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1. 发明授权

US07696242B2 Hepatitis C inhibitor peptide analogs 有权
标题翻译：丙型肝炎抑制肽类似物
公开(公告)号：US07696242B2
公开(公告)日：2010-04-13
申请号：US11185616
申请日：2005-07-19
申请人： Murray D. Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-André Poupart , Jean Rancourt
发明人： Murray D. Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-André Poupart , Jean Rancourt
IPC分类号： A61K31/40 , C07D207/00 , C07D453/02 , C07D217/02 , C07D217/22 , A61K31/74
CPC分类号： C07D401/04 , A61K38/00 , C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07K5/0205
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
摘要翻译：式（I）化合物：其中R 1，R 2，R 3，R 4，R 5，Y，n和m如本文所定义。该化合物可用作HCV NS3蛋白酶的抑制剂。

2. 发明授权

US07511157B2 Hepatitis C inhibitor dipeptide analogs 有权
标题翻译：丙型肝炎抑制剂二肽类似物
公开(公告)号：US07511157B2
公开(公告)日：2009-03-31
申请号：US11185671
申请日：2005-07-19
申请人： Murray D. Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-André Poupart , Jean Rancourt
发明人： Murray D. Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-André Poupart , Jean Rancourt
IPC分类号： C07D207/48 , C07D207/08 , C07D215/12 , C07D215/16 , C07D215/06
CPC分类号： C07D413/04 , A61K38/00 , C07K5/06139 , C07K5/06191
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
摘要翻译：式（I）化合物：其中R 1，R 2，R 3，R 4，n和m如本文所定义。该化合物可用作HCV NS3蛋白酶的抑制剂。

3. 再颁专利

USRE40525E1 Hepatitis C inhibitor tri-peptides 有权
公开(公告)号：USRE40525E1
公开(公告)日：2008-09-30
申请号：US11241899
申请日：2005-09-30
申请人： Montse Llinas-Brunet , Murray D. Bailey , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Dominik M. Wernic
发明人： Montse Llinas-Brunet , Murray D. Bailey , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Dominik M. Wernic
IPC分类号： A61K38/00 , A61K31/47 , A61K31/40 , C07D215/16 , C07D405/00
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： A racemate diastereoisomer and optical isomer 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 may be 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 derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative 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 C2—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 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.

4. 发明授权

US06323180B1 Hepatitis C inhibitor tri-peptides 有权
标题翻译：丙型肝炎抑制剂三肽
公开(公告)号：US06323180B1
公开(公告)日：2001-11-27
申请号：US09368866
申请日：1999-08-05
申请人： Montse Llinas-Brunet , Murray D. Bailey , Dale Cameron , Elise Ghiro , Nathalie Goudreau , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Anne-Marie Faucher , Teddy Halmos , Dominik M. Wernic , Bruno Simoneau
发明人： Montse Llinas-Brunet , Murray D. Bailey , Dale Cameron , Elise Ghiro , Nathalie Goudreau , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Anne-Marie Faucher , Teddy Halmos , Dominik M. Wernic , Bruno Simoneau
IPC分类号： A61K3800
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： A racemate, diastereoisomer and optical isomer 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 may be 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 derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative 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 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.
摘要翻译：式（I）化合物的外消旋物，非对映异构体和旋光异构体：其中B为H，C6或C10芳基，C7-16芳烷基; Het或（低级烷基）-Het，其全部可以任选被C 1-6烷基取代; C 1-6烷氧基 C 1-6烷酰基; 羟基; 羟烷基光环; 卤代烷基硝基氰基; 氰基烷基任选被C 1-6烷基取代的氨基; 氨基酸或（低级烷基）酰胺; 或B是式R4-C（O） - 的酰基衍生物; 式R4-O-C（O） - 的羧基衍生物; 式R 4 -N（R 5）-C（O） - 的酰胺衍生物; 式R 4 -N（R 5）-C（S） - 的硫代酰胺衍生物; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; 并且Y是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，全部被羟基，C 1-6烷氧基，C 1-6硫烷基，酰氨基，（低级烷基），C6或C10芳基或C7-16芳烷基; R2是CH2-R20，NH-R20，O-R20或S-R20，其中R20是饱和或不饱和的C3-7环烷基或C4-10（烷基环烷基），全部其任选被R 21单取代，二取代或三取代，或R 20为任选取代的C 6或C 10芳基或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）; C6或C10芳基，C7-14芳烷基或Het，所述芳基，芳烷基或Het任选被取代; 且R1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。

5. 发明授权

US07705146B2 Hepatitis C inhibitor peptide analogs 有权
标题翻译：丙型肝炎抑制肽类似物
公开(公告)号：US07705146B2
公开(公告)日：2010-04-27
申请号：US10595108
申请日：2005-06-22
申请人： Murray D. Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
发明人： Murray D. Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
IPC分类号： A61K31/535 , C07D413/00 , C07D401/00
CPC分类号： C07D413/04 , C07D207/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D495/04 , C07D498/04 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0819 , C07K5/0827
摘要： The invention relates to compounds of formula (I) wherein R′, R2, R3, R4, R5, R6, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，Y，n和m如本文所定义。该化合物可用于通过抑制HCV NS3蛋白酶治疗和预防哺乳动物中丙型肝炎病毒感染。本发明还涉及可与酰胺阴离子反应以制备式（I）化合物的式（III）的吖内酯化合物。

