公开(公告)号：US09145373B2

公开(公告)日：2015-09-29

申请号：US13963822

申请日：2013-08-09

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

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

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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：US08883785B2

公开(公告)日：2014-11-11

申请号：US13575019

申请日：2011-01-20

Applicant: Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Dirk Winkler ,  Frederick Brookfield ,  Paula C. De Aguiar Pena

Inventor： Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Dirk Winkler ,  Frederick Brookfield ,  Paula C. De Aguiar Pena

IPC: C07D403/04 ,  C07D413/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  C07D401/04 ,  C07D417/04

CPC classification number: C07D403/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

Abstract: 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：US20140329795A1

公开(公告)日：2014-11-06

申请号：US14241699

申请日：2012-08-28

Applicant: Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson ,  Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Ignacio Munoz

Inventor： Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson ,  Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Ignacio Munoz

IPC: C07D239/28 ,  C07D401/12 ,  C07D403/06 ,  C07D417/12 ,  C07D239/42 ,  C07D403/12 ,  C07D471/04 ,  C07D405/12 ,  C07D487/04 ,  C07D401/04 ,  C07D413/12

CPC classification number: C07D239/28 ,  A61K31/506 ,  C07D239/42 ,  C07D239/52 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

Abstract: 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.

Abstract translation: 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

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

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

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

CPC classification number: 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

Abstract: 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：US20130116216A1

公开(公告)日：2013-05-09

申请号：US13509783

申请日：2010-11-12

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

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

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

CPC classification number: 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

Abstract: 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

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

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

IPC: 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 classification number: C07D205/04 ,  C07D207/48 ,  C07D211/96 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

Abstract: 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.

Abstract translation: 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：US20110230428A1

公开(公告)日：2011-09-22

申请号：US13054931

申请日：2009-07-22

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

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

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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

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

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

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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：US07897619B2

公开(公告)日：2011-03-01

申请号：US12218754

申请日：2008-07-16

Applicant: Qingping Zeng ,  Dawei Zhang ,  Guomin Yao ,  George E. Wohlhieter ,  Xianghong Wang ,  James Rider ,  Andreas Reichelt ,  Holger Monenschein ,  Fang-Tsao Hong ,  James R. Falsey ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

Inventor： Qingping Zeng ,  Dawei Zhang ,  Guomin Yao ,  George E. Wohlhieter ,  Xianghong Wang ,  James Rider ,  Andreas Reichelt ,  Holger Monenschein ,  Fang-Tsao Hong ,  James R. Falsey ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

IPC: A61K31/47 ,  A61K31/416 ,  C07D217/02 ,  C07D231/56

CPC classification number: C07D413/04 ,  C07D263/48 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D417/04

Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及用于治疗由蛋白激酶B（PKB）介导的疾病的式I的杂环化合物及其组合物，其中变量具有本文提供的定义。 本发明还涉及这些化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病状态中的治疗用途。

公开(公告)号：US07858623B2

公开(公告)日：2010-12-28

申请号：US11412302

申请日：2006-04-26

Applicant: Tae-Seong Kim ,  Shon Booker ,  Celia Dominguez ,  Jean-Christophe Harmange

Inventor： Tae-Seong Kim ,  Shon Booker ,  Celia Dominguez ,  Jean-Christophe Harmange

IPC: A61K31/535 ,  C07D413/12

CPC classification number: C07D413/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。