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1. 发明专利

JP2010090150A Inhibitor of serine protease, particularly hcv ns3-ns4a protease incorporating condensed ring system 审中-公开
标题翻译：丝氨酸蛋白酶抑制剂，特异性HCV NS3-NS4A蛋白激酶融合环系统
公开(公告)号：JP2010090150A
公开(公告)日：2010-04-22
申请号：JP2009279701
申请日：2009-12-09
申请人： John H Van Drie , Robert B Pernie , Janos Pitlik , Vertex Pharmaceut Inc , ジョン・エイチ・バン・ドリーJohn H. Van Drie , バーテックスファーマシューティカルズインコーポレイテッドVertex Pharmaceuticals Incorporated , ヤーノシュ・ピトリクJanos Pitlik , ロバート・ビー・パーニRobert B. Perni
发明人： PERNIE ROBERT B , PITLIK JANOS , DRIE JOHN H VAN , FARMER LUC J
IPC分类号： C07K5/107 , C12N9/99 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P43/00 , C07D403/12 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/02 , C07K7/06
CPC分类号： C07D491/147 , A61K31/407 , A61K38/00 , A61K45/06 , C07D403/12 , C07K5/06191 , C07K5/0827 , C07K5/101 , C07K5/1027 , C07K7/02 , C07K7/06
摘要： PROBLEM TO BE SOLVED: To provide effective anti-HCV therapies. SOLUTION: Peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease are represented by the formula (1). They act as antiviral agents by interfering with the life cycle of the hepatitis C virus. Also provided are compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection, and methods of treating an HCV infection in a patient by administering a composition comprising a compound. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供有效的抗HCV疗法。解决方案：抑制丝氨酸蛋白酶活性的肽模拟化合物，特别是丙型肝炎病毒NS3-NS4A蛋白酶的活性由式（1）表示。它们通过干扰丙型肝炎病毒的生命周期作为抗病毒剂。还提供了包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物，以及通过施用包含化合物的组合物来治疗患者HCV感染的方法。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP4460294B2 Incorporating a fused ring system, serine proteases, especially c hepatitis ns3-NS4A protease inhibitors 有权
公开(公告)号：JP4460294B2
公开(公告)日：2010-05-12
申请号：JP2003537627
申请日：2002-10-24
申请人：ジョン・エイチ・バン・ドリーJohn H. Van Drie , バーテックスファーマシューティカルズインコーポレイテッドVertex Pharmaceuticals Incorporated , ヤーノシュ・ピトリクJanos Pitlik , ロバート・ビー・パーニRobert B. Perni
发明人：ジョン・エイチ・バン・ドリー , ヤーノシュ・ピトリク , リュック・ジ・ファルメ , ロバート・ビー・パーニ
IPC分类号： C07K5/107 , C12N9/99 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D403/12 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/02 , C07K7/06
CPC分类号： C07D491/147 , A61K31/407 , A61K38/00 , A61K45/06 , C07D403/12 , C07K5/06191 , C07K5/0827 , C07K5/101 , C07K5/1027 , C07K7/02 , C07K7/06
摘要： The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

3. 发明专利

JP2005526002A Incorporating a fused ring system, serine proteases, especially c hepatitis ns3-NS4A protease inhibitors 有权
公开(公告)号：JP2005526002A
公开(公告)日：2005-09-02
申请号：JP2003537627
申请日：2002-10-24
申请人：ジョン・エイチ・バン・ドリーJohn H. Van Drie , バーテックスファーマシューティカルズインコーポレイテッドVertex Pharmaceuticals Incorporated , ヤーノシュ・ピトリクJanos Pitlik , ロバート・ビー・パーニRobert B. Perni
发明人：ジョン・エイチ・バン・ドリー , ヤーノシュ・ピトリク , リュック・ジ・ファルメ , ロバート・ビー・パーニ
IPC分类号： C12N9/99 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P43/00 , C07D403/12 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/02 , C07K7/06
CPC分类号： C07D491/147 , A61K31/407 , A61K38/00 , A61K45/06 , C07D403/12 , C07K5/06191 , C07K5/0827 , C07K5/101 , C07K5/1027 , C07K7/02 , C07K7/06
摘要： The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

4. 发明申请

US20110104115A1 INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 失效
标题翻译：丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂
公开(公告)号：US20110104115A1
公开(公告)日：2011-05-05
申请号：US12825237
申请日：2010-06-28
申请人： Robert B. Perni , John J. Court , Shawn D. Britt , Janos Pitlik , John H. Van Drie
发明人： Robert B. Perni , John J. Court , Shawn D. Britt , Janos Pitlik , John H. Van Drie
IPC分类号： A61K38/21 , C07K5/107 , C07K7/06 , A61K38/07 , A61K38/08 , C12N9/99 , A01N37/18 , A01P1/00 , A61P31/12 , A61P37/02 , A61P31/14
CPC分类号： C07K5/1016 , A01N43/60 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K45/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0202 , C07K5/0207 , C07K5/1027 , C07K7/02 , A61K2300/00
摘要： The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，用于离体使用或给予患有HCV感染的患者。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

