公开(公告)号：US08252923B2

公开(公告)日：2012-08-28

申请号：US12231982

申请日：2008-09-08

申请人： Robert Edward Babine ,  Shu-Hui Chen ,  Jason Eric Lamar ,  Nancy June Snyder ,  Xicheng Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Ivan Collado ,  Cristina Garcia-Paredes ,  Raymond Samuel Parker, III ,  Ling Jin ,  Deqi Guo ,  John Irvin Glass

发明人： Robert Edward Babine ,  Shu-Hui Chen ,  Jason Eric Lamar ,  Nancy June Snyder ,  Xicheng Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Ivan Collado ,  Cristina Garcia-Paredes ,  Raymond Samuel Parker, III ,  Ling Jin ,  Deqi Guo ,  John Irvin Glass

IPC分类号： C07D265/34 ,  C07D241/08 ,  C07D275/06 ,  C07D417/02 ,  C07D233/32 ,  C07D403/02 ,  C07D207/08 ,  C07D493/14 ,  C07C229/00

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。 本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

公开(公告)号：US20120064034A1

公开(公告)日：2012-03-15

申请号：US13293812

申请日：2011-11-10

申请人： ROBERT EDWARD BABINE ,  SHU HUI CHEN ,  IVAN COLLADO ,  CRISTINA GARCIA-PAREDES ,  JOHN IRVIN GLASS ,  DEQI GUO ,  LING JIN ,  JASON ERIC LAMAR ,  RAYMOND SAMUEL PARKER, III ,  NANCY JUNE SNYDER ,  XICHENG DAVID SUN ,  YVONNE YEE MAI YIP ,  Q. MAY WANG ,  FRANTZ VICTOR ,  MARK JOSEPH TEBBE ,  ROBERT B. PERNI ,  LUC FARMER

发明人： ROBERT EDWARD BABINE ,  SHU HUI CHEN ,  IVAN COLLADO ,  CRISTINA GARCIA-PAREDES ,  JOHN IRVIN GLASS ,  DEQI GUO ,  LING JIN ,  JASON ERIC LAMAR ,  RAYMOND SAMUEL PARKER, III ,  NANCY JUNE SNYDER ,  XICHENG DAVID SUN ,  YVONNE YEE MAI YIP ,  Q. MAY WANG ,  FRANTZ VICTOR ,  MARK JOSEPH TEBBE ,  ROBERT B. PERNI ,  LUC FARMER

IPC分类号： A61K38/08 ,  C07K5/037 ,  A61K38/21 ,  C12N5/071 ,  C07C229/42 ,  C07D209/52 ,  C12N9/99 ,  C07K7/06 ,  A61K38/20

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

公开(公告)号：US20100137583A1

公开(公告)日：2010-06-03

申请号：US12231982

申请日：2008-09-08

申请人： Robert Edward Babine ,  Shu-Hui Chen ,  Jason Eric Lamar ,  Nancy June Snyder ,  Xicheng Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Ivan Collado ,  Cristina Garcia-Paredes ,  Raymond Samuel Parker, III ,  Ling Jin ,  Deqi Guo ,  John Irvin Glass

发明人： Robert Edward Babine ,  Shu-Hui Chen ,  Jason Eric Lamar ,  Nancy June Snyder ,  Xicheng Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Ivan Collado ,  Cristina Garcia-Paredes ,  Raymond Samuel Parker, III ,  Ling Jin ,  Deqi Guo ,  John Irvin Glass

IPC分类号： C07D265/34 ,  C07D265/32 ,  C07D241/08 ,  C07D275/06 ,  C07D417/02 ,  C07D233/32 ,  C07D403/02 ,  C07D207/08 ,  C07D493/14 ,  C07C229/00

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。 本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

公开(公告)号：US20120282219A1

公开(公告)日：2012-11-08

申请号：US13541436

申请日：2012-07-03

申请人： ROBERT EDWARD BABINE ,  SHU HUI CHEN ,  IVAN COLLADO ,  CRISTINA GARCIA-PAREDES ,  JOHN IRVIN GLASS ,  DEQI GUO ,  LING JIN ,  JASON ERIC LAMAR ,  RAYMOND SAMUEL PARKER, III ,  NANCY JUNE SNYDER ,  XICHENG DAVID SUN ,  MARK JOSEPH TEBBE ,  FRANTZ VICTOR ,  Q. MAY WANG ,  YVONNE YEE MAI YIP ,  ROBERT B. PERNI ,  LUC FARMER

