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1. 发明公开

EP2028186A3 Hepatitis C inhibitor tri-peptides 有权
标题翻译：丙型肝炎三肽抑制剂
公开(公告)号：EP2028186A3
公开(公告)日：2009-04-01
申请号：EP08169026.5
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Simoneau, Bruno , Bailey, Murray D. , Llinas-Brunet, Montse , Cameron, Dale , Faucher, Anne-Marie , Wernic, Dominik M. , Goudreau, Nathalie , Poupart, Marc-André , Rancourt, Jean , Tsantrizos, Youla S. , Halmos, Teddy , Ghiro, Elise
IPC分类号： C07K5/083 , C07K5/087 , A61K38/06 , C07C229/48 , C12P41/00
CPC分类号： C12P13/02 , A61K38/21 , A61K45/06 , C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C12P41/005 , A61K2300/00
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.

2. 发明公开

EP1891951A1 Viral polymerase inhibitors 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：EP1891951A1
公开(公告)日：2008-02-27
申请号：EP07117984.0
申请日：2002-02-18
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Beaulieu, Pierre Louis , Fazal, Gulrez , Goulet, Sylvie , Kukolj, George , Poirier, Martin , Tsantrizos, Youla , Jolicoeur, Eric , Gillard, James , Poupart, Marc-André , Rancourt, Jean
IPC分类号： A61K31/404 , A61K31/381 , C07D417/14 , C07D403/12 , C07D209/08 , C07D405/12 , C07D405/14 , C07D401/14 , C07D409/14 , C07D413/14 , C07D405/04 , C07D401/04 , C07D417/04 , C07D409/04 , C07D413/04 , C07D403/04 , C07D471/04
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
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 NR 3 or CR 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 CR 4 , wherein R 4 is defined herein;
L is N or CR 5 , wherein R 5 has the same definition as R 4 ;
M is N or CR 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.
摘要翻译：由式I表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中：A是O，S，NR 1或CR 1，其中R 1如本文所定义; -----表示单键或双键; R2选自：H，卤素，R21，OR21，SR21，COOR21，SO2N（R22）2，N（R22）2，CON（R22）2，NR22C（O）R22或NR22C（O）NR22， R22在此定义; B是NR 3或CR 3，条件是A或B之一是CR 1或CR 3，其中R 3如本文所定义; K是N或CR 4，其中R 4如本文所定义; L是N或CR 5，其中R 5具有与R 4相同的定义; M是N或CR7，其中R7具有与R4相同的定义; Y1是O或S; Z是N（R6a）R6或OR6，其中R6a是H或烷基或NR61R62，其中R61和R62如本文所定义; 和R6是H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het; 或者R 6是其中R 7和R 8和Q如本文所定义; Y2是O或S; （C 1-6）烷基 - 芳基或（C 1-6）烷基 - （C 3-7）环烷基，芳基，Het，烷基-Het，其全部任选被R90取代; 或R9与R7或R8中的任一个共价键合以形成5-或6-元杂环; 其盐或衍生物作为HCV NS5B聚合酶的抑制剂。

3. 发明授权

EP2028186B1 Hepatitis C inhibitor tri-peptides 有权
标题翻译：丙型肝炎三肽抑制剂
公开(公告)号：EP2028186B1
公开(公告)日：2013-01-23
申请号：EP08169026.5
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Simoneau, Bruno , Bailey, Murray D. , Llinas-Brunet, Montse , Cameron, Dale , Faucher, Anne-Marie , Wernic, Dominik M. , Goudreau, Nathalie , Poupart, Marc-André , Rancourt, Jean , Tsantrizos, Youla S. , Halmos, Teddy , Ghiro, Elise
IPC分类号： C07K5/083 , C07K5/087 , A61K38/06 , C07C229/48 , C12P41/00
CPC分类号： C12P13/02 , A61K38/21 , A61K45/06 , C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C12P41/005 , A61K2300/00

4. 发明公开

EP2335700A1 Hepatitis C virus polymerase inhibitors with a heterobicylic structure 审中-公开
标题翻译：丙型肝炎病毒聚合酶抑制剂
公开(公告)号：EP2335700A1
公开(公告)日：2011-06-22
申请号：EP10185316.6
申请日：2002-02-18
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Beaulieu, Pierre Louis , Fazal, Gulrez , Goulet, Sylvie , Kukolj, George , Poirier, Martin , Tsantrizos, Youla , Jolicoeur, Eric , Gillard, James , Poupart, Marc-André , Rancourt, Jean
IPC分类号： A61K31/404 , A61K31/381 , C07D417/14 , C07D403/12 , C07D209/08 , C07D405/12 , C07D405/14 , C07D401/14 , C07D409/14 , C07D413/14 , C07D405/04 , C07D401/04 , C07D417/04 , C07D409/04 , C07D413/04 , C07D403/04 , C07D471/04
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
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.
摘要翻译：由式I表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中：A是O，S，N R 1或C R 1，其中R 1在本文中定义; -----表示单键或双键; R 2选自：H，卤素，R 21，OR 21，SR 21，COO R 21，SO 2 N（R 22）2，N（R 22）2，CON（R 22）2，NR 22 C （O）R 22或NR 22 C（O）NR 22，其中R 21和每个R 22在本文中定义; B是N R 3或C R 3，条件是A或B中的一个是C R 1或C R 3，其中R 3在本文中定义; K是N或C R 4，其中R 4在本文中定义; L是N或C R 5，其中R 5具有与R 4相同的定义; M是N或C R 7，其中R 7具有与R 4相同的定义; Y 1为O或S; Z是N（R 6a）R 6或O R 6，其中R 6a是H或烷基或N R 61 R 62，其中R 61和R 62在本文中定义; R 6为H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het; 或R 6是其中R 7和R 8和Q如本文所定义; Y 2为O或S; R 9是H，（C 1-6烷基），（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基，芳基，Het，（C 1-6）烷基 - 芳基或（C 1-6）烷基-Het，它们全部被R 90取代; 或R 9与R 7或R 8中的任一个共价键合以形成5-或6-元杂环; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

