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1. 发明专利

AU2008212760B2 HCV inhibiting macrocyclic phenylcarbamates 未知
公开(公告)号：AU2008212760B2
公开(公告)日：2014-02-27
申请号：AU2008212760
申请日：2008-02-08
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： RABOISSON PIERRE JEAN-MARIE BERNARD , ANTONOV DMITRY , AYESA ALVAREZ SUSANA , BELFRAGE ANNA KARIN GERTRUD LINNEA , JONSSON CARL ERIK DANIEL , MC GOWAN DAVID CRAIG , NILSSON KARL MAGNUS , ROSENQUIST ASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL
IPC分类号： C07D245/04 , A61K31/538 , A61P31/14 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
摘要： Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof;usefulas HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.

3. 发明专利

CA2617096A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：CA2617096A1
公开(公告)日：2007-02-08
申请号：CA2617096
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： AYESA ALVAREZ SUSANA , CLASSON BJORN OLOF , DE KOCK HERMAN AUGUSTINUS , JONSSON CARL ERIK DANIEL , SIMMEN KENNETH ALAN , SAMUELSSON BENGT BERTIL , ROSENQUIST ASA ANNICA KRISTINA , RABOISSON PIERRE JEAN-MARIE BE , ANTONOV DMITRY , SALVADOR ODEN LOURDES , NILSSON KARL MAGNUS
IPC分类号： C07D401/12 , A61K31/4523 , A61P31/14 , C07D245/04 , C07D403/12
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

4. 发明专利

AU2006274862B2 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274862B2
公开(公告)日：2012-03-22
申请号：AU2006274862
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： SAMUELSSON BENGT BERTIL , CLASSON BJORN OLOF , ROSENQUIST ASA ANNICA KRISTINA , AYESA ALVAREZ SUSANA , WALLBERG HANS KRISTIAN , JONSSON CARL ERIK DANIEL , SIMMEN KENNETH ALAN , NILSSON KARL MAGNUS , DE KOCK HERMAN AUGUSTINUS
IPC分类号： C07D401/12 , A61K31/538 , A61P31/14 , C07D403/12 , C07D413/12
摘要： Inhibitors of HCV replication of formula (I) and the -oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R is -OR, -NH-SOR; Ris hydrogen, and where X is C or CH, R may also be Calkyl; R is hydrogen, Calkyl, CalkoxyCalkyl, or Ccycloalkyl; n is 3, 4, 5, or 6; R and R taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from formula (II) wherein said ring system may optionally be substituted with 1-3 substituents; R is hydrogen; aryl; Het; Ccycloalkyl optionally substituted with Calkyl; or Calkyl optionally substituted with Ccycloalkyl, aryl or with Het; Ris aryl; Het; Ccycloalkyl optionally substituted with Calkyl; or Calkyl optionally substituted with Ccycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 substituents pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

5. 发明专利

AU2008212760A1 HCV inhibiting macrocyclic phenylcarbamates 未知
公开(公告)号：AU2008212760A1
公开(公告)日：2008-08-14
申请号：AU2008212760
申请日：2008-02-08
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： JONSSON CARL ERIK DANIEL , RABOISSON PIERRE JEAN-MARIE BERNARD , ROSENQUIST ASA ANNICA KRISTINA , ANTONOV DMITRY , BELFRAGE ANNA KARIN GERTRUD LINNEA , GOWAN DAVID CRAIG MC , SAMUELSSON BENGT BERTIL , NILSSON KARL MAGNUS , ALVAREZ SUSANA AYESA
IPC分类号： C07D245/04 , A61K31/538 , A61P31/14 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
摘要： Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.

6. 发明专利

AU2006274861A1 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274861A1
公开(公告)日：2007-02-08
申请号：AU2006274861
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： CLASSON BJORN OLOF , JONSSON CARL ERIK DANIEL , SAMUELSSON BENGT BERTIL , SIMMEN KENNETH ALAN , ANTONOV DMITRY , ODEN LOURDES SALVADOR , KOCK HERMAN AUGUSTINUS DE , NILSSON KARL MAGNUS , ALVAREZ SUSANA AYESA , ROSENQUIST ASA ANNICA KRISTINA , RABOISSON PIERRE JEAN-MARIE BE
IPC分类号： C07D401/12 , A61K31/4523 , A61P31/14 , C07D245/04 , C07D403/12
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

