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：US07678784B2

公开(公告)日：2010-03-16

申请号：US11940597

申请日：2007-11-15

Applicant: Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

Inventor： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

IPC: C07D267/22 ,  C07D225/04 ,  A61K31/33

CPC classification number: C07D273/00

Abstract: There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X 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: 提供了一系列式（I）的含肟的大环酰基胍或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4，n和X，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：US07494986B2

公开(公告)日：2009-02-24

申请号：US11183699

申请日：2005-07-18

Applicant: Yong-Jin Wu ,  Huan He

Inventor： Yong-Jin Wu ,  Huan He

IPC: A01N43/00 ,  A61K31/33 ,  C07D225/00 ,  C07D295/00

CPC classification number: C07D225/02

Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof and pharmaceutically acceptable formulations 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。 具体实施方案涉及式（I）化合物或其异构体，药学上可接受的盐或溶剂合物和药学上可接受的制剂，其包含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：US07390925B2

公开(公告)日：2008-06-24

申请号：US11693026

申请日：2007-03-29

Applicant: Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

Inventor： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

IPC: C07C233/05 ,  A61K31/65

CPC classification number: C07D209/20 ,  C07C257/20 ,  C07C279/22

Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 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: 提供了一系列式（I）的取代的含肟基的酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中R 1，R 2，R 3，R 4，R R 5，R 6和R 7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：US20080139523A1

公开(公告)日：2008-06-12

申请号：US11940597

申请日：2007-11-15

Applicant: Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

Inventor： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

IPC: A61K31/395 ,  C07D405/14 ,  A61P25/28

CPC classification number: C07D273/00

Abstract: There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X 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: 提供了一系列式（I）的含肟的大环酰基胍或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，n和X 如本文所定义的，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：US20070032470A1

公开(公告)日：2007-02-08

申请号：US11494145

申请日：2006-07-27

Applicant: Yong-Jin Wu ,  Yunhui Zhang

Inventor： Yong-Jin Wu ,  Yunhui Zhang

IPC: A61K31/554 ,  A61K31/55 ,  A61K31/54 ,  A61K31/445 ,  A61K31/425 ,  A61K31/4015

CPC classification number: C07C251/48 ,  C07C235/42 ,  C07C235/84 ,  C07C311/08 ,  C07C317/44 ,  C07D279/02

Abstract: There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y 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）的新型苯基羧酰胺或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，X和Y，其药物组合物和方法 的使用。 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：US07135472B2

公开(公告)日：2006-11-14

申请号：US10719187

申请日：2003-11-21

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

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

IPC: A61K31/50 ,  A61K31/496 ,  C07D213/44 ,  C07D413/00 ,  C07D233/54

CPC classification number: C07D213/40 ,  C07D213/82 ,  C07D231/12 ,  C07D233/54 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het 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 novel 3-heterocyclic benzylamides 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: 本发明提供新的3-杂环苄基酰胺和具有通式I的相关衍生物，其中R 1，R 2，R 3，R 3， 其中R 4，R 5，R 6，A和H e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，其中 是KCNQ钾通道的开放剂或活化剂。 本发明还提供包含所述新型3-杂环苄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：US06900210B2

公开(公告)日：2005-05-31

申请号：US10719538

申请日：2003-11-21

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

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

IPC: C07D213/38 ,  C07D213/65 ,  C07D213/68 ,  C07D213/74 ,  C07D239/34 ,  C07D405/12 ,  C07D409/12 ,  C07D213/643 ,  A61K31/4412 ,  A61K31/513 ,  C07D241/18

CPC classification number: C07D213/74 ,  C07D213/38 ,  C07D213/65 ,  C07D213/68 ,  C07D239/34 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z 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 heterocyclic 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的新型杂环酰胺和相关衍生物，其中R 1，R 2，R 3，R 3， 4，R 5，R 6，A，B和Z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，其中 是KCNQ钾通道的开放剂或活化剂。 本发明还提供包含所述杂环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：US06498146B1

公开(公告)日：2002-12-24

申请号：US09688679

申请日：2000-10-16

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08 ,  A61K31/70

Abstract: The invention relates to compounds of the formula 1, 2, and 3 and to pharmaceutically acceptable salts and prodrugs thereof, wherein the groups are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula 1, 2, and 3 the treatment of infections, and methods of preparing said compounds of formula 1, 2, and 3.

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