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1. 发明专利

BRPI0614654B1 inibidores macrocíclicos de vírus de hepatite c 未知
公开(公告)号：BRPI0614654B1
公开(公告)日：2019-03-12
申请号：BRPI0614654
申请日：2006-07-28
申请人： JANSSEN R & D IRELAND , JANSSEN SCIENCES IRELAND UC , MEDIVIR AB , TIBOTEC PHARM LTD , TIBOTEC PHARM LTD
发明人： ABDELLAH TAHRI , ANNA KARIN GERTRUD LINNEA BELFRAGE , ASA ANNICA KRISTINA ROSENQUIST , BENGT BERTIL SAMUELSSON , DOMINIQUE LOUIS NESTOR GHISLAIN SURLERAUX , HERMAN AUGUSTINUS DE KOCK , KARL MAGNUS NILSSON , KENNETH ALAN SIMMEN , LILI HU , MICHAEL PELCMAN , PER-OLA MIKAEL JOHANSSON , PIERRE JEAN-MARIE BERNARD RABOISSON , SANDRINE MARIE HELENE VENDEVILLE , VLADIMIR IVANOV
IPC分类号： A61K31/33 , A61K38/05 , A61P31/14 , C07D245/04 , C07D487/04 , C07K5/06 , C07K5/078
摘要： inibidores macrocíclicos de vírus de hepatite c. a presente invenção refere-se a inibidores de replicação de hcv de fórmula (i) e os n-óxidos, sais, e estereoisômeros, em que cada linha tracejada representa uma ligação dupla opcional; x e n, ch e onde x contém uma ligação dupla ele é c; r^1^ é -or^7^, -nh-so~2~r^8^; r^2^ é hidrogênio, e onde x é c ou ch, r^2^ também pode ser c~1-6~alquila, r^3^ é hidrogênio, c~1-6~alquila, c~1-6~alcóxic~1-6~alquila, c~3-7~cicloalquila; r^4^ é arila ou het, n é 3, 4, 5 ou 6; r^5^ é halo, c~1-6~ alquila, hidróxi, c~1-6~alcóxi, fenila, ou het; r^6^ é c~1-6~alcóxi, ou dimetilamino; r^7^ é hidrogênio; arila; het; c~3-7~cicloalquila opcionalmente substituída com c~1-6~ alquila; ou c~1-6~alquila opcionalmente substituída com c~3-7~cicloalquila, arila ou com het; r^8^ é arila; het; c~3-7~cicloalquila opcionalmente substituída com c~1-6~alquila; ou c~1-6~alquila opcionalmente substituída com c~3-7~cicloalquila, arila ou com het; arila é fenila opcionalmente substituída com um, dois ou três substituintes; het é um anel heterocíclico parcialmente insaturado ou completamente saturado, saturado, de 5 ou 6 membros, contendo 1 a 4 heteroátomos selecionados dentre nitrogênio, oxigênio e enxofre, e sendo opcionalmente susbstituído com um, dois, ou três substituintes; composições farmacêuticas contendo compostos (i) e processos para preparar compostos (i). combinações biodisponíveis dos inibidores de hcv de fórmula (i) com ritonavir são também providas.

3. 发明专利

MY151026A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY151026A
公开(公告)日：2014-03-31
申请号：MYPI20063670
申请日：2006-07-28
申请人： MEDIVIR AB , TIBOTEC PHARM LTD
发明人： SIMMEN KENNETH ALAN , SAMUELSSON BENGT BERTIL , ROSENQUIST ÅSA ANNICA KRISTINA , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJÖRN OLOF , KOCK HERMAN AUGUSTINUS DE , RABOISSON PIERRE JEAN-MARIE , LILI HU , LINDQUIST KARIN CHARLOTTA , LINDSTRÖM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LINNEA , WÄHLING HORST JÜRGEN , NILSSON KARL MAGNUS
IPC分类号： C07D417/04
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, C?-C?ALKYL, C?-C?ALKYLENECARBOCYCLYL, C?-C?ALKYLENE-HETEROCYCLYL; R² IS C?-C?ALKYL, C?-C?ALKYLENECARBOCYCLYL, C?-C?ALKYLENEHETEROCYCLYL; 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 C?-C?ALKYL; Rr IS QUINAZOLINYL, OPTIONALLY SUBSTITUTED WITH ONE TWO OR THREE SUBSTITUENTS EACH INDEPENDENTLY SELECTED FROM C?-C?ALKYL, C?-C?ALKOXY, HYDROXYL, HALO, HALOC?-C?ALKYL, AMINO, MONO- OR DIALKYLAMINO, MONO- OR DIALKYLAMINOCARBONYL, C?-C?ALKYL-CARBONYLAMINO, C?-C?ALKYLENECARBOCYCLYL AND C?-C?ALKYLENEHETEROCYCLYL; R? IS HYDROGEN, C?-C?ALKYL, C?-C?ALKOXYC?-C?ALKYL OR C?-C?CYCLOALKYL; R? IS HYDROGEN, C?-C?ALKYL, C?-C?ALKOXY, C?-C?ALKYLENECARBOCYCLYL, C?-C?ALKYLENEHETEROCYCLYL, HYDROXY, BROMO, CHLORO OR FLUORO HAVE UTILITY IN THE TREATMENT OR PROPHYLAXIS OF FLAVIVIRAL INFECTIONS SUCH AS HCV.