6. 发明申请

US20050192212A1 Macrocyclic peptides active against the hepatitis C virus 有权
标题翻译：对丙型肝炎病毒有活性的大环肽
公开(公告)号：US20050192212A1
公开(公告)日：2005-09-01
申请号：US11039698
申请日：2005-01-19
申请人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
发明人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
IPC分类号： A61K38/00 , C07K5/08 , C07K5/083 , C07K5/087 , A61K38/12 , A61K31/4709 , C07K5/12
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
摘要： Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.
摘要翻译：式（I）化合物：其中R 1，R 2，X，R 3，D和虚线b如上所定义在这里或其药学上可接受的盐或酯可用作HCV NS3蛋白酶的抑制剂。

7. 发明授权

US06767991B1 Hepatitis C inhibitor peptides 有权
标题翻译：丙型肝炎抑制肽
公开(公告)号：US06767991B1
公开(公告)日：2004-07-27
申请号：US09368670
申请日：1999-08-05
申请人： Montse Llinas-Brunet , Murray D. Bailey , Dale Cameron , Elise Ghiro , Nathalie Goudreau , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Bruno Simoneau , Dominik M. Wernic
发明人： Montse Llinas-Brunet , Murray D. Bailey , Dale Cameron , Elise Ghiro , Nathalie Goudreau , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Bruno Simoneau , Dominik M. Wernic
IPC分类号： C07K700
CPC分类号： C07K7/06 , A61K38/00 , C07K5/06139 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/08 , C07K14/005 , C12N2770/24222
摘要： Disclosed herein are hepatitis C viral protease inhibitors of 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; R6, when present, is C1-6 alkyl substituted with carboxyl; R5, when present, is C1-6 alkyl optionally substituted with carboxyl; R4 is C1-10 alkyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R3 is C1-10 alkyl optionally substituted with carboxyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R2 is CH2—R20, NH—R20, O—R20 or S—R20; wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkyl cycloalkyl) being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10aryl, C7-16 aralkyl, Het or (lower alkyl)-Het, all optionally mono-, di- or tri-substituted with R21, wherein R21 is as defined herein; R1 is C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, all optionally substituted with halogen; and W is hydroxy or a N-substituted amino: or W taken together with the carbonyl group to which it is bonded represents an ester group, or a pharmaceutically acceptable salt thereof.
摘要翻译：本文公开了式（I）的丙型肝炎病毒蛋白酶抑制剂：其中a为0或1; b为0或1; Y是H或C 1-6烷基; B是H，酰基衍生物或磺酰基衍生物;当存在时，R 6是被羧基取代的C 1-6烷基;当存在时，R 5是任选被羧基取代的C 1-6烷基; R4是C1-10烷基，C3-7环烷基或C4-10（烷基环烷基）; R3是任选被羧基取代的C1-10烷基，C3-7环烷基或C4-10（烷基环烷基）; R2是CH2-R20，NH- R20，O-R20或S-R20; 其中R 20是饱和或不饱和的C 3-7环烷基或任选被R 21单取代，二或三取代的C 4-10（烷基环烷基），或R 20是C 6或C 10芳基，C 7-16芳烷基，Het或（低级烷基）-Het，全部任选被R 21单取代，二取代或三取代，其中R 21如本文所定义; R 1是C 1-6烷基，C 2-6烯基或C 2-6炔基，全部被卤素取代; 和W是羟基或N-取代的氨基：或W与其键合的羰基一起代表酯基或其药学上可接受的盐。

8. 发明授权

US07939667B2 Hepatitis C inhibitor compounds 有权
标题翻译：丙型肝炎抑制剂化合物
公开(公告)号：US07939667B2
公开(公告)日：2011-05-10
申请号：US11766171
申请日：2007-06-21
申请人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
发明人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
IPC分类号： C07D215/38 , A61K31/02
CPC分类号： A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
摘要： Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
摘要翻译：式（I）化合物：其中B，X，R3，L0，L1，L2，R2，R1和RC如本文所定义。该化合物可用作用于治疗丙型肝炎病毒感染的HCV NS3蛋白酶的抑制剂。

9. 发明申请

US20060258868A1 Hepatitis c inhibitor peptide analogs 有权
标题翻译：丙型肝炎抑制肽类似物
公开(公告)号：US20060258868A1
公开(公告)日：2006-11-16
申请号：US10595108
申请日：2005-06-22
申请人： Murray Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
发明人： Murray Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
IPC分类号： C07D215/00
CPC分类号： C07D413/04 , C07D207/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D495/04 , C07D498/04 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0819 , C07K5/0827
摘要： The invention relates to compounds of formula (I) wherein R′, R2, R3, R4, R5, R6, Y, n and m are as defined (herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 5， R 6，Y，n和m如本文所定义（本文中，该化合物可用于通过抑制HCV NS3蛋白酶治疗和预防哺乳动物中丙型肝炎病毒感染。本发明进一步涉及可与酰胺阴离子反应以制备式（I）化合物的式（III）的吖内酯化合物。

10. 发明申请

US20050020503A1 Hepatitis C inhibitor compounds 有权
标题翻译：丙型肝炎抑制剂化合物
公开(公告)号：US20050020503A1
公开(公告)日：2005-01-27
申请号：US10850101
申请日：2004-05-20
申请人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
发明人： Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
IPC分类号： A61K31/4709 , A61K38/00 , A61K38/21 , A61P31/00 , C07K5/08 , C07K5/083 , A61K38/05 , C07K5/06
CPC分类号： A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
摘要： Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
摘要翻译：式（I）化合物：其中B，X，R 3，L 0，L 1，L 2，R 2，R 1和R C如本文所定义。该化合物可用作用于治疗丙型肝炎病毒感染的HCV NS3蛋白酶的抑制剂。

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