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21. 发明专利

MY141245A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY141245A
公开(公告)日：2010-03-31
申请号：MYPI20063663
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： KOCK HERMAN AUGUSTINUS DE , SIMMEN KENNETH ALAN , NSSON CARL ERIK DANIEL J XD , ALVAREZ SUSANA AYESA , CLASSON BJ XD RN OLOF , NILSSON KARL MAGNUS , ROSENQUIST AASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL , WALLBERG HANS KRISTIAN
IPC分类号： C07D401/12
摘要： INHIBITORS OF HCV REPLICATION OF FORMULA (1) AND THE AL-OXIDES, SALTS, OR STEREOISORNERS 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-SO2R'; * 2IS HYDROGEN, AND WHERE X IS C OR CH, R2 MAV ALSO BE C1-6ALKYL: 10 R 3IS HYDROGEN, CI-6ALKV], C1.6ALKOXYCJ-6ALKYL, OR C3-7CVC]OALKYL- N IS 3, 4@ 5, OR 6@ * 4AND R 5TAKEN TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A BICYCLIC FING SYSTEM SELECTED FROM (N/ 0 AND WHEREIN SAID RING SYSTEM MAY OPTIONALLY BE SUBSTITUTED WITH I -3) SUBSTITUENTS; 15 R6 IS HYDROGEN; ARYL; HET; C.1-7CYC]OALKYL OPTIONALLY SUBSTITUTED WITH CI-6ALKYLL OR CI-6ALKVL OPTIONALLY SUBSTITUTED WITH C_1-7CVCLOAIKVL. ARV] OR WITH HET; R7 IS ARYL; HET.- C-,-7CYCLOALKVL OPTIONALLY SUBSTITUTED WITH C1-6ALKYL- OR C].6ALKYL OPTIONALLY SUBSTITUTED WITH C3-7CYCLOALKYL, ARYL OR WITH HET; ARYL IS PHENYL OR NAPHTHVL, EACH OF WHICH MAY BE OPTIONALLY SUBSTITUTED WITH 1-3 20 SUBSTITUENTS: HET IS A 5 OR 6 MEMBERED SATURATED, PARTIALLY UNSATURATED OR COMPLETELY UNSATURATED HETEROCYCLIC FING CONTAINING I TO 4 HETEROATOMS EACH INDEPENDENTLY SELECTED FROM N, 0 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.

22. 发明专利

PE20070343A1 INHIBIDORES MACROCICLICOS DEL VIRUS DE LA HEPATITIS C 未知
公开(公告)号：PE20070343A1
公开(公告)日：2007-05-12
申请号：PE2006000903
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
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

26. 发明专利

SG163617A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：SG163617A1
公开(公告)日：2010-08-30
申请号：SG2010051407
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 , VENDEVILLE SANDRINE MARIE HELENE , TAHRI ABDELLAH , SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN , SIMMEN KENNETH ALAN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTINA , IVANOV VLADIMIR , PELCMAN MICHAEL , BELFRAGE ANNA KARIN GERTRUD LINNEA , JOHANSSON PER-OLA MIKAEL
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C;R1is-OR7,NH-SO2R8;R2is hydrogen, and where X is C or CH, R 2 may also be C1-6alkyl;R3is hydrogen,C1- 6alkyl,C1-6alkoxyC1-6alkyl,C 3- 7 cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5is halo,C1-6alkyl, hydroxy,C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl or C1-6alkyl optionally substituted with C3- 7cycloalkyl; aryl or with Het; R8is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; orC1-6optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three 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.

