公开(公告)号：WO2008024398B1

公开(公告)日：2008-08-14

申请号：PCT/US2007018571

申请日：2007-08-22

Applicant: VALEANT PHARMACEUTICALS INT ,  VERNIER JEAN-MICHEL ,  DE LA ROSA MARTHA ALICIA ,  CHEN HUANMING ,  WU JIM ZHEN ,  LARSON GARY LEE ,  CHENEY IAN WAYNE

Inventor： VERNIER JEAN-MICHEL ,  DE LA ROSA MARTHA ALICIA ,  CHEN HUANMING ,  WU JIM ZHEN ,  LARSON GARY LEE ,  CHENEY IAN WAYNE

IPC: A61K31/47

CPC classification number: C07D217/14 ,  C07D217/16

Abstract: This invention provides a compound of formula (IA) where X = O or S; Y is O or S; q = 1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract translation: 本发明提供其中X = O或S的式（IA）化合物; Y为O或S; q = 1或0; 和其它取代基在本文中定义。 这种化合物可影响电压门控钾通道的开启或以其他方式调节。 它们可用于治疗和预防受到钾离子通道活化或调节影响的疾病和病症。 一种这样的病症是癫痫发作。

公开(公告)号：WO2008024398A3

公开(公告)日：2008-06-26

申请号：PCT/US2007018571

申请日：2007-08-22

Applicant: VERNIER JEAN-MICHEL ,  DE LA ROSA MARTHA ALICIA ,  CHEN HUANMING ,  WU JIM ZHEN ,  LARSON GARY LEE ,  CHENEY IAN WAYNE

Inventor： VERNIER JEAN-MICHEL ,  DE LA ROSA MARTHA ALICIA ,  CHEN HUANMING ,  WU JIM ZHEN ,  LARSON GARY LEE ,  CHENEY IAN WAYNE

IPC: A61K31/47

CPC classification number: C07D217/14 ,  C07D217/16

Abstract: This invention provides a compound of formula (IA) where X = O or S; Y is O or S; q = 1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract translation: 本发明提供了式（IA）的化合物，其中X = O或S; Y是O或S; q = 1或0; 和其他取代基在本文中定义。 这种化合物可影响电压门控钾通道的开放或调节。 它们可能用于治疗和预防受钾离子通道活化或调节影响的疾病和病症。 其中一种情况是癫痫症。

公开(公告)号：WO2008024398A2

公开(公告)日：2008-02-28

申请号：PCT/US2007/018571

申请日：2007-08-22

Applicant: VERNIER, Jean-Michel ,  DE LA ROSA, Martha, Alicia ,  CHEN, Huanming ,  WU, Jim, Zhen ,  LARSON, Gary, Lee ,  CHENEY, Ian, Wayne

Inventor： VERNIER, Jean-Michel ,  DE LA ROSA, Martha, Alicia ,  CHEN, Huanming ,  WU, Jim, Zhen ,  LARSON, Gary, Lee ,  CHENEY, Ian, Wayne

CPC classification number: C07D217/14 ,  C07D217/16

Abstract: This invention provides a compound of formula (IA) where X = O or S; Y is O or S; q = 1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract translation: 本发明提供了式（IA）的化合物，其中X = O或S; Y是O或S; q = 1或0; 和其他取代基在本文中定义。 这种化合物可影响电压门控钾通道的开放或调节。 它们可能用于治疗和预防受钾离子通道活化或调节影响的疾病和病症。 其中一种情况是癫痫症。

公开(公告)号：WO2011094953A1

公开(公告)日：2011-08-11

申请号：PCT/CN2010/070562

申请日：2010-02-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  WANG, Lisha ,  CHEN, Li ,  QIU, Zongxing ,  TANG, Guozhi ,  LIN, Xianfeng ,  WU, Jim Zhen ,  YANG, Wengang

Inventor： WANG, Lisha ,  CHEN, Li ,  QIU, Zongxing ,  TANG, Guozhi ,  LIN, Xianfeng ,  WU, Jim Zhen ,  YANG, Wengang

