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11. 发明专利

IN211493B A COMPOUND OF FORMULA ( I ) 未知
公开(公告)号：IN211493B
公开(公告)日：2008-01-25
申请号：IN127MUN2001
申请日：2001-02-07
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： HALMOS TEDDY , SIMONEAU BRUNO , LLINAS-BRUNET MONTSE , POUPART MARC-ANDRE , RANCOURT JEAN , GOUDREAU NATHALIE , CAMERON DALE , BAILEY MURRAY D , GHIRO ELISE , WERNIC DOMINIK , FAUCHER ANNE MARIE , TSANTRIZOS YOULA S
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： Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C 6 or C 10 aryl, C 7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C 1-6 alkyl; C 1-6 alkoxy; C 1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C 1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R 4 -C(O)-; a carboxyl of formula R 4 -O-C(O)-; an amide of formula R 4 -N( R 5 )-C(O)-; a thioamide of formula R 4 -N( R 5 )-C(S)-;or a sulfonyl of formula R 4 -SO 2 ; R 5 is H or C 1-6 alkyl; and Y is H or C 1-6 alkyl; R 3 is C 1-8 alkyl, C 3-7 cycloalkyl, or C 4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C 1-6 alkoxy, C 1-6 thioalkyl, amido, (lower alkyl)amido, C 6 or C 10 aryl, or C 7-16 aralkyl; R 2 is CH 2 - R 20 , NH- R 20 , O- R 20 or S- R 20 , wherein R 20 is a saturated or unsaturated C 3-7 cycloalkyl or C 4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or trisubstituted with R 21 , or R 20 is a C 6 or C 10 aryl or C 7-14 aralkyl optionally substituted, or R 20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C 6 or C 10 aryl, C 7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R 1 is H; C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, or C 2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

12. 发明专利

EE04816B1 未知
公开(公告)号：EE04816B1
公开(公告)日：2007-04-16
申请号：EEP200100516
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS YOULA S , CAMERON DALE R , FAUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , LLINAS-BRUNET MONTSE
IPC分类号： A61K38/05 , A61K45/00 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/06 , A61K38/12 , A61K38/21 , A61K38/43 , A61K38/46 , A61P1/16 , A61P31/14 , A61P43/00 , C07K5/078 , C07K5/08 , C07K5/097
摘要： Macrocyclic peptides (I) and their salts and esters are new. Macrocyclic peptides of formula (I) and their salts and esters are new. [Image] W = CH or N; R 21 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, hydroxy or N(R 23) 2; R 23 = H, 1-6C alkyl or 3-6C cycloalkyl; R 2 2 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C thioalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, 2-7C alkoxyalkyl, 3-6C cycloalkyl, 6C or 10C aryl or Het; Het = 5-7-membered optionally saturated heterocycle containing 1-4 N, O or S; cycloalkyl, aryl or Het are substituted by R 24; R 24 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, NO 2, N(R 25), NHC(O)R 25, NHC(O)NHR 25 or NH-C(O)-OR 26; R 2 5 = H, 1-6C alkyl or 3-6C cycloalkyl; R 26 = 1-6C alkyl or 3-6C cycloalkyl; R 3 = OH, NH 2 or NHR 31; R 31 = 6 or 10C aryl, heteroaryl, C(O)R 32, C(O)NHR or C(O)OR 32; R 32 = 1-6C alkyl or 3-6C cycloalkyl; D = 5-10-atom optionally saturated alkylene chain optionally containing 1-3 O, S or NR 41; R 41 = H, 1-6C alkyl, 3-6C cycloalkyl or C(O)R 42; R 42 = 1-6C alkyl, 3-6C cycloalkyl or 6 or 10C aryl; R 4 = H or 1-3 of 1-6C alkyl, 1-6C haloalkyl, 1-6C alkoxy, hydroxy, halo, amino, oxo, thio or 1-6C thioalkyl; A = C(O)NNHR 5 or a carboxylic acid; R 5 = 1-8C alkyl, 3-6C cycloalkyl, 6 or 10C aryl or 7-16C aralkyl. An independent claim is also included for the use of a composition comprising (I) in admixture with a carrier medium or an auxiliary for the manufacture of a medicament for treating hepatitis C viral infection in a mammal. ACTIVITY : Antiviral. MECHANISM OF ACTION : Selective inhibitors of NS3 protease of HCV. In an NS3 protease cell-based assay using Huh-7 cell, a human cell line derived from a hepatoma cotransfected with 2 DNA constructs, a compound of formula (Ia) exhibited an EC 50 value of less than 1 MicroM. [Image].

