公开(公告)号：WO2008157404A2

公开(公告)日：2008-12-24

申请号：PCT/US2008066984

申请日：2008-06-13

Applicant: VALEANT PHARMACEUTICALS INT ,  VERNIER JEAN-MICHEL ,  OUK SAMEDY ,  DE LA ROSA MARTHA ALICIA

Inventor： VERNIER JEAN-MICHEL ,  OUK SAMEDY ,  DE LA ROSA MARTHA ALICIA

IPC: C07D401/04 ,  A61K31/4725 ,  A61P25/08 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

Abstract: This invention provides potassium channel modulators which are compounds of formula (I), (formula I), where at least one of W and Z is N; where the moiety (formula II), is one of Groups A or B below (formula A), where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.

Abstract translation: 本发明提供钾通道调节剂，其为式（I），（式I）的化合物，其中W和Z中的至少一个为N; 其中部分（式II）是下文A或B中的一个（式A），其中Ar是1,2-稠合的六元环芳族基团，带有如下定义的取代基R 1和R 2，并且含有0或 一环氮原子; 并且其中其它取代基在本文中定义。 本发明还提供包含药学上可接受的载体和至少一种以下的组合物：i）药学有效量的式I化合物和ii）其药学上可接受的盐，酯或前药。 本发明还提供了预防或治疗受钾通道活性影响的疾病或病症的方法，包括向有需要的患者施用治疗有效量的式I化合物或其盐，酯或前药 。

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：WO2012102985A1

公开(公告)日：2012-08-02

申请号：PCT/US2012/022161

申请日：2012-01-23

Applicant: GLAXOSMITHKLINE LLC ,  DE LA ROSA, Martha Alicia ,  HAYDAR, Simon, N. ,  JOHNS, Brian Alvin ,  VELTHUISEN, Emile Johann

Inventor： DE LA ROSA, Martha Alicia ,  HAYDAR, Simon, N. ,  JOHNS, Brian Alvin ,  VELTHUISEN, Emile Johann

IPC: A01N43/42 ,  A61K31/47

CPC classification number: C07D217/24 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14

Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).

Abstract translation: 本发明提供了其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由逆转录病毒病毒家族成员（例如人类免疫缺陷病毒（HIV））介导的病毒感染的用途。

公开(公告)号：WO2008157404A3

公开(公告)日：2008-12-24

申请号：PCT/US2008/066984

申请日：2008-06-13

Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL ,  VERNIER, Jean-michel ,  OUK, Samedy ,  DE LA ROSA, Martha, Alicia

Inventor： VERNIER, Jean-michel ,  OUK, Samedy ,  DE LA ROSA, Martha, Alicia

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  A61K31/4725 ,  A61P25/08

Abstract: This invention provides potassium channel modulators which are compounds of formula (I), (formula I), where at least one of W and Z is N; where the moiety (formula II), is one of Groups A or B below (formula A), where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.

公开(公告)号：WO2013012649A1

公开(公告)日：2013-01-24

申请号：PCT/US2012/046354

申请日：2012-07-12

Applicant: GLAXOSMITHKLINE LLC ,  DE LA ROSA, Martha, Alicia ,  JOHNS, Brian, Alvin ,  SAMANO, Vicente ,  VELTHUISEN, Emile, Johann ,  WEATHERHEAD, Jason

Inventor： DE LA ROSA, Martha, Alicia ,  JOHNS, Brian, Alvin ,  SAMANO, Vicente ,  VELTHUISEN, Emile, Johann ,  WEATHERHEAD, Jason

IPC: A01N43/42 ,  A61K31/44

CPC classification number: A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/538 ,  C07D471/04 ,  C07D491/052

Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).

Abstract translation: 本发明提供了其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由逆转录病毒病毒家族成员（例如人类免疫缺陷病毒（HIV））介导的病毒感染的用途。

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。