5. 发明申请

US20090291902A1 INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 失效
标题翻译：丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂
公开(公告)号：US20090291902A1
公开(公告)日：2009-11-26
申请号：US12265125
申请日：2008-11-05
申请人： Kevin M. Cottrell , Robert B. Perni , Janos Pitlik , Wayne C. Schairer
发明人： Kevin M. Cottrell , Robert B. Perni , Janos Pitlik , Wayne C. Schairer
IPC分类号： A61K38/06 , A61K38/07 , C07K5/08 , C07K5/10
CPC分类号： C07K5/10 , C07K7/06
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且作为抗病毒剂是有用的。本发明还涉及包含用于离体使用或用于给予HCV感染患者的所述化合物的药学上可接受的组合物以及制备该化合物的方法。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗患者HCV感染的方法。

6. 发明申请

US20080125376A1 INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 有权
标题翻译：丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂
公开(公告)号：US20080125376A1
公开(公告)日：2008-05-29
申请号：US12026705
申请日：2008-02-06
申请人： Kevin M. Cottrell , John Maxwell , Robert B. Perni , Janos Pitlik
发明人： Kevin M. Cottrell , John Maxwell , Robert B. Perni , Janos Pitlik
IPC分类号： A61K38/05 , A61P41/00 , A61P31/12
CPC分类号： C07K5/0804 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且作为抗病毒剂是有用的。本发明还涉及包含用于离体使用或用于给予HCV感染患者的所述化合物的药学上可接受的组合物以及制备该化合物的方法。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗患者HCV感染的方法。

7. 发明授权

US07378422B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US07378422B2
公开(公告)日：2008-05-27
申请号：US10936450
申请日：2004-09-07
申请人： Robert B. Perni , John J. Court , Shawn D. Britt , Janos Pitlik , John H. van Drie
发明人： Robert B. Perni , John J. Court , Shawn D. Britt , Janos Pitlik , John H. van Drie
IPC分类号： A61K31/517 , A61K31/497 , C07D239/88 , C07D241/24
CPC分类号： C07K5/1016 , A01N43/60 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K45/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0202 , C07K5/0207 , C07K5/1027 , C07K7/02 , A61K2300/00
摘要： The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，用于离体使用或给予患有HCV感染的患者。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

8. 发明授权

US07109172B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 有权
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US07109172B2
公开(公告)日：2006-09-19
申请号：US10893748
申请日：2004-07-16
申请人： Shawn D. Britt , Kevin M. Cottrell , Robert B. Perni , Janos Pitlik
发明人： Shawn D. Britt , Kevin M. Cottrell , Robert B. Perni , Janos Pitlik
IPC分类号： A61K38/00
CPC分类号： C07K7/06
摘要： The present invention relates to compounds of formula I or formula Ia or pharmaceutically acceptable salts thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I或式Ia化合物或其药学上可接受的盐。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且作为抗病毒剂是有用的。本发明还涉及包含用于离体使用或用于给予HCV感染的患者的所述化合物的药学上可接受的组合物和用于制备所述化合物的方法。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗患者HCV感染的方法。

9. 发明申请

US20050137139A1 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US20050137139A1
公开(公告)日：2005-06-23
申请号：US10936450
申请日：2004-09-07
申请人： Robert Perni , John Court , Shawn Britt , Janos Pitlik , John van Drie
发明人： Robert Perni , John Court , Shawn Britt , Janos Pitlik , John van Drie
IPC分类号： A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K38/05 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/02 , C07K5/06 , C07K5/10 , C07K7/02 , C07D43/02
CPC分类号： C07K5/1016 , A01N43/60 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K45/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0202 , C07K5/0207 , C07K5/1027 , C07K7/02 , A61K2300/00
摘要： The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，用于离体使用或给予患有HCV感染的患者。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

10. 发明授权

US08536136B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 有权
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US08536136B2
公开(公告)日：2013-09-17
申请号：US12639162
申请日：2009-12-16
申请人： David Deininger , John Court , Luc Farmer , Janos Pitlik , Kevin Cottrell , Robert B. Perni
发明人： David Deininger , John Court , Luc Farmer , Janos Pitlik , Kevin Cottrell , Robert B. Perni
IPC分类号： A61K38/06 , A61K39/42 , A61P31/12 , A61P1/16 , C07K14/81
CPC分类号： C07K5/10 , A61K38/00 , A61K38/07 , A61K45/06 , C07K5/0202 , C07K7/02 , C07K14/005 , C12N2770/24222
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐或混合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物和制备该化合物的方法。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

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