13. 发明专利

MY127538A HEPATITIS C INHIBITOR TRI-PEPTIDES 未知
公开(公告)号：MY127538A
公开(公告)日：2006-12-29
申请号：MYPI9903397
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , WERNIC DOMINIK , FAUCHER ANNE-MARIE , BAILEY MURRAY D , CAMERON DALE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , POUPART MARC-ANDRE , RANCOURT JEAN , TSANTRIZOS YOULA
IPC分类号： C07K5/083 , C12N15/09 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/06 , A61K38/21 , A61P1/16 , A61P31/12 , A61P31/14 , C07C229/48 , C07K1/06 , C07K5/08 , C07K5/087 , C12N9/50 , C12N9/99 , C12P21/02 , C12P41/00
摘要： RACEMATES, DIASTEREOISOMERS AND OPTICAL ISOMERS OF A COMPOUND OF FORMULA (&Igr;): WHEREIN B IS H, A C6 OR C10 ARYL, C7-16 ARALKYL; HET OR (LOWER ALKYL)-HET, ALL OF WHICH OPTIONALLY SUBSTITUTED WITH C1-6 ALKYL; C1-6 ALKOXY; C1-6 ALKANOYL; HYDROXY; HYDROXYALKYL; HALO: HALOALKYL; NITRO; CYANO; CYANOALKYL; AMINO OPTIONALLY SUBSTITUTED WITH C1-6 ALKYL; AMIDO; OR (LOWER ALKYL)AMIDE; OR B IS AN ACYL DERIVATIVE OF FORMULA R4-C(O)-; A CARBOXYL OF FORMULA R4-O-C(O)-; AN AMIDE OF FORMULA R4-NH-C(O)-; A THIOAMIDE OF FORMULA R4-N(R5)-C(S)-;OR A SULFONYL OF FORMULA R4-SO2; R5 IS H OR C1-6 ALKYL; AND Y IS H OR C1-6 ALKYL;R3 IS C1-8 ALKYL, C3-7 CYCLOALKYL, OR C4-10 ALKYLCYCLOALKYL, ALL OPTIONALLY SUBSTITUTED WITH HYDROXY, C1-6 ALKOXY, C1-6 THIOALKYL, AMIDO, (LOWER ALKYL)AMIDO, C6 OR C10 ARYL, OR C7-16 ARALKYL;R2 IS CH2-R20, NH-R20, O-R20 OR S-R20, WHEREIN R20 IS A SATURATED OR UNSATURATED C3-7 CYCLOALKYL OR C4-10 (ALKYLCYCLOALKYL), ALL OF WHICH BEING OPTIONALLY MONO-, DI- OR TRI-SUBSTITUTED WITH R21 OR R20 IS A C6 OR C10 ARYL OR C7-14 ARALKYL OPTIONALLY SUBSTITUTED, OR R20 IS HAT OR (LOWER ALKYL)-HET, BOTH OPTIONALLY SUBSTITUTED, HET OR (LOWER ALKYL)-HET; CARBOXYL; CARBOXY(LOWER ALKYL); C6 OR C10 ARYL, C7-14 ARALKYL OR HET, SAID ARYL, ARALKYL OR HAT BEING OPTIONALLY SUBSTITUTED; AND R1 IS H; C1-6 ALKYL, C3-7 CYCLOALKYL, ORC2-6 ALKENYL, ALL OPTIONALLY SUBSTITUTED WITH HALOGEN; OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ESTER THEREOF.