27. 发明专利

MY139988A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY139988A
公开(公告)日：2009-11-30
申请号：MYPI20063666
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： RABOISSON PIERRE JEAN-MARIE , SIMMEN KENNETH ALAN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTINA , WALLBERG HANS KRISTIAN , KOCK HERMAN AUGUSTINUS DE , DORANGE ISMET , VENDEVILLE SANDRINE MARIE HELENE , SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN , TAHRI ABDELLAH , SIMONNET YVAN , VREKEN WIM VAN DE , LILI HU
IPC分类号： A61K31/14
摘要： 12 1 MACROC17LIC INHIBRRORS OF HEPATITIS C NARUS ABSTRACT 5 INHIBITORS OF HCV REPLICATION OF FORNIULA (1) 0 @R 4 R 2 0@ 0 N R 3 R1 AND THE N-OXIDES, SALTS. AND STEREOISORNERS THEREOF. WHEREIN X IS N, CH AND WHEREN BEARS A DOUBLE BOND IT IS C; R' IS -OR5. -NH-SO,R', I 0 R 2 I S HYDROGEN, AND WHERE X IS C OR CH, R 2 MAY ALSO BE CJ_6AIKVI * 3 I S HV(IROPEN, CJ_(,ALKVL CJ_6AIKOXVCJ_6AIKV], OR C3 7CVC10ALKY]; * 4 I S ISOQUIRIOLINYL OPTIONALLY SUBSTITUTED WITH ONE, TWO OI THREE SUBS-TILUENTS EACH INDEPENDENTLY SELECTED TROM CT-(,ALKYT, CI-6ALKOXV, HVDROXY, LIALO, POLVHALO- CI-6ALKVL, POLVHA]OC]-6A]KOXV, AMINO, MONO- OI- DICJ-(,AIK-VIAROINO, NIONO- OR 1 5 DIQ-6ALKYLARNINOCARBONVL. CI-6ALKCARBONVL-AMINO, ARYL, AND HET; N IS 3), 4, 5, OR 6: EACH DASHED LINE (REPRESENTED BY ----- ) REPRESENTS AN OPTIONAL DOUBLE BOND, R5 IS HYDROGEN-, ARYL- 7 HET; C3 7C)'CLOALKV] OPTIONALLY SUBSTITUTED WITH CI 6ALKYLL OR CI-6ALKVI OPTIONALLY SUBSTITUTED WITH C 7C@'CLOALKVL, ARYL OR WITH HET: 3 20 R' IS ARYL; HET; C3-7CYCIOALKVL OPTIONALLY SUBSTITUTED WITH CI-6ALKYL, 01 CI-6ALKYL OPTIONALLY SUBSTITUTED WITH C3-7CVCLOALKY1, ARYL OR WITH HET EACH ARY) IS PLIENYL OPTIONALLY SUBSTITUTED WITH ONE, TWO OR THREE SUBSTILUENTS AND EACH HET IS A 5 OR 6 MEMBERED SATURATED, PARTIALLY UNSATURATED OR COMPLELEIV UNSATURATED HETEROCVCLIC RING CONTAINING I TO 4 HELEROALOIRIS CACH INDEPENDENTLY 2) 5 SELECTED FROM NITROGEN, OXV,,CN AND SULFUR, AND BEING OPTIONALLY SUBSTATILED WILH ONE, TWO OR THREE SUBSTITUENTS: PLIARNIACEUTICAL COMPOSNIONS CONTAINING COMPOUNDS (1) AND PROCESSES FOL I)IEPARNIL. COMPOUNDS (1). BIOAVAILABLE COMBINATION, OF THE INHIBITORS OF HCV OF FORINULA (1) WITH

28. 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.

