公开(公告)号：US20090105318A1

公开(公告)日：2009-04-23

申请号：US12225375

申请日：2007-03-27

申请人： Paul J. Coleman ,  John D. Schreier

发明人： Paul J. Coleman ,  John D. Schreier

IPC分类号： A61K31/427 ,  C07D417/12 ,  A61K31/4192 ,  C07D403/12 ,  A61P25/20

CPC分类号： C07D403/12 ,  C07D417/12

摘要： The present invention is directed to amidoethylthioether compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲肽受体的拮抗剂的酰氨基乙硫醚化合物，其可用于治疗或预防涉及食欲肽受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US08623863B2

公开(公告)日：2014-01-07

申请号：US13125174

申请日：2009-10-15

申请人： Paul J. Coleman ,  Mark E. Fraley ,  John D. Schreier

发明人： Paul J. Coleman ,  Mark E. Fraley ,  John D. Schreier

IPC分类号： A61K31/55 ,  A61P43/00 ,  C07D223/12

CPC分类号： C07D223/12 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

摘要： The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的二取代氮杂环庚烷和氧氮杂环酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US08592457B2

公开(公告)日：2013-11-26

申请号：US13124568

申请日：2009-10-26

申请人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mamio Christa Mattern ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker

发明人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mamio Christa Mattern ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker

IPC分类号： A61K31/4436 ,  C07D417/14

CPC分类号： C07D401/04 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D417/14

摘要： The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的异烟酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US08003797B2

公开(公告)日：2011-08-23

申请号：US12669909

申请日：2008-08-07

申请人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mark E. Fraley ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker ,  Justin T. Steen

发明人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mark E. Fraley ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker ,  Justin T. Steen

IPC分类号： C07D213/22 ,  C07D213/44

CPC分类号： C07D213/82 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  C07D401/04 ,  C07D401/14

摘要： The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的吡啶羧酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US20100261724A1

公开(公告)日：2010-10-14

申请号：US12739294

申请日：2008-10-23

申请人： James C. Barrow ,  Paul J. Coleman ,  Thomas S. Reger ,  Kelly-Ann S. Schlegel ,  Youheng Shu ,  Zhi-Qiang Yang

发明人： James C. Barrow ,  Paul J. Coleman ,  Thomas S. Reger ,  Kelly-Ann S. Schlegel ,  Youheng Shu ,  Zhi-Qiang Yang

IPC分类号： A61K31/5025 ,  C07D401/12 ,  A61K31/517 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61K31/497 ,  A61K31/4439 ,  C07D487/04 ,  C07D413/12 ,  A61K31/443 ,  C07D405/12 ,  C07D417/12 ,  A61K31/437 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D213/65 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

摘要： The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

摘要翻译： 本发明涉及作为T型钙通道拮抗剂的杂环苯酰胺化合物，其可用于治疗或预防涉及T型钙通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US20100152191A1

公开(公告)日：2010-06-17

申请号：US12600960

申请日：2008-05-19

申请人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

发明人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

IPC分类号： A61K31/427 ,  C07D417/14 ,  A61K31/498 ,  A61P25/00

CPC分类号： C07D417/14 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/41 ,  C07D403/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D473/36 ,  C07D498/04

摘要： The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的环丙基脯氨酸双酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US07294640B2

公开(公告)日：2007-11-13

申请号：US11040522

申请日：2005-01-21

申请人： Paul J. Coleman ,  Robert M. Garbaccio ,  Lou Anne Neilson

发明人： Paul J. Coleman ,  Robert M. Garbaccio ,  Lou Anne Neilson

IPC分类号： A61K31/426 ,  C07D277/22 ,  C07D277/28 ,  C07D277/26 ,  C07D277/24

CPC分类号： C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/40 ,  C07D277/56 ,  C07D417/04

摘要： The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白和MCAK活性相关的疾病以及用于抑制KSP驱动蛋白和MCAK的取代的噻唑衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：US08410142B2

公开(公告)日：2013-04-02

申请号：US12528142

申请日：2008-02-29

申请人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

发明人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

IPC分类号： A61K31/4418 ,  C07D213/22

CPC分类号： C07D213/82 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

摘要： The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的联吡啶羧酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US20110207747A1

公开(公告)日：2011-08-25

申请号：US13126620

申请日：2009-10-26

申请人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Anthony J. Roecker ,  John D. Schreier

发明人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Anthony J. Roecker ,  John D. Schreier

IPC分类号： A61K31/497 ,  C07D213/56 ,  A61K31/4418 ,  C07D401/14 ,  A61K31/444 ,  C07D401/10 ,  C07D231/10 ,  A61K31/415 ,  A61K31/4439 ,  A61P3/04 ,  A61P25/00

CPC分类号： A61K31/437 ,  A61K31/4439 ,  C07D213/56 ,  C07D213/61 ,  C07D231/12 ,  C07D241/12 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14

摘要： The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的2,5-二取代的苯基甲酰胺化合物，其可用于治疗或预防其中涉及食欲肽受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

公开(公告)号：US08685370B2

公开(公告)日：2014-04-01

申请号：US12922594

申请日：2009-03-13

申请人： Milind Rajopadhye ,  Guojie Ho ,  Bohumil Bednar ,  Le T. Duong ,  Paul J. Coleman

发明人： Milind Rajopadhye ,  Guojie Ho ,  Bohumil Bednar ,  Le T. Duong ,  Paul J. Coleman

IPC分类号： A61K49/00

CPC分类号： A61K49/04 ,  A61K47/65 ,  A61K49/0002 ,  A61K49/0032 ,  A61K49/0052 ,  A61K49/0056 ,  A61K49/0065 ,  A61K49/085 ,  A61K49/10 ,  A61K49/1839 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0497 ,  B82Y5/00 ,  C09B23/0008 ,  C09B23/083 ,  C09B23/086 ,  G01N33/574

摘要： The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

摘要翻译： 本发明提供靶向整联蛋白的药物家族，其可以用作成像剂和/或治疗剂。 这些药剂可用于影像受试者的血管生成，炎症或其他生理过程。