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：US07098203B2

公开(公告)日：2006-08-29

申请号：US11183691

申请日：2005-07-18

Applicant: Yong-Jin Wu ,  Huan He

Inventor： Yong-Jin Wu ,  Huan He

IPC: A61P25/00 ,  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.

Abstract translation: 本公开涉及化学化合物及其在人类治疗中的用途。 在具体实施方案中，式（I）化合物或其异构体，药学上可接受的盐或溶剂合物或药学上可接受的制剂，其包含用于治疗或预防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 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：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：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。