专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明公开

EP1437362A1 Macrocyclic peptides inhibiting the hepatitis C virus ns3 protease 审中-公开
标题翻译： Makrozyklische Peptide als丙型肝炎病毒ns3蛋白酶抑制剂
公开(公告)号：EP1437362A1
公开(公告)日：2004-07-14
申请号：EP04009264.5
申请日：2000-04-03
申请人： BOEHRINGER INGELHEIM (CANADA) 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： C07K5/08 , C07K5/078 , A61K38/05 , A61K38/06 , A61P31/14
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0802 , C07K5/0821 , Y02A50/463
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; R 21 is H, halo, C 1-6 alkyl, cycloalkyl, haloalkyl, C 1-6 alkoxy, cycloalkoxy, hydroxy, or N( R 23 ) 2 , wherein each R 23 is independently H, C 1-6 alkyl or cycloalkoxy; and R 22 is H, halo, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 haloalkyl, C 1-6 thioalkyl, C 1-6 alkoxy, C 3-6 cycloalkoxy, C 2-7 alkoxyalkyl, C 3-6 cycloalkyl, C 6 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 R 24 , wherein R 24 is H, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 3-6 cycloalkoxy, NO 2 , N( R 25 ) 2 , NH-C(O)- R 25 ; or NH-C(O)-NH- R 25 , wherein each R 25 is independently: H, C 1-6 alkyl or C 3-6 cycloalkyl; or R 24 is NH-C(O)-O R 26 wherein R 26 is C 1-6 alkyl or C 3-6 cycloalkyl; R 3 is hydroxy, NH 2 , or a group of formula - NH- R 31 , wherein R 31 is C 6 or 10 aryl, heteroaryl, -C(O)- R 32 , -C(O)-O R 32 or -C(O)-NH R 32 , wherein R 32 is: C 1-6 alkyl or C 3-6 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- R 41 , wherein R 41 is H, C 1-6 alkyl, cycloalkyl or -C(O)- R 42 , wherein R 42 is C 1-6 alkyl, cycloalkyl or C 6 or 10 aryl; R 4 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: C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, hydroxy, halo, amino, oxo, thio or C 1-6 thioalkyl, and A is an amide of formula -C(O)-NH- R 5 , wherein R 5 is selected from the group consisting of: C 1-8 alkyl, C 3-6 cycloalkyl, C 6 or 10 aryl or C 7-16 aralkyl; or A is a carboxylic acid or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：大环肽（I）及其盐和酯是新的。式（I）的大环肽及其盐和酯是新的。 [图像] W = CH或N; R 21 = H，卤素，1-6C烷基，3-6C环烷基，1-6C卤代烷基，1-6C烷氧基，3-6C环烷氧基，羟基或N（R 23）2; R 23 = H，1-6C烷基或3-6C环烷基; R 2 2 = H，卤素，1-6C烷基，3-6C环烷基，1-6C卤代烷基，1-6C硫代烷基，1-6C烷氧基，3-6C环烷氧基，2-7C烷氧基烷基，3-6C环烷基，6C或 10C芳基或Het; Het = 5-7元任选饱和的含有1-4个N，O或S的杂环; 环烷基，芳基或Het被R 24取代; R 24 = H，卤素，1-6C烷基，3-6C环烷基，1-6C烷氧基，3-6C环烷氧基，NO 2，N（R 25），NHC（O）R 25，NHC（O）NHR 25或 NH-C（O）-OR 26; R 2 5 = H，1-6C烷基或3-6C环烷基; R 26 = 1-6C烷基或3-6C环烷基; R 3 = OH，NH 2或NHR 31; R 31 = 6或10芳基，杂芳基，C（O）R 32，C（O）NHR或C（O）OR 32; R 32 = 1-6C烷基或3-6C环烷基; 任选含有1-3个O，S或NR 41的5-10元任选的饱和亚烷基链; R 41 = H，1-6C烷基，3-6C环烷基或C（O）R 42; R 42 = 1-6C烷基，3-6C环烷基或6或10芳基; R 4 = 1-6C烷基，1-6C卤代烷基，1-6C烷氧基，羟基，卤素，氨基，氧代，硫代或1-6C硫代烷基的H或1-3; A = C（O）NNHR 5或羧酸; R 5 = 1-8C烷基，3-6C环烷基，6或10芳基或7-16C芳烷基。还包括使用包含（I）与载体介质或辅助剂混合的组合物的独立权利要求，用于制备用于治疗哺乳动物中的丙型肝炎病毒感染的药物。活动：抗病毒。作用机制：HCV NS3蛋白酶的选择性抑制剂。在使用Huh-7细胞的NS3基于蛋白酶细胞的测定中，衍生自与2个DNA构建体共转染的肝癌的人细胞系，式（Ia）的化合物显示小于1MicroM的EC 50值。 [图片]。

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

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.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式