29. 发明专利

MY139923A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY139923A
公开(公告)日：2009-11-30
申请号：MYPI20063665
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： RABOISSON PIERRE JEAN-MARIE , KOCK HERMAN AUGUSTINUS DE , LILI HU , SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN , SIMMEN KENNETH ALAN , LOURDES SALVADOR ODEN , NILSSON KARL MAGNUS , ROSENQUIST AASA ANNICA KRISTINA , SAMUELSSON BENGT BERTIL
IPC分类号： C07D487/04
摘要： 1 19 MACROCYLIC INHIBITORS OF NEPATITIS C VIRUS ABSTRACT 5 INHIBITORS OF HCV REPLICATION OF FORI-NULA (1) R 4 R2, 0 N RLB R3@ NH-S(O)P-N / \RLA AND THE N-OXIDES, SALTS, AND STEREOISORNERS THEREOFWHEI EM EACH DASHED LINE REPRESENTS ,IN OPTIONAL DOUBLE BOND@ X IS N, CH AND WHERE X BEARS A DOUBLE BOND IT IS C; I 0 R" AND RIB ARE HYDROGEN, C3.7CYCIOALKVL ARYL, HET, CI-(,ALKOXV, CL-(,ALKYL OPTIONALLY SUBSTITUTED WITH HALO, CI-6ALKOXV, CYARIO, POLYHALOC,,,ALKOXY, C3-7CYCLOALKYL, ARYL, OR WITH HET; OR R" AND R LB TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED FORM A 4 TO 6 MEMBERED HETEROCYCLIC RING WHICH MAY BE OPTIONALLY SUBSTITUTED: L IS A DIRECT BOND, -0-, -0-CI-4ALKANEDIYL-, -0-CO-, -0-C(=O)-NR 5A OR 15 --0-C(=0)-NR"-CI4ALKANEDIYI-; R2 IS HYDROGEN, AND WHERE X IS C OR CH, R2 MAV ALSO BE CL-FIALKYL; R 3IS HYDROGEN, CL-TALKVI, CJ_6ALKOXYCL_(,ALKYI, CI-7CYCLOALKYL, AMINO, MONO- OR DIC,-6A]KYLAMINO; R 4IS ARYL OR A SATURATED, A PARTIALLY UNSATURATED OI- COMPLETELY UNSATURATED 5 OR 6 20 MEMBERED MONOCYCLIE OR 9 TO I 2 I-NEIRIBERC.1 VS'EM WHEREIN SAID RING SYSTEM CONTAINS ONE NITROGEN, AND OPTIONALLY ONE TO THREE ADDITIONAL HETEROATOMS SELECTED FROM 0, S AND N, AND WHEREIN THE REMAINING RING MEMBERS ARE CARBON ATOMS; WHEREIN SAID RING SYSTEM MAY BE OPTIONALLY SUBSTITUTED@ N IS 3, 4, 5, OR 6; P IS I OR 2-, 25 ARVI IS PHENYL, NAPHTHYL, INDANYL, OR 1.2,3,4-LETRAHYDRONAPHLHYL, EACH OF WHICH MAY BE OPTIONALLY SUBSTITUTED WITH ONE. TWO OR THREE SUBSTITUENM AND HET IS A 5 OR 6 MEMBERED SATURATED, PARTIALLY UNSATURATED OR COMPLETELY UNSALUR3LED HETEROCYCLIC RING CONTAINING I TO 4 HELLEROALORRIS SELECTED FROM N, 0 AND S, BEING OPTIONALLY CONDENSED WITH A BENZENE RING, AND WHEREIN HET INAY BE OPTIONAILY 30 SUBSTITUTED WITH ONE, TWO OR THREE SUBSTITUENTS:

30. 发明专利

MX2009008541A FENILCARBAMATOS MACROCICLICOS QUE INHIBEN EL VIRUS DE HEPATITIS C. 未知
公开(公告)号：MX2009008541A
公开(公告)日：2009-08-18
申请号：MX2009008541
申请日：2008-02-08
申请人： TIBOTEC PHARM LTD
发明人： RABOISSON PIERRE JEAN-MARIE BERNARD , BELFRAGE ANNA KARIN GERTRUD LINNEA , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTINA , ANTONOV DMITRY , JOENSSON CARL ERIK DANIEL , AYESA ALVAREZ SUSANA , MC GOWAN DAVID CRAIG
IPC分类号： C07D245/04 , A61K31/538 , A61P31/14 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
摘要： Compuestos de la fórmula I: (ver fórmula (I)) incluyendo un estereoisómero del mismo, o un N-óxido; una sal de adición farmacéuticamente aceptable o un solvato de adición farmacéuticamente aceptable de los mismos; útiles como inhibidores de HCV; procedimientos para preparar estos compuestos así como composiciones farmacéuticas que comprenden estos compuestos como ingrediente activo.

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