4. 发明专利

CR9783A INHIBIDORES MACROCICLICOS DEL VIRUS DE LA HEPATITIS C 未知
公开(公告)号：CR9783A
公开(公告)日：2008-09-09
申请号：CR9783
申请日：2008-02-29
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： PIERRE JEAN-MARIE BERNARD RABOISSON , HERMAN AGUSTINUS DE KOCK , LILI HU , SANDRINE MARIE HELENE VENDEVILLE , ABDELLAH TAHRI , DOMINIQUE LOUIS NESTOR GHISLAIN SURLERAUX , KENNETH ALAN SIMMEN , KARL MAGNUS NILSSON , BENGT BERTIL SAMUELSSON , ASA ANNICA ROSENQUIST , VLADIMIR IVANOV , MICHAEL PELCAM , ANNA KARIN GERTRUD LINNEA BELFRAGE , PER-OLA MIKAEL JOHANSSON
IPC分类号： A61K31/33 , A61K38/05 , A61P31/14 , C07D245/04 , C07D487/04 , C07K5/06 , C07K5/078
摘要： Inhibidores de la replicacion del VHC de formula (I) y los N-oxidos, sales y estereoisomeros, donde cada linea punteada representa un doble enlace opcional; X es N, CH y cuando X posee un doble enlace es C; R1 es -OR7, -NH-SO2R8; R2 es hidrogeno y cuando X es C o CH, R2 tambien puede ser alquilo C1-6; R3 es hidrogeno, alquilo C1-6-alquilo C1-6, cicloalquilo C3-7; R4 es arilo O Het, n es 3, 4, 5 o 6; R5 es halo, alquilo C-6, hidroxi, alcoxi C1-6, fenilo o Het; R6 es alcoxi C1-6 o dimetilamino; R7 es hidrogeno; arilo; Het; cicloalquilo C3-7 sustituido opcionalmente con alquilo C1-6; o alquilo C1-6 sustituido opcionalmente con cicloalquilo C3-7, arilo o con Het; R8 es arilo; Het.

5. 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

6. 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:

7. 发明专利

MY144217A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY144217A
公开(公告)日：2011-08-15
申请号：MYPI20063669
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB
发明人： RABOISSON PIERRE JEAN-MARIE , ROSENQUIST ASA ANNICA KRISTINA , IVANOV VLADIMIR , PELCMAN MICHAEL , BELFRAGE ANNA KARIN GERTRUD LINNEA , JOHANSSON PER-OLA MIKAEL , KOCK HERMAN AUGUSTINUS DE , LILI HU , VENDEVILLE SANDRINE MARIE HELENE , TAHRI ABDELLAH , SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN , SIMMEN KENNETH ALAN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL
IPC分类号： C07D487/04
摘要： MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 5 INHIBITORS OF HCV REPLICATION OF FORMULA (1) / R5 ZWC366_C7 R6 R 4 0 R2 _11 OZZ@ 0 N R3' R1 AND THEAL-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; I 0 R' IS -OR', -NH-SO2R8 ; *2IS HYDROGEN, AND WHERE X IS C OR CH, R 2MAY ALSO BE CI-6ALK-YI., *3IS HYDROGEN, C1_6ALKYL, C1-6ALKOXYCI-6ALKYL, C3-7CN'CLOA1KV1; R4IS ARYL OR HET; N IS 3), 4, 5, OR 6; RS IS HALO, C1-6ALKYL, HYDROXY, CI-6ALKOXY, PHERTYL. OR HET; 6 IS 1 5 R CI-6ALKOXY, OR DIMETHYLAMINO; R7 IS HYDROGEN- ARYL; HET; C3-7CYCLOALKYL OPTIONALLY SUBSTITUTED WITH CI-6ALKVL; OR 7 . I CI-6ALKVL OPTIONALLY SUBSTITUTED WITH C3-7CICLOALKVL, ARVI OR WITH LIET@ R8 IS ARYL; HET; C3-7CYCLOALKYL OPTIONALLY SUBSTITUTED WITH CI-6ALKYL-, OR CI-6A]KVL OPTIONALLY SUBSTITUTED WITH C3-7CYCLOALKYL, ARYL OR WITH HET; 20 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 FING CONTAINING I TO 4 HETEROATONIS SELECTED FROM NITROGEN, OXYGEN AND SULFUR, AND BEING OPTIONALLY SUBSTITUTED WITH ONE. TWO OR THREE SUBSTITUENTS PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS (1) AND PROCESSES FOR PREPARING