14. 发明专利

DE69929887D1 HEPATITIS C INHIBITOR PEPTIDE 未知
公开(公告)号：DE69929887D1
公开(公告)日：2006-04-20
申请号：DE69929887
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： LLINAS-BRUNET MONTSE , BAILEY D , CAMERON DALE , GHIRO ELISE , GOUDREAU NATHALIE , POUPART MARC-ANDRE , RANCOURT JEAN , TSANTRIZOS S
IPC分类号： C07K14/81 , 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 , G01J5/20 , G01V8/00 , H01Q5/00 , H01Q21/06
摘要： Formula (I) wherein a is 0 or 1; b is 0 or 1; Y is H or C1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative; W is hydroxy or a N-substituted amino; or a pharmaceutically acceptable salt or ester thereof, for use in the treatment of hepatitis C virus (HCV) infection.

15. 发明专利

IN127MU2001A Hepatitis C inhibitor tri-peptides 未知
公开(公告)号：IN127MU2001A
公开(公告)日：2005-03-04
申请号：IN127MU2001
申请日：2001-02-07
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： HALMOS TEDDY , SIMONEAU BRUNO , LLINAS-BRUNET MONTSE , POUPART MARC-ANDRE , RANCOURT JEAN , GOUDREAU NATHALIE , CAMERON DALE , BAILEY MURRAY D , GHIRO ELISE , WERNIC DOMINIK , FAUCHER ANNE MARIE , TSANTRIZOS YOULA S
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： Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C 6 or C 10 aryl, C 7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C 1-6 alkyl; C 1-6 alkoxy; C 1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C 1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R 4 -C(O)-; a carboxyl of formula R 4 -O-C(O)-; an amide of formula R 4 -N( R 5 )-C(O)-; a thioamide of formula R 4 -N( R 5 )-C(S)-;or a sulfonyl of formula R 4 -SO 2 ; R 5 is H or C 1-6 alkyl; and Y is H or C 1-6 alkyl; R 3 is C 1-8 alkyl, C 3-7 cycloalkyl, or C 4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C 1-6 alkoxy, C 1-6 thioalkyl, amido, (lower alkyl)amido, C 6 or C 10 aryl, or C 7-16 aralkyl; R 2 is CH 2 - R 20 , NH- R 20 , O- R 20 or S- R 20 , wherein R 20 is a saturated or unsaturated C 3-7 cycloalkyl or C 4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or trisubstituted with R 21 , or R 20 is a C 6 or C 10 aryl or C 7-14 aralkyl optionally substituted, or R 20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C 6 or C 10 aryl, C 7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R 1 is H; C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, or C 2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

16. 发明专利

SI1169339T1 MACROCYCLIC PEPTIDES INHIBITING THE HEPATITIS C VIRUS NS3 PROTEASE 未知
公开(公告)号：SI1169339T1
公开(公告)日：2005-02-28
申请号：SI200030555
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS YOULA S , CAMERON DALE R , FAUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , LLINAS-BRUNET MONTSE
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/12 , A61K38/21 , A61K38/43 , A61K38/46 , A61P1/16 , A61P31/14 , A61P43/00 , C07K5/078 , C07K5/08 , C07K5/097
摘要： Macrocyclic peptides (I) and their salts and esters are new. Macrocyclic peptides of formula (I) and their salts and esters are new. [Image] W = CH or N; R 21 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, hydroxy or N(R 23) 2; R 23 = H, 1-6C alkyl or 3-6C cycloalkyl; R 2 2 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C thioalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, 2-7C alkoxyalkyl, 3-6C cycloalkyl, 6C or 10C aryl or Het; Het = 5-7-membered optionally saturated heterocycle containing 1-4 N, O or S; cycloalkyl, aryl or Het are substituted by R 24; R 24 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, NO 2, N(R 25), NHC(O)R 25, NHC(O)NHR 25 or NH-C(O)-OR 26; R 2 5 = H, 1-6C alkyl or 3-6C cycloalkyl; R 26 = 1-6C alkyl or 3-6C cycloalkyl; R 3 = OH, NH 2 or NHR 31; R 31 = 6 or 10C aryl, heteroaryl, C(O)R 32, C(O)NHR or C(O)OR 32; R 32 = 1-6C alkyl or 3-6C cycloalkyl; D = 5-10-atom optionally saturated alkylene chain optionally containing 1-3 O, S or NR 41; R 41 = H, 1-6C alkyl, 3-6C cycloalkyl or C(O)R 42; R 42 = 1-6C alkyl, 3-6C cycloalkyl or 6 or 10C aryl; R 4 = H or 1-3 of 1-6C alkyl, 1-6C haloalkyl, 1-6C alkoxy, hydroxy, halo, amino, oxo, thio or 1-6C thioalkyl; A = C(O)NNHR 5 or a carboxylic acid; R 5 = 1-8C alkyl, 3-6C cycloalkyl, 6 or 10C aryl or 7-16C aralkyl. An independent claim is also included for the use of a composition comprising (I) in admixture with a carrier medium or an auxiliary for the manufacture of a medicament for treating hepatitis C viral infection in a mammal. ACTIVITY : Antiviral. MECHANISM OF ACTION : Selective inhibitors of NS3 protease of HCV. In an NS3 protease cell-based assay using Huh-7 cell, a human cell line derived from a hepatoma cotransfected with 2 DNA constructs, a compound of formula (Ia) exhibited an EC 50 value of less than 1 MicroM. [Image].

