公开(公告)号：US09090573B2

公开(公告)日：2015-07-28

申请号：US13498491

申请日：2010-10-01

申请人： Thomas J Seiders ,  Lucy Zhao ,  Jeannie Arruda ,  Bowei Wang ,  Brian Andrew Stearns ,  Yem Pham Truong ,  Jill Melissa Scott ,  John Howard Hutchinson ,  Ryan Clark ,  Heather Renee Coate ,  Nicholas Simon Stock ,  Deborah Volkots

发明人： Thomas J Seiders ,  Lucy Zhao ,  Jeannie Arruda ,  Bowei Wang ,  Brian Andrew Stearns ,  Yem Pham Truong ,  Jill Melissa Scott ,  John Howard Hutchinson ,  Ryan Clark ,  Heather Renee Coate ,  Nicholas Simon Stock ,  Deborah Volkots

IPC分类号： C07D495/04 ,  C07D417/12 ,  C07D413/06 ,  C07D413/12 ,  C07D261/08 ,  C07D261/14 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/519

CPC分类号： C07D261/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/519 ,  C07D261/14 ,  C07D261/18 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。

公开(公告)号：US20120289522A1

公开(公告)日：2012-11-15

申请号：US13498491

申请日：2010-10-01

申请人： Thomas J. Seiders ,  Lucy Zhao ,  Jeannie Arruda ,  Bowei Wang ,  Brian Andrew Stearns ,  Yen Pham Truong ,  Jill Melissa Scott ,  John Howard Hutchinson ,  Ryan Clark ,  Heather Renee Coate ,  Nicholas Simon Stock ,  Deborah Volkots

发明人： Thomas J. Seiders ,  Lucy Zhao ,  Jeannie Arruda ,  Bowei Wang ,  Brian Andrew Stearns ,  Yen Pham Truong ,  Jill Melissa Scott ,  John Howard Hutchinson ,  Ryan Clark ,  Heather Renee Coate ,  Nicholas Simon Stock ,  Deborah Volkots

IPC分类号： A61K31/42 ,  C07D261/08 ,  C07D413/12 ,  A61K31/4439 ,  C07D417/12 ,  A61P17/00 ,  C07D495/04 ,  A61K31/519 ,  A61P11/00 ,  A61P13/12 ,  A61P1/16 ,  C07D261/14 ,  A61K31/428

CPC分类号： C07D261/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/519 ,  C07D261/14 ,  C07D261/18 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

公开(公告)号：US08664220B2

公开(公告)日：2014-03-04

申请号：US13499052

申请日：2010-09-29

申请人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas J. Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

发明人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas J. Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

IPC分类号： A61K31/42 ,  C07D261/14

CPC分类号： C07D231/38 ,  C07D261/08 ,  C07D261/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。

公开(公告)号：US20130072490A1

公开(公告)日：2013-03-21

申请号：US13499052

申请日：2010-09-29

申请人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas Jon Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

发明人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas Jon Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

IPC分类号： A61K31/42 ,  C07D413/14 ,  C07D413/04 ,  C07D261/14 ,  C07D413/06 ,  C07D261/06

CPC分类号： C07D231/38 ,  C07D261/08 ,  C07D261/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。

公开(公告)号：US07087601B2

公开(公告)日：2006-08-08

申请号：US10497452

申请日：2002-11-26

申请人： Jeannie Arruda ,  Celine Bonnefous ,  Brian T. Campbell ,  Rowena V. Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

发明人： Jeannie Arruda ,  Celine Bonnefous ,  Brian T. Campbell ,  Rowena V. Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

IPC分类号： A61K31/5383 ,  A61K31/437 ,  C07D413/14 ,  C07D491/048

CPC分类号： C07D263/57 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

摘要： Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

摘要翻译： 苯基化合物在1-位上被一个稠合的双环自由基组成，它由与六元碳环稠合的五元杂环，六元芳基或六元杂芳基形成，并进一步任选地被取代在3位上 ，4个位置是mGluR5调节剂，可用于治疗精神病和情绪障碍，例如精神分裂症，焦虑，抑郁和恐慌，以及治疗疼痛和其他疾病。

公开(公告)号：US20050065340A1

公开(公告)日：2005-03-24

申请号：US10497452

申请日：2002-11-26

申请人： Jeannie Arruda ,  Celine Bonnefous ,  Brian Campbell ,  Rowena Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

发明人： Jeannie Arruda ,  Celine Bonnefous ,  Brian Campbell ,  Rowena Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

