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51. 发明专利

ES2257066T3 PEPTIDOS INHIBIDORES DE LA HEPATITIS C. 未知
公开(公告)号：ES2257066T3
公开(公告)日：2006-07-16
申请号：ES99938085
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , BAILEY MURRAY D , CAMERON DALE , GHIRO ELISE , GOUDREAU NATHALIE , POUPART MARC-ANDRE
IPC分类号： C12N15/09 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K38/55 , A61K45/00 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07K1/10 , C07K5/10 , C07K5/107 , C07K7/06 , C07K14/81 , G01J5/20 , G01V8/00 , H01Q5/00 , H01Q21/06
摘要： Un compuesto de fórmula (I), incluyendo los racematos, diaestereoisómeros e isómeros ópticos: en la que a es 0 ó 1; b es 0 ó 1; Y es H o alquilo C1-C6; B es H, un derivado de acilo de fórmula R7-C(O)- o un sulfo nilo de fórmula R7-SO2, en la que R7 es (i) alquilo C1-10 opcionalmente sustituido con carboxilo, alcanoiloxi C1-C6 o alcoxi C1-6; (ii) cicloalquilo C3-7 opcionalmente sustituido con carboxilo, (alcoxi C1-6)carbonilo o fenilmetoxicarbonilo; (iii) arilo C6 o C10 o aralquilo C7-16 opcionalmente sustituido con alquilo C1-6, hidroxi o amino opcionalmente sustituido con alquilo C1-C6; o (iv) Het opcionalmente sustituido con alquilo C1-6, hidroxi, amino opcionalmente sustituido con alquilo C1-6, o amido opcionalmente sustituido con alquilo C1-6; R6 es alquilo C1-6 sustituido con carboxilo; R5 es alquilo C1-6 opcionalmente sustituido con carboxilo; R4 es alquilo C1-10, cicloalquilo C3-7 o (alquilcicloalquilo)C4-10; R3 es alquilo C1-C10, cicloalquilo C3-C7 o (alquilcicloalquilo)C4-C10; R2 es CH2-R20, NH-R20, O-R20 o S-R20, en donde R20 es un cicloalquilo C3-7 saturado o insaturado o (alquilcicloalquilo)C4-10 que está opcionalmente mono-, di- o tri-sustituido con R21.

52. 发明专利

ES2241157T3 PEPTIDOS INHIBIDORES DE LA HEPATITIS C. 未知
公开(公告)号：ES2241157T3
公开(公告)日：2005-10-16
申请号：ES98939450
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , POUPART MARC-ANDRE , RANCOURT JEAN , SIMONEAU BRUNO , TSANTRIZOS YOULA , WERNIC DOMINIK
IPC分类号： A61K38/00 , A61K38/21 , A61P1/16 , A61P31/12 , C07K5/078 , C07K5/083 , C07K5/103 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/18 , A61K38/04 , A61K38/16
摘要： La invención se refiere a un compuesto activo contra el virus de la hepatitis C, el cual corresponde a la fórmula (I) donde Q representa CH{sub,2}, a es igual a =, b es igual a = y B representa un derivado de amido. Cuando Q representa N-Y donde Y representa H o alquilo C{sub,1-6}, B representa un derivado de acilo. R{sup,6}, cuando está presente, representa un alquilo C{sub,1-6} opcionalmente sustituido por un carboxilo. Cuando Q representa CH{sub,2} o N-Y, Z representa oxi o tioxo. R{sup,4} representa un alquilo C{sub,1-10}, un cicloalquielo C{sub,3-7} o un (alquilcicloalquilo) C4-10. R{sup,3} representa un alquilo C1-10 opcionalmente sustituido por un carboxilo, un cicloalquilo C3-/ o un (alquilcicloalquilo) C4-10. W representa un derivado de prolina, mientras que R{sup,1}'' representa hidrógeno y que R{sup,1} representa un alquilo C{sub,1-6} opcionalmente sustituido por un tiol. R{sup,1} también puede representar alquenilo C{sub,1-6}, o R{sup,1}'' y R{sup,1} pueden ambos formar un anilloque comprende de 3 a 6 elementos. A representa finalmente hidroxi. Esta invención se refiere también a una sal o a un éster de este compuesto farmacéuticamente aceptables.

