公开(公告)号：US08946197B2

公开(公告)日：2015-02-03

申请号：US13509783

申请日：2010-11-12

申请人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

发明人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

IPC分类号： A61K31/635 ,  C07C311/46 ,  C07D211/34 ,  C07D211/54 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D215/38 ,  C07D217/14 ,  C07D217/22 ,  C07D239/42 ,  C07D263/58 ,  C07D277/42 ,  C07D295/205 ,  C07D295/26 ,  C07D307/52 ,  C07D401/04 ,  C07D487/04 ,  C07D495/04

CPC分类号： C07C311/46 ,  C07C2601/14 ,  C07D211/34 ,  C07D211/54 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D215/38 ,  C07D217/14 ,  C07D217/22 ,  C07D239/42 ,  C07D263/58 ,  C07D277/42 ,  C07D295/205 ,  C07D295/26 ,  C07D307/52 ,  C07D401/04 ,  C07D487/04 ,  C07D495/04

摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

摘要翻译： 本文提供了某些化合物和药学上可接受的盐。 还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。 描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。 这些疾病状态包括神经变性疾病如亨廷顿病。 还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

公开(公告)号：US08889716B2

公开(公告)日：2014-11-18

申请号：US13466018

申请日：2012-05-07

申请人： Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas MacDonald ,  John Wityak

发明人： Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas MacDonald ,  John Wityak

IPC分类号： A61K31/445 ,  C07D211/96 ,  C07D409/12 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07D207/48 ,  C07D401/14 ,  C07D401/12

CPC分类号： C07D205/04 ,  C07D207/48 ,  C07D211/96 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

摘要翻译： 本文提供了某些化合物和药学上可接受的盐。 还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。 描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。 这些疾病状态包括神经变性疾病如亨廷顿病。 还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

公开(公告)号：US20130116216A1

公开(公告)日：2013-05-09

申请号：US13509783

申请日：2010-11-12

申请人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

发明人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

IPC分类号： A61K31/55 ,  A61K31/496 ,  C07D401/02 ,  A61K31/45 ,  C07D413/02 ,  C07D403/04 ,  A61K31/5377 ,  A61K31/495

CPC分类号： C07C311/46 ,  C07C2601/14 ,  C07D211/34 ,  C07D211/54 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D215/38 ,  C07D217/14 ,  C07D217/22 ,  C07D239/42 ,  C07D263/58 ,  C07D277/42 ,  C07D295/205 ,  C07D295/26 ,  C07D307/52 ,  C07D401/04 ,  C07D487/04 ,  C07D495/04

摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

公开(公告)号：US20120302539A1

公开(公告)日：2012-11-29

申请号：US13466018

申请日：2012-05-07

申请人： Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas Macdonald ,  John Wityak

发明人： Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas Macdonald ,  John Wityak

IPC分类号： A61K31/4468 ,  C07D405/12 ,  A61K31/453 ,  C07D207/48 ,  A61K31/40 ,  A61K31/4525 ,  C07D409/12 ,  A61K31/4535 ,  C07D401/12 ,  A61K31/454 ,  C07D405/14 ,  C07D205/04 ,  A61K31/397 ,  A61K31/4545 ,  C07D401/14 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  A61P25/28 ,  A61P1/16 ,  A61P13/12 ,  A61P25/00 ,  A61P35/04 ,  A61P35/02 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P19/02 ,  A61P17/06 ,  A61P9/00 ,  A61P9/10 ,  A61P3/10 ,  A61P17/10 ,  A61P27/12 ,  A61P27/10 ,  A61P21/00 ,  A61P17/02 ,  A61P1/00 ,  A61P25/14 ,  A61P25/16 ,  C07D211/96

CPC分类号： C07D205/04 ,  C07D207/48 ,  C07D211/96 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

摘要翻译： 本文提供了某些化合物和药学上可接受的盐。 还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。 描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。 这些疾病状态包括神经变性疾病如亨廷顿病。 还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

公开(公告)号：US08691824B2

公开(公告)日：2014-04-08

申请号：US13056919

申请日：2009-08-03

申请人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： A61K31/497

CPC分类号： A61K31/42 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

摘要翻译： 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：US20130331370A1

公开(公告)日：2013-12-12

申请号：US13963822

申请日：2013-08-09

申请人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： C07D239/52 ,  C07D403/12 ,  C07D401/12 ,  C07D239/38 ,  C07D239/69

CPC分类号： C07D239/52 ,  A61K31/505 ,  A61K31/506 ,  C07D213/79 ,  C07D213/81 ,  C07D239/28 ,  C07D239/38 ,  C07D239/42 ,  C07D239/69 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US20120329812A1

公开(公告)日：2012-12-27

申请号：US13056919

申请日：2009-08-03

申请人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： A61K31/42 ,  C07D413/12 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/08 ,  A61K31/437 ,  A61K31/422 ,  C07D413/06 ,  A61P25/28 ,  A61P25/16 ,  C07D261/04 ,  C07D471/04

CPC分类号： A61K31/42 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

摘要翻译： 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：US09145373B2

公开(公告)日：2015-09-29

申请号：US13963822

申请日：2013-08-09

申请人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： A61K31/506 ,  C07D239/52 ,  C07D213/79 ,  C07D213/81 ,  C07D239/28 ,  C07D239/42 ,  C07D239/69 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D239/38 ,  C07D403/12 ,  A61K31/505

CPC分类号： C07D239/52 ,  A61K31/505 ,  A61K31/506 ,  C07D213/79 ,  C07D213/81 ,  C07D239/28 ,  C07D239/38 ,  C07D239/42 ,  C07D239/69 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

摘要翻译： 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：US08536186B2

公开(公告)日：2013-09-17

申请号：US13056305

申请日：2009-08-04

申请人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/52 ,  A61K31/505 ,  A61K31/506 ,  C07D213/79 ,  C07D213/81 ,  C07D239/28 ,  C07D239/38 ,  C07D239/42 ,  C07D239/69 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US20110230428A1

公开(公告)日：2011-09-22

申请号：US13054931

申请日：2009-07-22

申请人： John Wityak ,  Leticia M. Toledo-sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

发明人： John Wityak ,  Leticia M. Toledo-sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC分类号： A61K31/7024 ,  C07D271/06 ,  A61K31/4245 ,  C07D233/64 ,  A61K31/4164 ,  C07D257/04 ,  A61K31/41 ,  C07C251/38 ,  A61K31/15 ,  C07D207/50 ,  A61K31/40 ,  C07C255/64 ,  A61K31/277 ,  C07D471/04 ,  A61K31/437 ,  C07C311/05 ,  A61K31/18 ,  A61K31/192 ,  C07D295/13 ,  A61K31/5375 ,  C07H13/04 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  A61P25/08

CPC分类号： C07C311/05 ,  C07C251/48 ,  C07C251/58 ,  C07C255/61 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D211/46 ,  C07D211/56 ,  C07D213/53 ,  C07D213/71 ,  C07D213/75 ,  C07D231/40 ,  C07D233/61 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D261/14 ,  C07D271/06 ,  C07D285/125 ,  C07D309/10 ,  C07D471/04 ,  C07H15/18

摘要： Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

摘要翻译： 本文提供了某些化学实体。 包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。