公开(公告)号：US20100004237A1

公开(公告)日：2010-01-07

申请号：US12462302

申请日：2009-07-31

申请人： Timothy D. Machakewski ,  Cynthia M. Shafer ,  Christopher McBride ,  William Antonios-McCrea ,  Brandon M. Doughan ,  Barry H. Levine ,  Yi Xia ,  Maureen McKenna ,  X. Michael Wang ,  Kris Mendenhall ,  Yasheen Zhou ,  Baoqing Gong ,  Dan Gu ,  John Dolan ,  John Tulinsky ,  Kristin Brinner ,  Zhenhai Gao ,  Daniel Poon ,  Paul Barsanti ,  Xiaodong Lin ,  Abran Costales ,  Alice Rico ,  Nathan Brammeier ,  Teresa Pick ,  Paul A. Renhowe

发明人： Timothy D. Machakewski ,  Cynthia M. Shafer ,  Christopher McBride ,  William Antonios-McCrea ,  Brandon M. Doughan ,  Barry H. Levine ,  Yi Xia ,  Maureen McKenna ,  X. Michael Wang ,  Kris Mendenhall ,  Yasheen Zhou ,  Baoqing Gong ,  Dan Gu ,  John Dolan ,  John Tulinsky ,  Kristin Brinner ,  Zhenhai Gao ,  Daniel Poon ,  Paul Barsanti ,  Xiaodong Lin ,  Abran Costales ,  Alice Rico ,  Nathan Brammeier ,  Teresa Pick ,  Paul A. Renhowe

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/519

CPC分类号： C07D211/86 ,  C07D471/04

摘要： Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

摘要翻译： 公开了2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物，其立体异构体，互变异构体，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物的组合物，单独或与至少一种额外的 治疗剂。 还公开了将2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物单独使用或与至少一种另外的治疗剂组合使用的方法，用于预防 或治疗细胞增殖，病毒，自身免疫，心血管和中枢神经系统疾病。

公开(公告)号：US07071216B2

公开(公告)日：2006-07-04

申请号：US10405945

申请日：2003-03-31

申请人： Paul A. Renhowe ,  Savithri Ramurthy ,  Payman Amiri ,  Barry Haskell Levine ,  Daniel J. Poon ,  Sharadha Subramanian ,  Leonard Sung ,  Wendy Fantl ,  Teresa Hansen ,  Christopher McBride ,  Cynthia M. Shafer

发明人： Paul A. Renhowe ,  Savithri Ramurthy ,  Payman Amiri ,  Barry Haskell Levine ,  Daniel J. Poon ,  Sharadha Subramanian ,  Leonard Sung ,  Wendy Fantl ,  Teresa Hansen ,  Christopher McBride ,  Cynthia M. Shafer

IPC分类号： A61K31/4184 ,  A61K31/4439 ,  C07D235/30 ,  C07D401/12

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02

摘要： New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。 新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

公开(公告)号：US06774237B2

公开(公告)日：2004-08-10

申请号：US10284017

申请日：2002-10-30

申请人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Elisa Jazan

发明人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Elisa Jazan

IPC分类号： C07D21516

CPC分类号： C07D409/04 ,  A61K31/19 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/513 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  C07D471/04 ,  A61K2300/00

摘要： Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

摘要翻译： 提供具有式I和II的有机化合物，其中变量具有本文所述的值。药物制剂包括有机化合物或其药学上可接受的盐和药学上可接受的载体，并且可以通过将有机化合物或其药学上可接受的盐 有机化合物与载体和水。 治疗患者的方法包括向有需要的患者施用本发明的药物制剂。

公开(公告)号：US08415382B2

公开(公告)日：2013-04-09

申请号：US12205028

申请日：2008-09-05

申请人： Abran Costales ,  Teresa Hansen ,  Barry H. Levine ,  Christopher McBride ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia M. Shafer ,  Sharadha Subramanian ,  Joelle Verhagen

发明人： Abran Costales ,  Teresa Hansen ,  Barry H. Levine ,  Christopher McBride ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia M. Shafer ,  Sharadha Subramanian ,  Joelle Verhagen

IPC分类号： A61K31/44

CPC分类号： C07D401/12 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C04B35/632 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯唑化合物，抑制人或动物受试者中的Raf激酶活性的组合物和方法。 新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

公开(公告)号：US20100184754A1

公开(公告)日：2010-07-22

申请号：US12651612

申请日：2010-01-04

申请人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, JR. ,  Christopher McBride ,  Elisa Jazan

发明人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, JR. ,  Christopher McBride ,  Elisa Jazan

IPC分类号： A61K31/541 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/04

CPC分类号： C07D471/04 ,  A61K31/19 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/541 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  A61K2300/00

摘要： Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

摘要翻译： 提供具有式I和II的有机化合物，其中变量具有本文所述的值。 药物制剂包括有机化合物或其药学上可接受的盐和药学上可接受的载体，并且可以通过将有机化合物的有机化合物或药学上可接受的盐与载体和水混合来制备。 治疗患者的方法包括向有需要的患者施用本发明的药物制剂。