17. 发明专利

EA004765B1 ПЕПТИДНЫЕ ИНГИБИТОРЫ ВИРУСА ГЕПАТИТА C 未知
公开(公告)号：EA004765B1
公开(公告)日：2004-08-26
申请号：EA200100229
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 , RANCOURT JEAN , TRANTRIZOS YOULA S
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： Визобретенииописаносоединениеформулы (I), гдеа равно 0 или 1, b равно 0 или 1, Y обозначаетН илиС-Cалкил, ВобозначаетН, ацильноепроизводноеилисульфонильноепроизводное, W обозначаетгидроксиили N-замещеннуюаминогруппу, атакжеегофармацевтическиприемлемыесолиилисложныеэфиры. Такоесоединениеможетприменятьсядлялеченияинфекции, вызываемойвирусомгепатитаС (HCV).

18. 发明专利

ZA200107862B Macrocyclic peptides active against the hepatitis c virus. 未知
公开(公告)号：ZA200107862B
公开(公告)日：2004-06-30
申请号：ZA200107862
申请日：2001-09-25
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS YOULA STRATIGOULA , FAUCHER ANNE-MARIE , GOUDREAU NATHALIE , LLINAS-BRUNET MONTSE , CAMERON DALE R , GHIRO ELISE , HALMOS TEDDY
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/12 , A61K38/21 , A61K38/43 , A61K38/46 , A61P1/16 , A61P31/14 , A61P43/00 , C07K5/078 , C07K5/08 , C07K5/097 , A61K , A61P , C07K
摘要： Macrocyclic peptides (I) and their salts and esters are new. Macrocyclic peptides of formula (I) and their salts and esters are new. [Image] W = CH or N; R 21 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, hydroxy or N(R 23) 2; R 23 = H, 1-6C alkyl or 3-6C cycloalkyl; R 2 2 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C haloalkyl, 1-6C thioalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, 2-7C alkoxyalkyl, 3-6C cycloalkyl, 6C or 10C aryl or Het; Het = 5-7-membered optionally saturated heterocycle containing 1-4 N, O or S; cycloalkyl, aryl or Het are substituted by R 24; R 24 = H, halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkoxy, 3-6C cycloalkoxy, NO 2, N(R 25), NHC(O)R 25, NHC(O)NHR 25 or NH-C(O)-OR 26; R 2 5 = H, 1-6C alkyl or 3-6C cycloalkyl; R 26 = 1-6C alkyl or 3-6C cycloalkyl; R 3 = OH, NH 2 or NHR 31; R 31 = 6 or 10C aryl, heteroaryl, C(O)R 32, C(O)NHR or C(O)OR 32; R 32 = 1-6C alkyl or 3-6C cycloalkyl; D = 5-10-atom optionally saturated alkylene chain optionally containing 1-3 O, S or NR 41; R 41 = H, 1-6C alkyl, 3-6C cycloalkyl or C(O)R 42; R 42 = 1-6C alkyl, 3-6C cycloalkyl or 6 or 10C aryl; R 4 = H or 1-3 of 1-6C alkyl, 1-6C haloalkyl, 1-6C alkoxy, hydroxy, halo, amino, oxo, thio or 1-6C thioalkyl; A = C(O)NNHR 5 or a carboxylic acid; R 5 = 1-8C alkyl, 3-6C cycloalkyl, 6 or 10C aryl or 7-16C aralkyl. An independent claim is also included for the use of a composition comprising (I) in admixture with a carrier medium or an auxiliary for the manufacture of a medicament for treating hepatitis C viral infection in a mammal. ACTIVITY : Antiviral. MECHANISM OF ACTION : Selective inhibitors of NS3 protease of HCV. In an NS3 protease cell-based assay using Huh-7 cell, a human cell line derived from a hepatoma cotransfected with 2 DNA constructs, a compound of formula (Ia) exhibited an EC 50 value of less than 1 MicroM. [Image].