53. 发明专利

DE69827956T2 未知
公开(公告)号：DE69827956T2
公开(公告)日：2005-04-14
申请号：DE69827956
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , BAILEY DOUGLAS , HALMOS TEDDY , POUPART MARC-ANDRE , TSANTRIZOS YOULA
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/21 , A61P31/14 , C07K7/06 , C07K14/18 , C07K5/107 , C07K5/093 , A61K38/16 , A61K38/04
摘要： Compound of formula (I) active against the Hepatitis C virus: wherein B is an acyl derivative; a is 0 or 1; R6, when present, is carboxy(lower)alkyl; b is 0 or 1; R5, when present, is C1-6 alkyl, or carboxy (lower)alkyl; Y is H or C1-6 alkyl; R4 is C1-10 alkyl; R3 is C1-10 alkyl; W is -NH-CH(R2)-C(O)-, wherein R2 is C1-6 alkyl; C6 or C10 aryl; C7-16 aralkyl; or carboxy (lower)alkyl; or W is a proline derivative; Q is a group of the formula -Z(R1)-C(O)-R13, wherein Z is CH or N; R1 is C1-6 alkyl or C1-6 alkenyl both optionally substituted with thio or halo,; and R13 is an activated carbonyl substituent, or Q is a phosphonate group of the formula -CH(R1)-P(O)R15R16 wherein R15 and R16 are independently C6-20 aryloxy; and R1 is as defined above.

55. 发明专利

BR0211360A 未知
公开(公告)号：BR0211360A
公开(公告)日：2004-07-13
申请号：BR0211360
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , C07D403/12
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, N R 1 , or C R 1 , wherein R 1 is defined herein; ----- represents either a single or a double bond; R 2 is selected from: H, halogen, R 21 , O R 21 , S R 21 , COO R 21 , SO 2 N( R 22 ) 2 , N( R 22 ) 2 , , CON( R 22 ) 2 , N R 22 C(O) R 22 or N R 22 C(O)N R 22 wherein R 21 and each R 22 is defined herein; B is N R 3 or C R 3 , with the proviso that one of A or B is either C R 1 or C R 3 , wherein R 3 is defined herein; K is N or C R 4 , wherein R 4 is defined herein; L is N or C R 5 , wherein R 5 has the same definition as R 4 ; M is N or C R 7 , wherein R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N( R 6a ) R 6 or O R 6 , wherein R 6a is H or alkyl or N R 61 R 62 wherein R 61 and R 62 are defined herein; and R 6 is H, alkyl, cycloalkyl, alkenyl, Het , alkyl-aryl, alkyl- Het ; or R 6 is wherein R 7 and R 8 and Q are as defined herein; Y 2 is O or S; R 9 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl, aryl, Het , (C 1-6 )alkyl-aryl or (C 1-6 )alkyl- Het , all of which optionally substituted with R 90 ; or R 9 is covalently bonded to either of R 7 or R 8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

