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公开(公告)号：US07396846B2
公开(公告)日：2008-07-08
申请号：US10510393
申请日：2003-03-31
IPC分类号： A61K31/40 , A61K31/425 , C07D275/02 , C07D207/18
CPC分类号： C07K5/0606 , A61K38/00 , C07K5/06026 , C07K5/06034 , C07K5/06191
摘要： This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
摘要翻译： 本发明涉及可用于调节哺乳动物内源性生长激素水平的新化合物。 本发明还涉及用于合成所述化合物的新中间体，以及在这些合成中使用的新方法。 还包括治疗哺乳动物的方法，其包括施用所述化合物。
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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。
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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.
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公开(公告)号：US07405305B2
公开(公告)日：2008-07-29
申请号：US10506029
申请日：2003-03-05
申请人： Pamela Ann Albaugh , Jochen Ammenn , Timothy Paul Burkholder , Joshua Ryan Clayton , Scott Eugene Conner , Brian Eugene Cunningham , Thomas Albert Engler , Kelly Wayne Furness , James Robert Henry , Sushant Malhotra , Mark Joseph Tebbe , Guoxin Zhu , YiHong Li , Brian Raymond Berridge , Charles Edward Ruegg , John Morris Sullivan
发明人： Pamela Ann Albaugh , Jochen Ammenn , Timothy Paul Burkholder , Joshua Ryan Clayton , Scott Eugene Conner , Brian Eugene Cunningham , Thomas Albert Engler , Kelly Wayne Furness , James Robert Henry , Sushant Malhotra , Mark Joseph Tebbe , Guoxin Zhu , YiHong Li , Brian Raymond Berridge , Charles Edward Ruegg , John Morris Sullivan
IPC分类号： C07D209/12 , C07D207/24 , C07D211/06
CPC分类号： C07D451/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D471/04 , C07D491/04
摘要： The present invention provides kinase inhibitors of Formula (I)
摘要翻译： 本发明提供式（I）的激酶抑制剂，
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公开(公告)号：US5891874A
公开(公告)日：1999-04-06
申请号：US868760
申请日：1997-06-04
申请人： Joseph Matthew Colacino , Beverly Ann Heinz , Louis Nickolaus Jungheim , Shawn Christopher Miller , Wayne Alfred Spitzer , Joseph Chiou-chung Tang , Mark Joseph Tebbe , Frantz Victor
发明人： Joseph Matthew Colacino , Beverly Ann Heinz , Louis Nickolaus Jungheim , Shawn Christopher Miller , Wayne Alfred Spitzer , Joseph Chiou-chung Tang , Mark Joseph Tebbe , Frantz Victor
IPC分类号： A61K31/415 , C07D235/06 , C07D235/30 , C07D409/12 , A61K31/535 , A61K31/445 , C07D403/02 , C07D417/00
CPC分类号： C07D409/12 , C07D235/30
摘要： A series of benzimidazole compounds having the following general structure are provided which inhibit the growth of picornaviruses (e.g., rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus) and flaviviruses (e.g., hepatitis C and bovine diarrheal virus). ##STR1## A method for inhibiting picornaviruses and flaviviruses is also provided which includes administering to a host an effective amount of the inventive benzimidazole compounds.
摘要翻译： 提供了一系列具有以下一般结构的苯并咪唑化合物，其抑制小核糖核酸病毒（例如，鼻病毒，肠病毒，脊髓灰质炎病毒，A组和B组的柯萨奇病毒，回波病毒和Mengo病毒）和黄病毒（例如，丙型肝炎和牛 腹泻病毒）。 还提供了一种抑制微小核糖核酸病毒和黄病毒的方法，其包括向宿主施用有效量的本发明苯并咪唑化合物。
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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。
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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.
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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。
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公开(公告)号：US5821242A
公开(公告)日：1998-10-13
申请号：US868638
申请日：1997-06-04
申请人： Joseph Matthew Colacino , Beverly Ann Heinz , Louis Nickolaus Jungheim , Shawn Christopher Miller , Wayne Alfred Spitzer , Joseph Chiou-chung Tang , Mark Joseph Tebbe , Frantz Victor
发明人： Joseph Matthew Colacino , Beverly Ann Heinz , Louis Nickolaus Jungheim , Shawn Christopher Miller , Wayne Alfred Spitzer , Joseph Chiou-chung Tang , Mark Joseph Tebbe , Frantz Victor
IPC分类号： A61K31/415 , A61K31/4184 , A61P31/12 , C07D235/30 , C07D235/22 , C07D235/08
CPC分类号： C07D235/30
摘要： The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as hepatitis C and bovine diarrheal virus.
摘要翻译： 本申请提供了一系列苯并咪唑化合物，其抑制微小核糖核酸病毒，例如鼻病毒，肠病毒，脊髓灰质炎病毒，A组和B组的柯萨奇病毒，回波病毒和孟戈病毒以及黄病毒如丙型肝炎和牛腹泻病毒的生长。
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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。
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