公开(公告)号：US20100143341A1

公开(公告)日：2010-06-10

申请号：US11993433

申请日：2006-06-21

申请人： Steven Taylor ,  Stephen Murfin ,  Thomas Stephen Coulter ,  Stefan Jakel ,  Babette Aicher ,  Arndt-Rene Kelter ,  Joachim Kraemer ,  Christian Kirchhoff ,  Andreas Scheel ,  Julian Woelcke

发明人： Steven Taylor ,  Stephen Murfin ,  Thomas Stephen Coulter ,  Stefan Jakel ,  Babette Aicher ,  Arndt-Rene Kelter ,  Joachim Kraemer ,  Christian Kirchhoff ,  Andreas Scheel ,  Julian Woelcke

IPC分类号： A61K31/519 ,  C07D495/04 ,  A61K31/5377 ,  A61K38/28 ,  A61K31/60 ,  A61K39/395 ,  A61K31/704 ,  A61P3/00

CPC分类号： C07D495/04

摘要： The present invention relates to novel pharmaceutical compositions of general formula (I) comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

摘要翻译： 本发明涉及包含噻吩并嘧啶化合物的通式（I）的新型药物组合物。 此外，本发明涉及本发明的噻吩并嘧啶化合物用于生产药物组合物用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a）激酶活性的疾病的用途 或Mnk2b）和/或其变体。

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。

公开(公告)号：US20110183957A1

公开(公告)日：2011-07-28

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： A61K31/506 ,  C07D239/28 ,  C07D239/42 ,  C07D401/12 ,  C07D239/69 ,  C07D401/04 ,  C07D413/06 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04 ,  C07D239/38 ,  C07D417/12 ,  C07D403/12 ,  C07D413/12 ,  C07D213/79 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16

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：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。