发明人： ROBERT EDWARD BABINE ,  SHU HUI CHEN ,  IVAN COLLADO ,  CRISTINA GARCIA-PAREDES ,  JOHN IRVIN GLASS ,  DEQI GUO ,  LING JIN ,  JASON ERIC LAMAR ,  RAYMOND SAMUEL PARKER, III ,  NANCY JUNE SNYDER ,  XICHENG DAVID SUN ,  MARK JOSEPH TEBBE ,  FRANTZ VICTOR ,  Q. MAY WANG ,  YVONNE YEE MAI YIP ,  ROBERT B. PERNI ,  LUC FARMER

IPC分类号： A61K38/07 ,  C07D209/52 ,  C12N5/073 ,  A61P31/14 ,  A61K38/20 ,  C12N9/99 ,  C07K5/117 ,  A61K38/21

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备包括对中间体的新的立体选择性方法。 本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

公开(公告)号：US07820671B2

公开(公告)日：2010-10-26

申请号：US10344112

申请日：2001-08-31

申请人： Robert Edward Babine ,  Shu Hui Chen ,  Ivan Collado ,  Cristina Garcia-Paredes ,  John Irvin Glass ,  Deqi Guo ,  Ling Jin ,  Jason Eric Lamar ,  Raymond Samuel Parker, III ,  Nancy June Snyder ,  Xicheng David Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Robert B. Perni ,  Luc Farmer

发明人： Robert Edward Babine ,  Shu Hui Chen ,  Ivan Collado ,  Cristina Garcia-Paredes ,  John Irvin Glass ,  Deqi Guo ,  Ling Jin ,  Jason Eric Lamar ,  Raymond Samuel Parker, III ,  Nancy June Snyder ,  Xicheng David Sun ,  Mark Joseph Tebbe ,  Frantz Victor ,  Q. May Wang ,  Yvonne Yee Mai Yip ,  Robert B. Perni ,  Luc Farmer

IPC分类号： A61K31/497 ,  C07D241/02

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

公开(公告)号：US08529882B2

公开(公告)日：2013-09-10

申请号：US13541436

申请日：2012-07-03

申请人： Robert Edward Babine ,  Shu Hui Chen ,  Ivan Collado ,  Cristina Garcia-Paredes ,  John Irvin Glass ,  Ling Jin ,  Jason Eric Lamar ,  Raymond Samuel Parker, III ,  Nancy June Snyder ,  Xicheng David Sun ,  Deqi Guo ,  Yvonne Yee Mai Yip ,  Q. May Wang ,  Frantz Victor ,  Mark Joseph Tebbe ,  Robert B. Perni ,  Luc Farmer

发明人： Robert Edward Babine ,  Shu Hui Chen ,  Ivan Collado ,  Cristina Garcia-Paredes ,  John Irvin Glass ,  Ling Jin ,  Jason Eric Lamar ,  Raymond Samuel Parker, III ,  Nancy June Snyder ,  Xicheng David Sun ,  Deqi Guo ,  Yvonne Yee Mai Yip ,  Q. May Wang ,  Frantz Victor ,  Mark Joseph Tebbe ,  Robert B. Perni ,  Luc Farmer

IPC分类号： A61K38/07 ,  A61K38/20 ,  A61K38/21 ,  C07D209/52 ,  C12N5/073 ,  C12N9/99 ,  A61P31/14 ,  C07K5/117

CPC分类号： C07K7/02 ,  A61K38/07 ,  A61K38/08 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K45/06 ,  C07D209/02 ,  C07D209/52 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06 ,  C07K14/005 ,  C12N2770/24222 ,  Y02P20/55 ,  A61K2300/00

摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地说，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备包括对中间体的新的立体选择性方法。 本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

公开(公告)号：US07666879B2

公开(公告)日：2010-02-23

申请号：US11816416

申请日：2006-02-23

申请人： David Anthony Barda ,  Timothy Paul Burkholder ,  Joshua Ryan Clayton ,  Yan Hao ,  James Robert Henry ,  John Monte Knobeloch ,  Johnathan Alexander McLean ,  David Mendel ,  Mark Edward Rempala ,  Zhao-Qing Wang ,  Yvonne Yee Mai Yip ,  Boyu Zhong

发明人： David Anthony Barda ,  Timothy Paul Burkholder ,  Joshua Ryan Clayton ,  Yan Hao ,  James Robert Henry ,  John Monte Knobeloch ,  Johnathan Alexander McLean ,  David Mendel ,  Mark Edward Rempala ,  Zhao-Qing Wang ,  Yvonne Yee Mai Yip ,  Boyu Zhong

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  C07D401/00

CPC分类号： C07D471/04

摘要： The present invention provides compounds that are inhibitors of VEGF-R2 of the formula: (I) and methods of using these compounds.

摘要翻译： 本发明提供了下式所示的VEGF-R2抑制剂的化合物：（I）和使用这些化合物的方法。