56. 发明专利

EA003906B1 ТРИПЕПТИДНЫЕ ИНГИБИТОРЫ ВИРУСА ГЕПАТИТА C 未知
公开(公告)号：EA003906B1
公开(公告)日：2003-10-30
申请号：EA200100228
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , BAILEY MURRAY D , CAMERON DALE , FAUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , POUPART MARC-ANDRE , RANCOURT JEAN , TZANTRIZOS YOULA , WERNIC DOMINIK , SIMONEAU BRUNO
IPC分类号： C12N15/09 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/06 , A61K38/21 , A61P1/16 , A61P31/12 , A61P31/14 , C07C229/48 , C07K1/06 , C07K5/08 , C07K5/083 , C07K5/087 , C12N9/50 , C12N9/99 , C12P21/02 , C12P41/00
摘要： Визобретенииописанырацематы, диастериоизомерыи оптическиеизомерыформулы (I), гдеВ обозначаетН, С- илиСарил, C-C-аралкил, Het или (низш.)алкил-Het, всенеобязательнозамещенные C-C-алкилом, C-C-алкоксигруппу, C-C-алканоил, гидроксигруппу, гидроксиалкил, галоген, галоалкил, нитро-, цианогруппу, цианалкил, аминогруппу, необязательнозамещенную C-C-алкилом, амидогруппуили (низш.)алкиламидилиВ обозначаетацильноепроизводноеформулы R-C(O)-, карбоксилформулы R-О-С(О)-, амидформулы R-N(R)-C(O)-, тиоамидформулы R-N(R)-C(S)-илисульфонилформулы R-SO, где RобозначаетН или C-C-алкил, и Y обозначаетН или C-C-алкил, Rобозначает C-C-алкил, C-C-циклоалкилили C-C-алкилциклоалкил, всенеобязательнозамещенныегидрокси-, C-C-алкоксигруппой, C-C-тиоалкилом, амидо-, (низш.)алкиламидогруппой, С-илиСариломили C-C-аралкилом, Rобозначает CH-R, NH-R, O-Rили S-R, где Rобозначаетнасыщенныйилиненасыщенный C-C-циклоалкилили C-C(алкилциклоалкил), необязательномоно-, ди- илитризамещенныйрадикалом R, или RобозначаетС- илиСарилили C-C-аралкил, необязательнозамещенный, или Rобозначает Het или (низш.)алкил-Het, обанеобязательнозамещенные, Het или (низш.)алкил-Het, карбоксил, карбокси(низш.)алкил, C- илиСарил, C-C-аралкилили Het, гдеарил, аралкилили Het являютсянеобязательнозамещенными, и RобозначаетН, C-C-алкил, C-C-циклоалкил, C-C-алкенилили C-C-алкинил, всенеобязательнозамещенныегалогеном, иихфармацевтическиприемлемыесолии сложныеэфиры.

57. 发明专利

CA2450033A1 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH HETEROBICYCLIC STRUCTURE 未知
公开(公告)号：CA2450033A1
公开(公告)日：2003-02-06
申请号：CA2450033
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： RANCOURT JEAN , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , KUKOLJ GEORGE , BEAULIEU PIERRE LOUIS , FAZAL GULREZ
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , A61K31/4402
摘要： An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represent ed by formula (I) wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein ; represents either a single or a double bond;R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein;B is NR3 or CR3, wit h the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein;K is N or CR4, wherein R4 is defined herein;L is N or CR5, wherein R5 has the same definition as R4 defined above;M is N or CR7, wherein R7 has th e same definition as R4 defined above;Y1 is O or S;Z is N(R6a)R6 or OR6, where in R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein;a salt o r a derivative thereof, as an inhibitor of HCV NS5B polymerase.

58. 发明专利

CA2449180A1 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH A HETEROBICYCLIC STRUCTURE 未知
公开(公告)号：CA2449180A1
公开(公告)日：2003-02-06
申请号：CA2449180
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS YOULA S , RANCOURT JEAN , KUKOLJ GEORGE , GOULET SYLVIE , POUPART MARC-ANDRE , POIRIER MARTIN , GILLARD JAMES , JOLICOEUR ERIC , FAZAL GULREZ , BEAULIEU PIERRE LOUIS
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , C07D513/04 , C07D487/04 , C07D498/04 , C07D403/12 , A61K31/34 , A61K31/395 , A61K31/4353 , A61K31/44 , A61K31/495
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represente d by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond;R2 is selected from: H, halogen, R21, OR21, SR21, COOR21,SO2N(R22)2, N(R22)2, , CON(R22)2,NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, wi th the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het;or R6 is wherein R7 and R8 a nd Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalk yl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl- Het, all of which optionally substituted with R90; or R9 is covalently bonde d to either of R7 or R8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