7. 发明专利

AU2006274861B2 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274861B2
公开(公告)日：2012-11-08
申请号：AU2006274861
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： JONSSON CARL ERIK DANIEL , CLASSON BJORN OLOF , NILSSON KARL MAGNUS , AYESA ALVAREZ SUSANA , ROSENQUIST ASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL , DE KOCK HERMAN AUGUSTINUS , ANTONOV DMITRY , RABOISSON PIERRE JEAN-MARIE BERNARD , SIMMEN KENNETH ALAN , SALVADOR ODEN LOURDES
IPC分类号： C07D401/12 , A61K31/4523 , A61P31/14 , C07D245/04 , C07D403/12
摘要： Inhibitors of HCV replication of formula (I) and the -oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by ------) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R is -OR, -NH-SOR; R is hydrogen, and where X is C or CH, R may also be Calkyl; R is hydrogen, Calkyl, CalkoxyCalkyl, or Ccycloalkyl; n is 3, 4, 5, or 6; R and R independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, Calkyl, Calkoxy, CalkoxyCalkyl, Calkylcarbonyl, Calkoxy- carbonyl, amino, azido, mercapto, Calkylthio, polyhaloCalkyl, aryl or Het; W is aryl or Het; R is hydrogen; aryl; Het; Ccycloalkyl optionally substituted with Calkyl; or Calkyl optionally substituted with Ccycloalkyl, aryl or with Het; R is aryl; Het; Ccycloalkyl optionally substituted with Calkyl; or Calkyl optionally substituted with Ccycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

8. 发明专利

EA013475B1 МАКРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ ВИРУСА ГЕПАТИТА С 未知
公开(公告)号：EA013475B1
公开(公告)日：2010-04-30
申请号：EA200800478
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： DE KOCK HERMAN AUGUSTINUS , SIMMEN KENNETH ALAN , JONSSON CARL ERIK DANIEL , AYESA ALVAREZ SUSANA , CLASSON BJORN OLOF , NILSSON KARL MAGNUS , ROSENQUIST ASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL , WALLBERG HANS KRISTIAN
IPC分类号： C07D401/12 , A61K31/538 , A61P31/14 , C07D403/12 , C07D413/12
摘要： Ингибиторырепликации HCV формулы (I) иих N-оксиды, солиилистереоизомеры, вкоторыхкаждаяпунктирнаялинияпредставляетсобойнеобязательнуюдвойнуюсвязь; X представляетсобой N, СНи, когда X содержитдвойнуюсвязь, онпредставляетсобойС; Rпредставляетсобой -OR, -NHSOR; Rпредставляетсобойводороди, когда X представляетсобойС илиСН, Rтакжеможетпредставлятьсобой C-алкил; Rпредставляетсобойводород, C-алкил, С-алкокси-С-алкилилиС-циклоалкил; n равно 3, 4, 5 или 6; Rи R, взятыевместес атомомазота, ккоторомуониприсоединены, образуютбициклическуюкольцевуюсистему, выбраннуюизформулы (II), гдеупомянутаякольцеваясистеманеобязательноможетбытьзамещена 1-3 заместителями; Rпредставляетсобойводород, арил, Het, С-циклоалкил, необязательнозамещенный C-алкилом, или C-алкил, необязательнозамещенныйС-циклоалкилом, ариломили Het; Rпредставляетсобойарил; Het; С-циклоалкил, необязательнозамещенный C-алкилом, или C-алкил, необязательнозамещенныйС-циклоалкилом, ариломили Het; арилпредставляетсобойфенилилинафтил, каждыйизкоторыхнеобязательноможетбытьзамещен 1-3 заместителями; Het представляетсобой 5- или 6-членное, насыщенное, частичноненасыщенноеилиполностьюненасыщенноегетероциклическоекольцо, содержащееот 1 до 4 гетероатомов, каждыйизкоторыхнезависимовыбраниз N, Оили S, инеобязательнозамещенное 1-3 заместителями; фармацевтическиекомпозиции, содержащиесоединения (I), испособыполучениясоединений (I). Такжепредлагаютсябиодоступныекомбинацииингибиторов HCV формулы (I) сритонавиром.

9. 发明专利

AU2006274862A1 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274862A1
公开(公告)日：2007-02-08
申请号：AU2006274862
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： SAMUELSSON BENGT BERTIL , CLASSON BJORN OLOF , ROSENQUIST ASA ANNICA KRISTINA , ALVAREZ SUSANA AYESA , WALLBERG HANS KRISTIAN , JONSSON CARL ERIK DANIEL , SIMMEN KENNETH ALAN , NILSSON KARL MAGNUS , KOCK HERMAN AUGUSTINUS DE
IPC分类号： C07D401/12 , A61K31/538 , A61P31/14 , C07D403/12 , C07D413/12
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.

10. 发明专利

CA2617096C MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：CA2617096C
公开(公告)日：2013-12-24
申请号：CA2617096
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： RABOISSON PIERRE JEAN-MARIE BERNARD , DE KOCK HERMAN AUGUSTINUS , SIMMEN KENNETH ALAN , JONSSON CARL ERIK DANIEL , NILSSON KARL MAGNUS , ROSENQUIST ASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL , ANTONOV DMITRY , SALVADOR ODEN LOURDES , AYESA ALVAREZ SUSANA , CLASSON BJORN OLOF
IPC分类号： C07D417/12 , A61K31/407 , A61K31/4155 , A61K31/427 , A61P31/14 , C07D245/04 , C07D401/12 , C07D403/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by ------) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is -OR6, -NH-SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy- carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

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