19. 发明专利

NZ515286A Macrocyclic peptides active against the hepatitis C virus 未知
公开(公告)号：NZ515286A
公开(公告)日：2004-02-27
申请号：NZ51528600
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS YOULA S , CAMERON DALE R , FAUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , LLINAS-BRUNET MONTSE
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/12 , A61K38/21 , A61K38/43 , A61K38/46 , A61P1/16 , A61P31/14 , A61P43/00 , C07K5/078 , C07K5/08 , C07K5/097
摘要： The present invention covers macrocyclic compounds of formula (I) active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus wherein W is CH or N; R21 is H, halo, C1-6 alkyl, cycloalkyl, haloalkyl, C1-6 alkoxy, cycloalkoxy, hydroxy, or N(R23)2, wherein each R23 is independently H, C1-6 alkyl or cycloalkoxy; and R22 is H, halo, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, C1-6 thioalkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C2-7 alkoxyalkyl, C3-6 cycloalkyl, C6 or 10 aryl or Het, wherein Het is a five-, six-, or seven-membered saturated or unsaturated heterocycle containing from one to four heteroatoms selected from nitrogen, oxygen and sulfur; said cycloalkyl, aryl or Het being substituted with R24, wherein R24 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, C3-6 cycloalkoxy, NO2, N(R25)2, NH-C(O)-R25; or NH-C(O)-NH-R25, wherein each R25 is independently: H, C1-6 alkyl or C3-6 cycloalkyl; or R24 is NH-C(O)-OR26 wherein R26 is C1-6 alkyl or C3-6 cycloalkyl; R3 is hydroxy, NH2, or a group of formula -NH-R31, wherein R31 is C6 or 10 aryl, heteroaryl, -C(O)-R32, -C(O)-OR32 or -C(O)-NHR32, wherein R32 is: C1-6 alkyl or C3-6 cycloalkyl; D is a 5 to 10-atom saturated or unsaturated alkylene chain optionally containing one to three heteroatoms independently selected from: O, S, or N-R41, wherein R41 is H, C1-6 alkyl, cycloalkyl or -C(O)-R42, wherein R42 is C1-6 alkyl, cycloalkyl or C6 or 10 aryl; R4 is H or from one to three substituents at any carbon atom of said chain D, said substituent independently selected from the group consisting of: C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, hydroxy, halo, amino, oxo, thio or C1-6 thioalkyl, and A is an amide of formula -C(O)-NH-R5, wherein R5 is selected from the group consisting of: C1-8 alkyl, C3-6 cycloalkyl, C6 or 10 aryl or C7-16 aralkyl; or A is a carboxylic acid or a pharmaceutically acceptable salt or ester thereof.

20. 发明专利

NZ510396A Hepatitis C inhibitor tri-peptides 未知
公开(公告)号：NZ510396A
公开(公告)日：2004-02-27
申请号：NZ51039699
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： RANCOURT JEAN , TSANTRIZOS YOULA S , WERNIC DOMINIK M , LINAS-BRUNET MONTSE , BAILEY MURRAY D , CAMERON DALE , AUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , ALMOS TEDDY , POUPART MARC-ANDRE
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： Racemates, diastereoisomers and optical isomers of a compound of formula (I) wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl) amide; or B is an acyl derivative of formula R4-C(O)-; a carboxyl of formula R4-O- C(O)-; an amide of formula R4-N(R5)-C(O)-; a thioamide of formula R4-N(R5)-C(S)-;or a sulfonyl of formula R4-SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7- 16 aralkyl; R2 is CH2-R20, NH-R20, O-R20or S-R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

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