59. 发明专利

AU757072B2 Hepatitis C inhibitor peptide analogues 未知
公开(公告)号：AU757072B2
公开(公告)日：2003-01-30
申请号：AU8846698
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , BAILEY MURRAY DOUGLAS , HALMOS TEDDY , POUPART MARC-ANDRE , TSANTRIZOS YOULA
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/21 , A61P31/14 , C07K7/06 , C07K14/18 , A61K38/08
摘要： Compound of formula (I) active against the Hepatitis C virus: wherein B is an acyl derivative; a is 0 or 1; R6, when present, is carboxy(lower)alkyl; b is 0 or 1; R5, when present, is C1-6 alkyl, or carboxy (lower)alkyl; Y is H or C1-6 alkyl; R4 is C1-10 alkyl; R3 is C1-10 alkyl; W is -NH-CH(R2)-C(O)-, wherein R2 is C1-6 alkyl; C6 or C10 aryl; C7-16 aralkyl; or carboxy (lower)alkyl; or W is a proline derivative; Q is a group of the formula -Z(R1)-C(O)-R13, wherein Z is CH or N; R1 is C1-6 alkyl or C1-6 alkenyl both optionally substituted with thio or halo,; and R13 is an activated carbonyl substituent, or Q is a phosphonate group of the formula -CH(R1)-P(O)R15R16 wherein R15 and R16 are independently C6-20 aryloxy; and R1 is as defined above.

60. 发明专利

NZ503262A Hepatitis C NS3 protease inhibitor peptides and peptide analogues 未知
公开(公告)号：NZ503262A
公开(公告)日：2002-10-25
申请号：NZ50326298
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： WERNIC DOMINIK , TSANTRIZOS YOULA , LLINAS-BRUNET MONTSE , POUPART MARC-ANDRE , RANCOURT JEAN , SIMONEAU BRUNO
IPC分类号： A61K38/00 , A61K38/21 , A61P1/16 , A61P31/12 , C07K5/078 , C07K5/083 , C07K5/103 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/18 , A61K38/08
摘要： A compound of formula (I), wherein; Q is CH2 or N-Y, wherein Y is H or alkyl; a) when Q is CH2, a is 0, b is 0, and B is an amide derivative of formula R11aN(R11b)-C(O)- wherein R11a is H; alkylcycloalkyl optionally substituted with carboxy; alkoxycarbonyl; arylakyl; 2-tetrahydrofuranylmethyl; thienylmethyl; thiazolidylmethyl; alkyl optionally substituted with carboxyl or dialkylamino; cycloalkyl;aryl;alkylaryl; cycloalkylalkyl; heterocyclealkyl; R11b is alkyl substituted with carboxyl, alkoxycarbonyl or phenylmethoxycarbonyl; aralkyl substituted on the aromatic portion with carboxyl, alkoxycarbonyl, phenylmethoxycarbonyl or heterocyclealkyl; or R11a and R11b jointly form an optionally substituted 3 to 7-membered nitrogen-containing ring; or b) when Q is N-Y; a and b are 0 or 1, and B is of formula R11-C(O)-wherein R11 is (i) alkyl optionally substituted with carboxyl, alkanoyloxy or alkoxy; (ii) cycloalkyl optionally substituted with carboxyl, alkoxycarbonyl or phenylmethoxycarbonyl; (iii) cycloalkyl substituted with carboxyl and one to three alkyl substituents; (iv) optionally substituted alkylcycloalkyl; (v) a compound (A); or (iv)optionally substituted aryl or alkyl; R6 and R6 are alkyl substituted with carboxyl; or c) when Q is either CH2 or N-Y-; R4 is alkyl, cycloalkyl or alkylcycloalkyl; Z is oxo or thioxo; R3 is optionally substituted alkyl; W is a group of formula (II), wherein R2 is alkyl, aryl, aralkyl or optionally substituted cycloalkyl; or W is a group of formula (II') wherein X is CH or N; R2' is an optionally substituted alkylene which forms a ring with the attached carbon atom and X; or X is CH or N and R2 is alkylene which forms a ring with X and the attached carbon and fused to a second optionally substituted ring; R1' is H; R1 is alkenyl or optionally substituted alkyl or R1 and R1' together form an optionally substituted 3-6 membered ring; and A is hydroxy or salt thereof.

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