I）化合物，包括其药学上可接受的盐，在此列出：其中R 1，R 2，R 3，R 4，R 5和R 6独立地为氢，C 1 -C 6烷基或C 1 -C 6环烷基; Y和Z独立地是C 6 -C 10 - 芳基或5-10元杂环基，其中每个Y和Z基团可以任选地被0-3个选自卤素，氨基，C 1-4烷基氨基，C 1-4二烷基氨基 卤代C 1-4烷基，OH，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是键或是-NHCO-; L和Z一起可以不存在; m为1,2或3。