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1.发明申请2-AMIDO-4-ARYLOXY-1-CARBONYLPYRROLIDINE DERIVATIVES AS INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 审中-公开作为丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂的2-氨基-4-氰基-1-羰基吡咯烷衍生物
公开(公告)号：WO2005035525A3
公开(公告)日：2005-10-20
申请号：PCT/US2004029093
申请日：2004-09-07
Applicant: VERTEX PHARMA , PERNI ROBERT B , COURT JOHN J , BRITT SHAWN D , PITLIK JANOS , VAN DRIE JOHN H
Inventor： PERNI ROBERT B , COURT JOHN J , BRITT SHAWN D , PITLIK JANOS , VAN DRIE JOHN H
IPC: 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 , A61P31/14
CPC classification number: 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
Abstract: The present invention relates to compounds of formula I-A and I-B 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.
Abstract translation: 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-A和I-B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，并且也可用作抗病毒剂。 本发明还涉及包含这些化合物的组合物，用于离体使用或用于给予HCV感染患者。 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。
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2.发明申请INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 审中-公开丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂
公开(公告)号：WO2005077969A3
公开(公告)日：2005-12-01
申请号：PCT/US2005003381
申请日：2005-02-04
Applicant: VERTEX PHARMA , COTTRELL KEVIN M , COURT JOHN J , DEININGER DAVID D , FARMER LUC J , PITLIK JANOS , PERNI ROBERT B
Inventor： COTTRELL KEVIN M , COURT JOHN J , DEININGER DAVID D , FARMER LUC J , PITLIK JANOS , PERNI ROBERT B
IPC: A61K38/00 , A61K38/04 , A61K38/05 , C07K5/02 , C07K5/04 , C07K7/02 , C07K14/18 , A61K38/07 , A61K38/08
CPC classification number: C07K5/10 , A61K38/00 , A61K38/07 , A61K45/06 , C07K5/0202 , C07K7/02 , C07K14/005 , C12N2770/24222
Abstract: 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.
Abstract translation: 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其混合物。 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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3.发明申请INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE 审中-公开丝氨酸蛋白酶特异性HCV NS3-NS4A蛋白的抑制剂
公开(公告)号：WO2005007681A2
公开(公告)日：2005-01-27
申请号：PCT/US2004023054
申请日：2004-07-16
Applicant: VERTEX PHARMA , BRITT SHAWN D , COTTRELL KEVIN M , PERNI ROBERT B , PITLIK JANOS
Inventor： BRITT SHAWN D , COTTRELL KEVIN M , PERNI ROBERT B , PITLIK JANOS
CPC classification number: C07K7/06
Abstract: 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 by15 administering a pharmaceutical composition comprising a compound of this invention.
Abstract translation: 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。
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公开(公告)号：CA2536436C
公开(公告)日：2013-04-09
申请号：CA2536436
申请日：2004-09-07
Applicant: VERTEX PHARMA
Inventor： PERNI ROBERT B , COURT JOHN J , BRITT SHAWN D , PITLIK JANOS , VAN DRIE JOHN H
IPC: C07K5/107 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K38/05 , A61K38/06 , A61K45/06 , A61P31/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/02 , C07K5/06 , C07K5/10 , C07K7/02 , C12N9/50
Abstract: The present invention relates to compounds of formula I-A and I-B 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 vivouse 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.
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公开(公告)号：AU2003223602B2
公开(公告)日：2010-05-13
申请号：AU2003223602
申请日：2003-04-11
Applicant: VERTEX PHARMA
Inventor： PITLIK JANOS , PERNII ROBERT B , DRIE JOHN H VAN , FARMER LUC J , COTTRELL KEVIN M , MURCKO MARK A , COURTNEY LAWRENCE F
IPC: C12N9/99 , A61K38/00 , A61K38/04 , A61P1/16 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D471/04 , C07K5/04 , C07K5/06 , C07K5/10 , C07K7/02
Abstract: 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.
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Patent Agency Ranking
公开(公告)号：NZ545158A
公开(公告)日：2009-11-27
申请号：NZ54515804
申请日：2004-09-07
Applicant: VERTEX PHARMA
Inventor： PERNI ROBERT B , COURT JOHN J , BRITT SHAWN D , PITLIK JANOS , VAN DRIE JOHN H
IPC: C07D403/12 , A61K31/401 , A61K31/4025 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K38/05 , A61K45/06 , A61P31/14 , C07D207/12 , C07D207/16 , C07D241/24 , C07D401/12 , C07D401/14 , C07D403/14 , C07K5/02 , C07K5/06 , C07K5/10 , C07K7/02
Abstract: Disclosed are pyrazine functionalised peptide derivatives of formula I: wherein: Ar is a five to ten membered aromatic ring having up to 4 heteroatoms selected from O, S, N(H), SO, and SO2; W is -C(=O)C(=O)-R6, or -C(=O)C(=O)-N(R6)2; T is an optionally substituted pyrazine moiety, and the other substituents are defined herein. Also disclosed is the use of a compound as defined above for the manufacture of a medicament for inhibiting the activity of a serine protease such as an HCV NS3 protease.
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公开(公告)号：AU2002348414B2
公开(公告)日：2009-10-01
申请号：AU2002348414
申请日：2002-10-24
Applicant: VERTEX PHARMA
Inventor： DRIE JOHN H VAN , PERNIE ROBERT B , FARMER LUC J , PITLIK JANOS
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公开(公告)号：DE60217114T2
公开(公告)日：2007-10-25
申请号：DE60217114
申请日：2002-07-11
Applicant: VERTEX PHARMA
Inventor： FARMER LUC , PITLIK JANOS , PERNI ROBERT , COURTNEY LAWRENCE , VAN DRIE JOHN
IPC: A61K45/00 , C07K5/10 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61P31/12 , A61P31/14 , A61P43/00 , C07D453/06 , C07D471/08 , C07K5/103 , C07K5/107 , C07K5/11 , C07K5/117 , C07K7/02 , C07K7/06
Abstract: The present invention relates to peptidomimetic compounds which 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 compounds of this invention have a bridged bicyclic moiety at the P2 position. 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.
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公开(公告)号：HK1098164A1
公开(公告)日：2007-07-13
申请号：HK07104318
申请日：2007-04-24
Applicant: VERTEX PHARMA
Inventor： BRITT SHAWN D , COTTRELL KEVIN M , PERNI ROBERT B , PITLIK JANOS
IPC: A61K20060101 , A61P20060101 , A61P31/12 , C07K20060101 , C07K7/06
Abstract: 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.
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公开(公告)号：CA2536436A1
公开(公告)日：2005-04-21
申请号：CA2536436
申请日：2004-09-07
Applicant: VERTEX PHARMA
Inventor： PERNI ROBERT B , COURT JOHN J , BRITT SHAWN D , PITLIK JANOS , VAN DRIE JOHN H
IPC: C07D403/12 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K38/00 , A61K38/05 , A61K45/06 , A61P31/14 , C07D401/12 , C07D401/14 , C07D403/14 , C07K5/02 , C07K5/06 , C07K5/10 , C07K7/02
Abstract: The present invention relates to compounds of formula I-A and I-B that inhib it 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 vivouse 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.
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