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1. 发明专利

AU2006274866A1 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274866A1
公开(公告)日：2007-02-08
申请号：AU2006274866
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： LINDQUIST KARIN CHARLOTTA , KOCK HERMAN AUGUSTINUS DE , KAHNBERG PIA CECILIA , HU LILI , ROSENQUIST ASA ANNICA KRISTINA , RABOISSON PIERRE JEAN-MARIE BE , SAHLBERG SVEN CRISTER , LINDSTROM MATS STEFAN , NILSSON KARL MAGNUS , SIMMEN KENNETH ALAN , BELFRAGE ANNA KARIN GERTRUD LI , SAMUELSSON BENGT BERTIL , WALLBERG HANS KRISTIAN , WAHLING HORST JURGEN , CLASSON BJORN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
摘要： Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(-O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.

2. 发明专利

MY139987A MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY139987A
公开(公告)日：2009-11-30
申请号：MYPI20063667
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： KOCK HERMAN AUGUSTINUS DE , RABOISSON PIERRE JEAN-MARIE , SIMMEN KENNETH ALAN , LINDSTROM MATS STEFAN , KAHNBERG PIA CECILIA , ANTONOV DMITRY , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTINA
IPC分类号： C07K5/078
摘要： _81- AB@TRACT MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 5 INHIBITORS OF HCV OFFORNIULA (1) OME N 0 0 N 0 0 R1_N @)N N-SO2 (Z) R2 AND THE AL-OXIDES, SALTS, AND STEREOISORNERS THEREOF. WHEREIN THE DASHED LINE REPRESENTS I 0 AN OPTIONAL DOUBLE BOND BETWEEN ATOMS C7 AND C8; R' IS HVDROGEN OR CJ_,,ALKVL@ R2 IS HYDROGEN OR CL-(,ALKVL; AND N IS 3, 4, 5, OR 6@ 1 PHANNACEWICAL COMPOSITIONS COINAINML COMPOUNDS (1) AND PIOCE@SCS FOI PIEPALING COMPOUNDS (1) ARE PROVIDED. BIOAVAILABLE COMBINATION@ OFTHE INHIBITORS OJ'HCV OF FORNIULA (1) WITH RITONAVIR ARE ALSO PROVIDED.

3. 发明专利

CA2617103C MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：CA2617103C
公开(公告)日：2015-01-06
申请号：CA2617103
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 , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LINNEA , WAHLING HORST JURGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST ASA ANNICA KRISTINA , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJORN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(=O)PR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono-or dialkylaminocarbonyl, C1-C6alkyl- carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.