IPC: C07C211/48 ,  C07D213/74 ,  C07D237/06 ,  C07D261/20 ,  C07D231/56 ,  C07D277/82 ,  C07D217/22 ,  C07D237/26 ,  A61K31/16 ,  A61K31/136 ,  A61K31/44 ,  A61K31/505 ,  A61K31/42 ,  A61K31/416 ,  A61K31/423 ,  A61K31/428 ,  A61K31/495 ,  A61K31/47 ,  A61K31/517 ,  A61P31/16

CPC classification number: C07C215/42 ,  C07C211/52 ,  C07C217/52 ,  C07C217/84 ,  C07C219/24 ,  C07C235/40 ,  C07C237/24 ,  C07C237/30 ,  C07C255/58 ,  C07C255/60 ,  C07C2601/14 ,  C07D213/74 ,  C07D217/22 ,  C07D231/56 ,  C07D239/42 ,  C07D239/47 ,  C07D239/84 ,  C07D263/58

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R 1 to R 4 and Ar are as defined in description and in claims, can be used as a medicament.

Abstract translation: 式（I）化合物及其药学上可接受的盐，其中R 1至R 4和Ar如描述和权利要求中所定义，可用作药物。

公开(公告)号：WO2010008894A1

公开(公告)日：2010-01-21

申请号：PCT/US2009/048504

申请日：2009-06-24

Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL ,  WU, Jim, Zhen ,  VERNIER, Jean-michel ,  CHEN, Huanming ,  SONG, Jianlan

Inventor： WU, Jim, Zhen ,  VERNIER, Jean-michel ,  CHEN, Huanming ,  SONG, Jianlan

IPC: C07D213/30 ,  A61K31/472

CPC classification number: C07C233/25 ,  C07C233/26 ,  C07C271/28

Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula (I): The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract translation: 本发明涉及具有以下结构式（I）的苄氧基苯胺衍生物：本发明化合物可用于治疗和预防受到钾离子通道活化或调节影响的疾病和病症。 一种这样的病症是癫痫发作。

公开(公告)号：WO2008157802A1

公开(公告)日：2008-12-24

申请号：PCT/US2008/067763

申请日：2008-06-20

Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL ,  WU, Jim, Zhen ,  CHEN, Huanming

Inventor： WU, Jim, Zhen ,  CHEN, Huanming

IPC: C07D275/03 ,  A61K31/425 ,  A61P39/00

CPC classification number: C07D275/03

Abstract: This invention provides compounds of Formula (I), which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to said isothiocyanate group to form a thioamide adduct; d) cyclizing said thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to said cyano group to form a carboxamidine group.

Abstract translation: 本发明提供式（I）化合物，其为Chk2的抑制剂，可用作抗癌放射治疗中的辐射防护剂。 在体外调节Chk2的方法包括在式I化合物存在下用Chk2处理底物。制备式I化合物的方法包括：a）形成具有氨基（NH 2）基团的联芳基胺; b）将氨基转化为异硫氰酸酯基; c）向所述异硫氰酸酯基团加入氰基乙酰胺以形成硫代酰胺加合物; d）环化所述硫代酰胺加合物以形成具有氰基的异噻唑; 和e）向所述氰基中加入胺形成甲脒基。

公开(公告)号：WO2008066900A1

公开(公告)日：2008-06-05

申请号：PCT/US2007/024607

申请日：2007-11-28

Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL ,  CHEN, Huanming ,  SONG, Jenny ,  VERNIER, Jean-michel ,  WU, Jim, Zhen

Inventor： CHEN, Huanming ,  SONG, Jenny ,  VERNIER, Jean-michel ,  WU, Jim, Zhen

IPC: C07C233/41 ,  C07C271/30 ,  A61K31/165

CPC classification number: C07C233/41 ,  C07C2602/08 ,  C07C2602/10 ,  C07D213/74

Abstract: This invention is directed to compounds of formula (I), where G is -O-, -S-, -C(g1)(g2)-, or -NH-, and n = 1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.

