公开(公告)号：US20150057307A1

公开(公告)日：2015-02-26

申请号：US14311825

申请日：2014-06-23

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： C07D471/04 ,  C07D263/32 ,  C07D401/04 ,  C07D271/06 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

摘要翻译： 提供激活亚型1的鞘氨醇-1-磷酸受体的化合物。 某些化合物选择性地激活了关于鞘氨醇 - 1-磷酸受体亚型3的受体亚型1。本发明化合物的用途和方法用于治疗病症，其中在医学上指示S1P1的活化，激动，抑制或拮抗作用。

公开(公告)号：US08481573B2

公开(公告)日：2013-07-09

申请号：US13605561

申请日：2012-09-06

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： A61K31/4245 ,  C07D271/06

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.

公开(公告)号：US09089572B2

公开(公告)日：2015-07-28

申请号：US12321463

申请日：2009-01-20

申请人： Steven J. Brown ,  Tsui-Fen Chou ,  Raymond Deshaies ,  Amanda C. Jones ,  Hugh Rosen ,  Brian M. Stoltz

发明人： Steven J. Brown ,  Tsui-Fen Chou ,  Raymond Deshaies ,  Amanda C. Jones ,  Hugh Rosen ,  Brian M. Stoltz

IPC分类号： A61K31/519

CPC分类号： A61K31/519

摘要： One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.

公开(公告)号：US08530503B2

公开(公告)日：2013-09-10

申请号：US13605358

申请日：2012-09-06

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： A61K31/4245 ,  C07D271/06

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.

摘要翻译： 提供以下通用结构的化合物：这样的化合物活化亚型1（S1P1）的鞘氨醇-1-磷酸受体，并且可用于治疗由S1P1活化介导的病态。 更具体地，这些化合物有益于治疗例如多发性硬化，移植排斥和/或成人呼吸综合征。

公开(公告)号：US20120329838A1

公开(公告)日：2012-12-27

申请号：US13605358

申请日：2012-09-06

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： C07D271/06 ,  A61P37/06 ,  A61P25/00 ,  A61P11/00 ,  A61K31/4245 ,  C12N5/071

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

公开(公告)号：US20050070506A1

公开(公告)日：2005-03-31

申请号：US10501176

申请日：2003-01-14

申请人： George Doherty ,  Michael Forrest ,  Richard Hajdu ,  Jeffrey Hale ,  Li Zhen ,  Susanne Mandala ,  Sander Mills ,  Hugh Rosen ,  Edward Scolnick

发明人： George Doherty ,  Michael Forrest ,  Richard Hajdu ,  Jeffrey Hale ,  Li Zhen ,  Susanne Mandala ,  Sander Mills ,  Hugh Rosen ,  Edward Scolnick

IPC分类号： A61K31/00 ,  A61K31/66 ,  G01N33/566

CPC分类号： A61K31/66 ,  A61K31/00 ,  G01N33/566 ,  G01N2500/04

摘要： The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.

摘要翻译： 本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法，包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物，其中所述化合物 对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性，所述化合物以有效治疗所述免疫调节异常的量给药。 包括药物组合物。 本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法，并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。 本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法，包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物 其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。

公开(公告)号：US08466183B2

公开(公告)日：2013-06-18

申请号：US13605427

申请日：2012-09-06

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： A61K31/4245 ,  C07D271/06

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.

公开(公告)号：US20090253717A1

公开(公告)日：2009-10-08

申请号：US12321463

申请日：2009-01-20

申请人： Steven J. Brown ,  Tsui-Fen Chou ,  Raymond Deshaies ,  Amanda C. Jones ,  Hugh Rosen ,  Brian M. Stoltz

发明人： Steven J. Brown ,  Tsui-Fen Chou ,  Raymond Deshaies ,  Amanda C. Jones ,  Hugh Rosen ,  Brian M. Stoltz

IPC分类号： A61K31/519 ,  A61P35/00

CPC分类号： A61K31/519

摘要： One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.

摘要翻译： 本发明的一个方面涉及抑制p97活性的化合物，例如通过与活性位点中的半胱氨酸残基共价结合。 在某些实施方案中，本发明涉及疾病如癌症的治疗，其包括施用本发明的化合物。

公开(公告)号：US20120329839A1

公开(公告)日：2012-12-27

申请号：US13605427

申请日：2012-09-06

申请人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

发明人： Edward Roberts ,  Hugh Rosen ,  Steven Brown ,  Miguel A. Guerrero ,  Xuemei Peng ,  Ramulu Poddutoori

IPC分类号： A61K31/4245 ,  A61P11/00 ,  A61P37/06 ,  C07D271/06 ,  A61P25/00

CPC分类号： C07D271/06 ,  A61K31/4245 ,  C07D263/32 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04

摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

摘要翻译： 提供激活亚型1的鞘氨醇-1-磷酸受体的化合物。 某些化合物选择性地激活了关于鞘氨醇 - 1-磷酸受体亚型3的受体亚型1。本发明化合物的用途和方法用于治疗病症，其中在医学上指示S1P1的活化，激动，抑制或拮抗作用。

公开(公告)号：US06437165B1

公开(公告)日：2002-08-20

申请号：US09942411

申请日：2001-08-30

申请人： Suzanne Mandala ,  James Bergstrom ,  Richard Hajdu ,  Hugh Rosen ,  William Parsons ,  Deborah J. Card ,  Malcolm Maccoss ,  Rupprecht Kathleen

发明人： Suzanne Mandala ,  James Bergstrom ,  Richard Hajdu ,  Hugh Rosen ,  William Parsons ,  Deborah J. Card ,  Malcolm Maccoss ,  Rupprecht Kathleen

IPC分类号： A61K31662

CPC分类号： C07F9/094 ,  C07F9/3882

摘要： Immunoregulatory compounds are disclosed of the formula: as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

摘要翻译： 公开了具有下式的免疫调节化合物：以及其药学上可接受的盐和水合物。 该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥。包括药物组合物和使用方法。