4. 发明专利

ES2339702T3 INHIBIDORES MACROCICLICOS DEL VIRUS DE LA HEPATITIS C. 未知
公开(公告)号：ES2339702T3
公开(公告)日：2010-05-24
申请号：ES06764268
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 , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROM MATS STEFAN
IPC分类号： C07D417/04
摘要： Un compuesto de la fórmula I: **(Ver fórmula)** y N-óxidos, sales y estereoisómeros del mismo en donde A es OR1, NHS(=O)pR2; en donde: R1 es hidrógeno, C1-C6alquilo, C0-C3alquilenocarbociclilo, C0-C3alquileno-heterociclilo; R2 es C1-C6alquilo, C0-C3alquilenocarbociclilo, C0-C3alquilenoheterociclilo; p es independientemente 1 ó 2; n es 3, 4, 5 ó 6; ----- denota un enlace doble opcional; L es N o CRz; Rz es H o forma un enlace doble con el carbono que lleva el asterisco; Rq es H o, cuando L es CRz, Rq puede ser también C1-C6alquilo; Rr es quinazolinilo, sustituido opcionalmente con 1, 2 ó 3 sustituyentes, seleccionado cada uno independientemente de C1-C6alquilo, C1-C6alcoxi, hidroxilo, halo, haloC1-C6alquilo, amino, mono- o dialquilamino, mono- o dialquilaminocarbonilo, C1-C6alquilcarbonilamino, C0-C3alquilenocarbociclilo y C0-C3alquilenoheterocicliclo; R5 es hidrógeno, C1-C6alquilo, C1-C6alcoxiC1-C6alquilo o C3-C7cicloalquilo; y en donde cada C1-C6alquilo, C0-C3alquilenocarbociclilo o C0-C3alquilenoheterociclilo está sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo constituido por halo, oxo, nitrilo, azido, nitro, C1-C6alquilo, C0-C3alquilenocarbociclilo, C0-C3alquilenoheterociclilo, NH2C(=O)-, Y-NRaRb, Y-O-Rb, Y-C(=O)Rb, Y-(C=O)NRaRb, Y-NRaC(=O)Rb, Y-NHS(=O)pRb, Y-S(=O)pRb e Y-S(=O)pNRaRb, Y-C(=O)ORb, Y-NRaC(=O)ORb; Y es independientemente un enlace o C1-C3alquileno; Ra es independientemente H, C1-C6alcoxi, C1-C3alquilo o; (sic) Rb es independientemente H, C1-C6alquilo, C1-C6alcoxi, C0-C3alquilenocarbociclilo o C0-C3alquilenohe- terociclilo; o Ra y Rb junto con el nitrógeno al cual están fijados, se unen para formar un grupo heterociclilo.

5. 发明专利

AU2006274857A1 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274857A1
公开(公告)日：2007-02-08
申请号：AU2006274857
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： LINDSTROM MATS STEFAN , KAHNBERG PIA CECILIA , SAMUELSSON BENGT BERTIL , RABOISSON PIERRE JEAN-MARIE BE , ANTONOV DMITRY , ROSENQUIST ASA ANNICA KRISTINA , NILSSON KARL MAGNUS , KOCK HERMAN AUGUSTINUS DE , SIMMEN KENNETH ALAN
IPC分类号： C07K5/078 , A61K31/4709 , A61P31/14 , C07K5/06
摘要： Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

7. 发明专利

NZ564540A Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：NZ564540A
公开(公告)日：2010-03-26
申请号：NZ56454006
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 , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LINNEA , WAHLING HORST JURGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST ASA ANNICA KRISTINA , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJORN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
摘要： The disclosure relates to macrocyclic compounds of the formula (I) and N-oxides, salts, and stereoisomers thereof having inhibitory activity on the replication of the hepatitis C virus (HCV), wherein the variables are as defined in the specification. The disclosure further relates to compositions comprising these compounds as active ingredients as well as processes for preparing these compounds and compositions. These compounds are suitable for the treatment or prophylaxis of flaviviral infections such as HCV.

