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1. 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.

2. 发明专利

DE60014345D1 MAKROZYKLISCHE PEPTIDE ALS HEPATITIS C VIRUS NS3 PROTEASE INHIBITORE 未知
公开(公告)号：DE60014345D1
公开(公告)日：2004-11-04
申请号：DE60014345
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS S , CAMERON 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].

3. 发明专利

DE69929887T2 未知
公开(公告)号：DE69929887T2
公开(公告)日：2006-08-24
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.

4. 发明专利

DE60014345T2 未知
公开(公告)号：DE60014345T2
公开(公告)日：2005-02-17
申请号：DE60014345
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： TSANTRIZOS S , CAMERON 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].

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