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公开(公告)号:NZ579295A
公开(公告)日:2012-03-30
申请号:NZ57929508
申请日:2008-02-20
Applicant: VERTEX PHARMA
Inventor: FARMER LUC , BETHIEL RANDY SCOTT , JACOBS DYLAN , PERNI ROBERT B , MAXWELL JOHN , COTTRELL KEVIN , HALAS SUMMER
IPC: C07D487/10 , A61K31/407 , A61P31/12 , C07D498/10
Abstract: Disclosed are spiro compounds of formula I or pharmaceutically acceptable salts thereof, and methods for their synthesis. Specific examples of compounds of formula I include: (5S,8S)-7-((S)-2-(2-cyclohexylacetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-2-oxo-3-phenyl-1-oxa-3,7-diazaspiro[4.4]nonane-8-carboxamide, (5R,8S)-7-((S)-2-(2-cyclohexylacetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-2-oxo-3-phenyl-1-oxa-3,7-diazaspiro[4.4]nonane-8-carboxamide, Cyclopentyl-(S)-1-((3S,5R)-3-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-ylcarbamoyl)-8-oxo-7-phenyl-2,7-diazaspiro[4.4]nonan-2-yl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate, and Cyclopentyl (S)-1-((3S,5S)-3-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-ylcarbamoyl)-8-oxo-7-phenyl-2,7-diazaspiro[4.4]nonan-2-yl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate. Also disclosed is the use of compounds of formula I for treating a hepatitis C virus (HCV) infection.
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公开(公告)号:NZ571280A
公开(公告)日:2011-10-28
申请号:NZ57128007
申请日:2007-03-14
Applicant: VERTEX PHARMA
Inventor: PERNI ROBERT B , CHEN MINZHANG , JUNG YOUNG CHUN , FORSLUND RAYMOND E , TANOURY GERALD J , BENNANI YOUSSEF , ZLOKARNIK GREGOR , MALTAIS FRANCOIS
IPC: C07D209/52 , A61K31/403 , A61K31/422 , A61K31/498 , A61P31/12 , C07C231/20 , C07C237/04 , C07D403/12 , C07D403/14 , C07D498/10
Abstract: Disclosed is a keto-enriched alpha-ketoamido compound represented by general formula (I) wherein D is a deuterium atom. Also disclosed is the use of the compounds of formula (I) for treating hepatitis C virus (HCV) infection or a condition mediated by HCV protease
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公开(公告)号:AU2003223602B8
公开(公告)日:2010-05-27
申请号:AU2003223602
申请日:2003-04-11
Applicant: VERTEX PHARMA
Inventor: PITLIK JANOS , PERNI 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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公开(公告)号:ZA200808645B
公开(公告)日:2009-07-29
申请号:ZA200808645
申请日:2008-10-09
Applicant: VERTEX PHARMA
Inventor: PERNI ROBERT B , MINZHANG CHEN , CHUN JUNG YOUNG , FORSLUND RAYMOND E , TANOURY GERALD J , YOUSSEF BENNANI , GREGOR ZLOKARNIK , FRANCOIS MALTAIS
IPC: A61K20090101 , A61P20090101 , C07C20090101 , C07D20090101
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公开(公告)号:AU2008219704A1
公开(公告)日:2008-09-04
申请号:AU2008219704
申请日:2008-02-20
Applicant: VERTEX PHARMA
Inventor: HALAS SUMMER , PERNI ROBERT B , BETHIEL RANDY SCOTT , JACOBS DYLAN , MAXWELL JOHN , COTTRELL KEVIN , FARMER LUC
IPC: C07D487/10 , A61K31/407 , A61P31/12 , C07D498/10
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.
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公开(公告)号:MX2008001528A
公开(公告)日:2008-04-04
申请号:MX2008001528
申请日:2006-08-01
Applicant: VERTEX PHARMA
Inventor: PERNI ROBERT B , LYONS STEVE
IPC: C07D403/12 , A61K31/501 , A61P31/12
Abstract: La invencion se refiere a compuestos de la formula (I): (ver formula) o una sal farmaceuticamente aceptable o mezclas de los mismos en donde C* representa un carbono diaestereomerico que comprende una mezcla de isomeros R y S en donde el isomero R es mayor al 50% de la mezcla.
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公开(公告)号:HK1101402A1
公开(公告)日:2007-10-18
申请号:HK07106097
申请日:2007-06-07
Applicant: VERTEX PHARMA
Inventor: COTTRELL KEVIN M , COURT JOHN J , DEININGER DAVID D , FARMER LUC J , PITLIK JANOS , PERNI ROBERT B
IPC: A61K20060101 , A61K38/00 , A61K38/04 , A61K38/05 , C07K20060101 , C07K5/02 , C07K5/04 , C07K7/02 , C07K14/18
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 theses compounds.
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公开(公告)号:AU2007227544A1
公开(公告)日:2007-09-27
申请号:AU2007227544
申请日:2007-03-14
Applicant: VERTEX PHARMA
Inventor: PERNI ROBERT B , JUNG YOUNG CHUN , TANOURY GERALD J , CHEN MINZHANG , FORSLUND RAYMOND E , BENNANI YOUSSEF , MALTAIS FRANCOIS , ZLOKARNIK GREGOR
IPC: C07C231/20 , A61K31/403 , A61K31/422 , A61K31/498 , A61P31/12 , C07C237/04 , C07D209/52 , C07D403/12 , C07D403/14 , C07D498/10
Abstract: This invention relates to a process for preparing a compound of Formula 1 wherein: the carbon atoms alpha and beta to the carboxy group are stereocenters; R 1 is independently H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; R' 1 is deuterium such that the deuterium enrichment is at least 50%; R' 2 is -NHR 2 or -OE; R 2 is H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; and E is C 1-6 alkyl or benzyl; wherein the process comprises the steps of: a) forming a salt of a compound of Formula 1, and b) crystallizing said salt to give a compound of greater than 55% enantiomeric excess.
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公开(公告)号:ZA200602937B
公开(公告)日:2007-06-27
申请号:ZA200602937
申请日:2004-10-08
Applicant: VERTEX PHARMA
Inventor: COTTRELL KEVIN M , PERNI ROBERT B , JANOS PITLIK
IPC: A61K20090101 , C07K20090101
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公开(公告)号:ZA200601420B
公开(公告)日:2007-06-27
申请号:ZA200601420
申请日:2004-07-16
Applicant: VERTEX PHARMA
Inventor: BRITT SHAWN D , COTTRELL KEVIN M , PERNI ROBERT B , JANOS PITLIK
IPC: A61K20090101 , A61P20090101 , A61P31/12 , C07K20090101 , 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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