9. 发明专利

MY152153A MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 未知
公开(公告)号：MY152153A
公开(公告)日：2014-08-15
申请号：MYPI20063671
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD
发明人： RABOISSON PIERRE JEAN-MARIE , KOCK HERMAN AUGUSTINUS DE , VENDEVILLE SANDRINE MARIE HELENE , LILI HU , VREKEN WIM VAN DE , GOWAN DAVID GRAIG MC , TAHRI ABDELLAH , SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN , SIMMEN KENNETH ALAN
IPC分类号： C07D487/04
摘要： INHIBITORS OF HCV OF FORMULA (I) AND THE N-OXIDES, SALTS, AND STEREOCHEMICALLY ISOMERIC FORMS THEREOF, WHEREIN R1 IS ARYL OR A SATURATED, A PARTIALLY UNSATURATED OR COMPLETELY UNSATURATED 5 OR 6 MEMBERED MONOCYCLIC OR 8 TO 12 MEMBERED BICYCLIC HETEROCYCLIC RING SYSTEM CONTAINING ONE NITROGEN, AND OPTIONALLY ONE TO THREE OXYGEN, SULFUR OR NITROGEN, WHEREIN SAID RING SYSTEM MAY BE OPTIONALLY SUBSTITUTED; L IS A DIRECT BOND, -O-, -O-C1-4ALKANEDIYL-, -O-CO-, -0-C(=O)-NR5a- OR -O-C(=O)-NR5a-C1-4ALKANEDIYL-; R2 IS HYDROGEN, -OR6, -C(=O)OR6, -C(=O)R7, -C(=O)NR5aR5b, -C(=O)NHR5c, -NR5aR5b, -NHR5c, -NHSOpNR5aR5b, -NR5aSOpR8, OR -B(OR6)2: R3 AND R4 ARE HYDROGEN OR C1-6ALKYL; OR R3 AND R4 TAKEN TOGETHER MAY FORM A C3-7CYCLOALKYL RING; N IS 3, 4, 5, OR 6; P IS 1 OR 2; ARYL IS PHENYL, NAPHTHYL, INDANYL, OR 1,2,3,4-TETRAHYDRONAPHTHYL, EACH OF WHICH MAY BE OPTIONALLY SUBSTITUTED HET IS A 5 OR 6 MEMBERED SATURATED, PARTIALLY UNSATURATED OR COMPLETELY UNSATURATED HETEROCYCLIC RING CONTAINING 1 TO 4 HETEROATOMS EACH INDEPENDENTLY SELECTED FROM NITROGEN, OXYGEN AND SULFUR, BEING OPTIONALLY CONDENSED WITH A BENZENE RING, AND WHEREIN THE GROUP HET AS A WHOLE MAY BE OPTIONALLY SUBSTITUTED; 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.

10. 发明专利

UY30922A1 1,1-DIOXO-1-TIA-5,10-DIAZADIBENZOCICLOHEPTENOS UTILES COMO INHIBIDORES DEL VIRUS DE LA HEPATITIS C" 未知
公开(公告)号：UY30922A1
公开(公告)日：2008-09-02
申请号：UY30922
申请日：2008-02-15
申请人： TIBOTEC PHARM LTD
发明人： ABDELLAH TAHRI , JULIEN LAST STEFAAN , KLARA ROMBAUTS , DAVID CUMMINGS MAXWELL , MATHILDE VAN DEN BROECK WALTER , LILI HU , JALES LORY PEDRO MIGUL , MAURICE BOUTTON CARLO WILLY , EDUARD AMSSOMS KATIE INGRID , HELENE VENDEVILLE SANDRINE MARIE , CRAIG MCGOWAN DAVID , NYANGUILE ORIGENE , VANDYCK KOEN , RABOISSON PIERRE JEAN-MARIE BERNARD
IPC分类号： A61K39/29 , A61P31/12 , C07D243/12 , C07D335/00 , C07D487/12
摘要： Inhibidores de la replicacion del VHC de la formula (I) sus estereoisomeros, profármacos, tautomeros, racémicos, sales, hidratos o solvatos donde R1a, R1b, R2, R3, R4a Y r4B tienen el significado definido en las reivindicaciones. La presente invencion además se rfiere a procesos para prepara dichos compuestos, composiciones farmacéuticas que los contienen y su uso en la terapia de VHC.

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