8. 发明专利

PE03432007A1 INHIBIDORES MACROCICLICOS DEL VIRUS DE LA HEPATITIS C 未知
公开(公告)号：PE03432007A1
公开(公告)日：2007-05-12
申请号：PE0009032006
申请日：2006-07-26
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： SIMMEN KENNETH ALAN , RABOISSON PIERRE JEAN-MARIE , LINDQUIST KARIN CHARLOTTA , GERTRUD BELFRAGE ANNA KARIN , NILSSON KARL MAGNUS , ROSENQUIST AASA ANNICA KRISTINA , WALLBERG HANS KRISTIAN , CLASSON BJORN OLOF , KAHNBERG PIA CECILIA , SAHLBERG SVEN CRISTER , SAMUELSSON BENGT BERTIL , WAHLING HORST JURGEN , LINDSTROM MATS STEFAN , HU LILI , DE KOCK HERMAN AUGUSTINUS
IPC分类号： A61K31/517 , A61P31/12 , C07D239/72 , C07D417/04
CPC分类号： C07D487/10 , C07D245/04
摘要： REFERIDA A UN COMPUESTO MACROCICLICO DE FORMULA (I), DONDE A ES OR1, NHS(=O)pR2; R1 ES H, ALQUILO C1-C6, ALQUILEN C0-C3-CARBOCICLILO, ENTRE OTROS; R2 ES ALQUILO C1-C6, ALQUILEN C0-C3-CARBOCICLILO, ENTRE OTROS; p ES 1 O 2; n ES 3, 4, 5 O 6; ----- ES UN DOBLE ENLACE OPCIONAL; L ES N O CRZ; RZ ES H, O FORMA DOBLE ENLACE CON EL CARBONO CON ASTERISCO; Rq ES H O CUANDO L ES CRZ; Rq ES H O ALQUILO C1-C6; Rr ES QUINAZOLINILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6, ALCOXI C1-C6, HIDROXILO, ENTRE OTROS; R5 ES H, ALQUILO C1-C6, ALCOXI C1-C6-ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 17-[7-METOXI-2-(4-METOXI-FENIL)-8-METIL-QUINAZOLIN-4-ILOXI]-13-METIL-2,14-DIOXO-3,13,15-TRIAZA-TRICICLO[13.3.0.0*4,6*]OCTADEC-7-EN-4-CARBOXILICO, {17-[7-METOXI-2-(4-METOXI-FENIL)-8-METIL-QUINAZOLIN-4-ILOXI]-13-METIL-2,14-DIOXO-3,13,15-TRIAZA-TRICICLO[13.3.0.0*4,6*]OCTADEC-7-EN-4-CARBONIL}-AMIDA DEL ACIDO CICLOPROPANSULFONICO, {17-[7-METOXI-2-(4-METOXI-FENIL)-8-METIL-QUINAZOLIN-4-ILOXI]-13-METIL-2,14-DIOXO-3,13,15-TRIAZA-TRICICLO[13.3.0.0*4,6*]OCTADEC-7-EN-4-CARBONIL}-AMIDA DEL ACIDO 1-METIL-CICLOPROPANSULFONICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA REPLICACION DEL VIRUS DE LA HEPATITIS C (VHC) Y SON UTILES PARA EL TRATAMIENTO DE FIBROSIS DE HIGADO PROGRESIVA, ENTRE OTRAS, ASI COMO DE INFECCIONES CAUSADAS POR OTROS FLAVIVIRUS TALES COMO FIEBRE AMARILLA, FIEBRE DEL DENGUE, FIEBRE HEMORRAGICA, ENTRE OTRAS

9. 发明专利

CA2616954C MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：CA2616954C
公开(公告)日：2013-12-24
申请号：CA2616954
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： DE KOCK HERMAN AUGUSTINUS , RABOISSON PIERRE JEAN-MARIE BERNARD , SIMMEN KENNETH ALAN , LINDSTROM MATS STEFAN , KAHNBERG PIA CECILIA , ANTONOV DMITRY , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST ASA ANNICA KRISTINA
IPC分类号： C07K5/078 , A61K31/4709 , A61P31/14 , C07K5/06
摘要： Inhibitors of HCV of formula (I), and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

10. 发明专利

AU2006274857B2 Macrocyclic inhibitors of hepatitis C virus 未知
公开(公告)号：AU2006274857B2
公开(公告)日：2012-11-29
申请号：AU2006274857
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： SAMUELSSON BENGT BERTIL , SIMMEN KENNETH ALAN , ANTONOV DMITRY , KAHNBERG PIA CECILIA , DE KOCK HERMAN AUGUSTINUS , ROSENQUIST ASA ANNICA KRISTINA , RABOISSON PIERRE JEAN-MARIE BERNARD , LINDSTROM MATS STEFAN , NILSSON KARL MAGNUS
IPC分类号： C07D487/04 , A61K31/4709 , A61P31/14 , C07K5/06 , C07K5/078
摘要： Inhibitors of HCV of formula (I), and the -oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R is hydrogen or Calkyl; R is hydrogen or Calkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

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