公开(公告)号：US07064215B2

公开(公告)日：2006-06-20

申请号：US10187967

申请日：2002-07-02

申请人： Paul A. Renhowe ,  Cynthia M. Shafer ,  Christopher McBride ,  Joel Benjamin Silver ,  Sabina Pecchi ,  Timothy D. Machajewski ,  William R. McCrea, Jr. ,  Daniel J. Poon ,  Teresa Thomas

发明人： Paul A. Renhowe ,  Cynthia M. Shafer ,  Christopher McBride ,  Joel Benjamin Silver ,  Sabina Pecchi ,  Timothy D. Machajewski ,  William R. McCrea, Jr. ,  Daniel J. Poon ,  Teresa Thomas

IPC分类号： C07D271/02 ,  C07D285/14

CPC分类号： C07D403/04

摘要： Organic compounds having the structure I are provided where the variables have the values described herein. Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compound or a pharmaceutically acceptable salt of the organic compound with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation or medicament according to the invention to a patient in need thereof.

公开(公告)号：US06800760B2

公开(公告)日：2004-10-05

申请号：US10613411

申请日：2003-07-03

申请人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Elisa Jazan

发明人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Elisa Jazan

IPC分类号： C07D21516

CPC分类号： C07D409/04 ,  A61K31/19 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/513 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  C07D471/04 ,  A61K2300/00

摘要： Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

公开(公告)号：US06762194B2

公开(公告)日：2004-07-13

申请号：US10387355

申请日：2003-03-12

申请人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Eliza Jazan

发明人： Paul A. Renhowe ,  Sabina Pecchi ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Clarke Taylor ,  William R. McCrea, Jr. ,  Christopher McBride ,  Eliza Jazan

IPC分类号： A61K3147

CPC分类号： C07D409/04 ,  A61K31/19 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/513 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  C07D471/04 ,  A61K2300/00

摘要： Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

公开(公告)号：US07671059B2

公开(公告)日：2010-03-02

申请号：US11541462

申请日：2006-09-28

申请人： Timothy D. Machajewski ,  Cynthia M. Shafer ,  Christopher McBride ,  William Antonios-McCrea ,  Brandon M. Doughan ,  Barry H. Levine ,  Yi Xia ,  Maureen McKenna ,  X. Michael Wang ,  Kris Mendenhall ,  Yasheen Zhou ,  Kristin Brinner ,  Zhenhai Gao ,  Daniel Poon ,  Paul Barsanti ,  Xiaodong Lin ,  Abran Costales ,  Alice Rico ,  Nathan Brammeier ,  Teresa Pick ,  Paul A. Renhowe

发明人： Timothy D. Machajewski ,  Cynthia M. Shafer ,  Christopher McBride ,  William Antonios-McCrea ,  Brandon M. Doughan ,  Barry H. Levine ,  Yi Xia ,  Maureen McKenna ,  X. Michael Wang ,  Kris Mendenhall ,  Yasheen Zhou ,  Kristin Brinner ,  Zhenhai Gao ,  Daniel Poon ,  Paul Barsanti ,  Xiaodong Lin ,  Abran Costales ,  Alice Rico ,  Nathan Brammeier ,  Teresa Pick ,  Paul A. Renhowe

IPC分类号： A61K31/519 ,  A61K31/5355 ,  C07D471/04 ,  C07D487/04 ,  C07D413/06 ,  A61P35/00

CPC分类号： C07D211/86 ,  C07D471/04

摘要： Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

摘要翻译： 公开了2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物，其立体异构体，互变异构体，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物的组合物，单独或与至少一种额外的 治疗剂。 还公开了将2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物单独使用或与至少一种另外的治疗剂组合使用的方法，用于预防 或治疗细胞增殖，病毒，自身免疫，心血管和中枢神经系统疾病。

公开(公告)号：US20090281100A1

公开(公告)日：2009-11-12

申请号：US12317493

申请日：2008-12-23

申请人： Paul A. Barsanti ,  Dirksen Bussiere ,  Stephen D. Harrison ,  Carla C. Heise ,  Johanna M. Jansen ,  Elisa Jazan ,  Timothy D. Machajewski ,  Christopher McBride ,  William R. McCrea, JR. ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia M. Shafer ,  Joel B. Silver ,  Allan S. Wagman ,  Marion Wiesmann ,  Kelly Wayman

发明人： Paul A. Barsanti ,  Dirksen Bussiere ,  Stephen D. Harrison ,  Carla C. Heise ,  Johanna M. Jansen ,  Elisa Jazan ,  Timothy D. Machajewski ,  Christopher McBride ,  William R. McCrea, JR. ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia M. Shafer ,  Joel B. Silver ,  Allan S. Wagman ,  Marion Wiesmann ,  Kelly Wayman

IPC分类号： A61K31/5377 ,  A61K31/497 ,  A61K31/4709

CPC分类号： C07D401/04 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/52 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D453/02 ,  C07D453/06 ,  C07D471/04

摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.

摘要翻译： 提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。 具有结构I和IB的化合物具有以下结构并具有本文所述的变量。 这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。