5. 发明公开

EP2028186A2 Hepatitis C inhibitor tri-peptides 有权
标题翻译：丙型肝炎三肽抑制剂
公开(公告)号：EP2028186A2
公开(公告)日：2009-02-25
申请号：EP08169026.5
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Simoneau, Bruno , Bailey, Murray D. , Llinas-Brunet, Montse , Cameron, Dale , Faucher, Anne-Marie , Wernic, Dominik M. , Goudreau, Nathalie , Poupart, Marc-André , Rancourt, Jean , Tsantrizos, Youla S. , Halmos, Teddy , Ghiro, Elise
IPC分类号： C07K5/083 , C07K5/087 , A61K38/06 , C07C229/48 , C12P41/00
CPC分类号： C12P13/02 , A61K38/21 , A61K45/06 , C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C12P41/005 , A61K2300/00
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.
摘要翻译：式（I）化合物的外消旋体，非对映异构体和光学异构体：其中B是H，C 6或C 10芳基，C 7-16芳烷基; Het或（低级烷基）-Het，其全部任选被C 1-6烷基取代; C 1-6烷氧基; C 1-6烷酰基; 羟基; 羟; 光环; 卤代; 硝基; 氰基; 氰; 任选被C 1-6烷基取代的氨基; 酰胺基; 或（低级烷基）酰胺; 或B是式R 4 -C（O） - 的酰基衍生物; 式R 4 -O-C（O） - 的羧基; 式R 4 -N（R 5）-C（O） - 的酰胺; 式R 4 -N（R 5）-C（S） - 的硫代酰胺或式R 4 -SO 2的磺酰基; R 5为H或C 1-6烷基; Y为H或C 1-6烷基; R 3是C 1-8烷基，C 3-7环烷基或C 4-10烷基环烷基，全部任选被羟基，C 1-6烷氧基，C 1-6硫代烷基，酰氨基，（低级烷基）酰氨基，C 6 或C 10芳基或C 7-16芳烷基; R 2是CH 2 -R 20，NH-R 20，O-R 20或S-R 20，其中R 20是饱和或不饱和C 3-7环烷基或C 4-10（烷基环烷基），其全部是任选被R 21单取代，二取代或三取代，或R 20为C 6或C 10芳基或任选取代的C 7-14芳烷基，或R 20为Het或（低级烷基）-Het，均为任选取代的Het 或（低级烷基）-Het; 羧基; 羧基（低级烷基）; C 6或C 10芳基，C 7-14芳烷基或Het，所述芳基，芳烷基或Het任选被取代; 且R 1为H; C 1-6烷基，C 3-7环烷基，C 2-6烯基或C 2-6炔基，全部被卤素取代; 或其药学上可接受的盐或酯。

6. 发明公开

EP1891950A1 Viral polymerase inhibitors 审中-公开
标题翻译： Viren-Polymerasehemmer
公开(公告)号：EP1891950A1
公开(公告)日：2008-02-27
申请号：EP07117946.9
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： Beaulieu, Pierre, Louis , Fazal, Gulrez , Kukolj, George , Jolicoeur, Eric , Gillard, James , Poupart, Marc-André , Rancourt, Jean
IPC分类号： A61K31/404 , A61K31/381 , A61K31/4402 , A61K31/437 , C07D209/08 , C07D405/04 , C07D409/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D413/04 , C07D471/04
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
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 defined above;
M is N or C R 7 , wherein R 7 has the same definition as R 4 defined above;
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;
a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
摘要翻译：由式I表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中：A是O，S，N R 1或C R 1，其中R 1在本文中定义; -----表示单键或双键; R 2选自：H，卤素，R 21，OR 21，SR 21，COO R 21，SO 2 N（R 22）2，N（R 22）2，CON（R 22）2，NR 22 C （O）R 22或NR 22 C（O）NR 22，其中R 21和每个R 22在本文中定义; B是N R 3或C R 3，条件是A或B中的一个是C R 1或C R 3，其中R 3在本文中定义; K是N或C R 4，其中R 4在本文中定义; L是N或C R 5，其中R 5具有与上述R 4相同的定义; M是N或C R 7，其中R 7具有与上述R 4相同的定义; Y 1为O或S; Z是N（R 6a）R 6或O R 6，其中R 6a是H或烷基或N R 61 R 62，其中R 61和R 62在本文中定义; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

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