IPC分类号： C07D263/56 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P25/36 ,  A61P29/00 ,  A61P43/00 ,  C07D263/57 ,  C07D413/10 ,  C07D498/04 ,  C07D521/00 ,  C07D471/02 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

CPC分类号： C07D263/57 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

摘要： Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at 2 the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

摘要翻译： 苯基化合物在1位上被一个稠合的双环形成，由与六元碳环稠合的五元杂环，六元芳基或六元杂芳基形成，并进一步任选地在2位上被取代 3,4位是用于治疗精神病和情绪障碍（例如精神分裂症，焦虑，抑郁和恐慌）以及治疗疼痛和其他疾病的mGluR5调节剂。

公开(公告)号：US20070219206A1

公开(公告)日：2007-09-20

申请号：US11744555

申请日：2007-05-04

申请人： John Hutchinson ,  Petpiboon Prasit ,  Mark Moran ,  Jillian Evans ,  Brian Stearns ,  Jeffrey Roppe ,  Bowei Wang ,  Yen Truong ,  Yiwei Li ,  Jasmine Zunic ,  Jeannie Arruda ,  Nicholas Stock ,  Mustapha Haddach ,  Thomas Seiders ,  Jill Scott

发明人： John Hutchinson ,  Petpiboon Prasit ,  Mark Moran ,  Jillian Evans ,  Brian Stearns ,  Jeffrey Roppe ,  Bowei Wang ,  Yen Truong ,  Yiwei Li ,  Jasmine Zunic ,  Jeannie Arruda ,  Nicholas Stock ,  Mustapha Haddach ,  Thomas Seiders ,  Jill Scott

IPC分类号： A61K31/506 ,  A61K31/501 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/4439 ,  A61K31/42 ,  A61K31/428 ,  A61K31/404 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

公开(公告)号：US20070105866A1

公开(公告)日：2007-05-10

申请号：US11553946

申请日：2006-10-27

申请人： John Hutchinson ,  Petpiboon Prasit ,  Mark Moran ,  Jillian Evans ,  Yiwei Li ,  Jasmine Zunic ,  Jeannie Arruda ,  Nicholas Stock ,  Brian Stearns ,  Mustapha Haddach ,  Jeffrey Roppe

发明人： John Hutchinson ,  Petpiboon Prasit ,  Mark Moran ,  Jillian Evans ,  Yiwei Li ,  Jasmine Zunic ,  Jeannie Arruda ,  Nicholas Stock ,  Brian Stearns ,  Mustapha Haddach ,  Jeffrey Roppe

IPC分类号： A61K31/501 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/427 ,  C07D417/02 ,  C07D403/02

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

公开(公告)号：US20070123587A1

公开(公告)日：2007-05-31

申请号：US10574655

申请日：2004-10-18

申请人： Jeannie Arruda ,  Benito Munoz ,  Brian Stearns

发明人： Jeannie Arruda ,  Benito Munoz ,  Brian Stearns

IPC分类号： A61K31/235 ,  C07C317/24

CPC分类号： C07C317/46 ,  C07C2601/02

摘要： The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).

摘要翻译： 本发明包括式（I）和式（II）的新型化合物，其是在体内转化成可用于治疗环氧合酶-2介导的疾病的二芳基-2-（5H） - 呋喃酮的前药。 这些前药在水性介质中比在体内转化的活性剂更易溶于水。 因为式（I）和（II）的这样的化合物除了其它的静脉内给药之外是有利的。 本发明还包括用于治疗环氧合酶-2介导的疾病的某些药物组合物和方法，其包括使用式（I）和式（II）的化合物。

公开(公告)号：US20060154929A1

公开(公告)日：2006-07-13

申请号：US10520962

申请日：2003-07-08

申请人： Naomi Anker ,  Jeannie Arruda ,  Brian Campbell ,  Benito Munoz ,  Petpiboon Prasit ,  Brian Stearns ,  Tao Hu

发明人： Naomi Anker ,  Jeannie Arruda ,  Brian Campbell ,  Benito Munoz ,  Petpiboon Prasit ,  Brian Stearns ,  Tao Hu

IPC分类号： A61K31/503

CPC分类号： C07D487/04 ,  A61K31/045 ,  A61K31/05 ,  A61K31/435 ,  A61K31/495 ,  A61K31/50 ,  A61K31/503

摘要： 6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.

摘要翻译： 6H-吡咯并[3,4-d]哒嗪化合物及其用作电压门控钙通道（VGCC）配体的方法，可用于治疗神经性疼痛，以及精神和心境障碍，例如精神分裂症， 焦虑，抑郁，恐慌和双相情感障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等。