Abstract translation: 本发明涉及式（I）化合物，其中G是-O - ， - S - ， - C（g1）（g2） - 或-NH-，n = 1,2或3。 调节钾通道。 该化合物可用于治疗和预防受钾离子通道调节影响的疾病和病症。 一种这样的病症是癫痫发作。

公开(公告)号：WO2013020993A1

公开(公告)日：2013-02-14

申请号：PCT/EP2012/065499

申请日：2012-08-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHEN, Li ,  FENG, Lichun ,  FENG, Song ,  GAO, Lu ,  GUO, Tao ,  HUANG, Mengwei ,  LIANG, Chungen ,  LIU, Yongfu ,  WANG, Lisha ,  WONG, Jason Christopher ,  WU, Jim Zhen ,  WU, Xihan ,  YUN, Hongying ,  ZHENG, Xiufang

Inventor： CHEN, Li ,  FENG, Lichun ,  FENG, Song ,  GAO, Lu ,  GUO, Tao ,  HUANG, Mengwei ,  LIANG, Chungen ,  LIU, Yongfu ,  WANG, Lisha ,  WONG, Jason Christopher ,  WU, Jim Zhen ,  WU, Xihan ,  YUN, Hongying ,  ZHENG, Xiufang

IPC: C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  A61K31/553 ,  A61K31/554 ,  A61P11/00 ,  A61P31/12

CPC classification number: C07D493/10 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D491/107

Abstract: A compound of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R 1 to R 10 , A, Q, X and Y are as defined in description and in claims, can be used as a medicament for the treatment of respiratory syncytial virus.

Abstract translation: 式（I）化合物及其药学上可接受的盐，其中R 1至R 10，A，Q，X和Y如描述和权利要求中所定义，可用作治疗呼吸道合胞病毒的药物 。

公开(公告)号：WO2011128251A1

公开(公告)日：2011-10-20

申请号：PCT/EP2011/055473

申请日：2011-04-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHEN, Li ,  FENG, Lichun ,  HUANG, Mengwei ,  LIU, Yongfu ,  WU, Guolong ,  WU, Jim, Zhen ,  ZHOU, Mingwei

Inventor： CHEN, Li ,  FENG, Lichun ,  HUANG, Mengwei ,  LIU, Yongfu ,  WU, Guolong ,  WU, Jim, Zhen ,  ZHOU, Mingwei

IPC: C07D215/12 ,  C07D215/18 ,  C07D215/36 ,  C07D215/48 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D471/04 ,  A61K31/47 ,  A61P3/00

CPC classification number: C07D215/48 ,  C07D215/12 ,  C07D215/18 ,  C07D215/36 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D471/04

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R 1 to R 5 have the significance given in claim 1, can be used as a medicament.

Abstract translation: 式（I）化合物及其药学上可接受的盐，其中R 1至R 5具有权利要求1中给出的含义，可用作药物。

公开(公告)号：WO2011095576A1

公开(公告)日：2011-08-11

申请号：PCT/EP2011/051626

申请日：2011-02-04

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHEN, Li ,  LIN, Xianfeng ,  QIU, Zongxing ,  TANG, Guozhi ,  WANG, Lisha ,  WU, Jim Zhen ,  YANG, Wengang

Inventor： CHEN, Li ,  LIN, Xianfeng ,  QIU, Zongxing ,  TANG, Guozhi ,  WANG, Lisha ,  WU, Jim Zhen ,  YANG, Wengang

IPC: C07C215/70 ,  C07C235/40 ,  C07C237/24 ,  C07C237/30 ,  C07C255/59 ,  A61K31/16 ,  A61K31/135

CPC classification number: C07C215/42 ,  C07C211/52 ,  C07C217/52 ,  C07C217/84 ,  C07C219/24 ,  C07C235/40 ,  C07C237/24 ,  C07C237/30 ,  C07C255/58 ,  C07C255/60 ,  C07C2601/14 ,  C07D213/74 ,  C07D217/22 ,  C07D231/56 ,  C07D239/42 ,  C07D239/47 ,  C07D239/84 ,  C07D263/58

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R 1 to R 4 and Ar are as defined in description and in claims, can be used as a medicament.

Abstract translation: 式（I）的化合物及其药学上可接受的盐，其中R 1至R 4和Ar如说明书中所定义 并且在权利要求中，可以用作药物。