公开(公告)号：USRE41894E1

公开(公告)日：2010-10-26

申请号：US12042627

申请日：2008-03-05

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K31/505 ,  A61K31/52 ,  C07D239/00 ,  C07D239/02 ,  C07D239/72

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 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; hydroxy-alkyl; 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 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）化合物的外消旋体，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 羟基 - 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; 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R4-SO2的磺酰基; R5是H或C1-6烷基; Y为H或C 1-6烷基; R 3为C 3-7环烷基或C 4-10烷基环烷基，全部任选被羟基取代，C 1-6烷氧基，C 1-6硫烷基，酰氨基，（低级烷基）酰氨基，C 6或C 10芳基或C 7-16芳烷基; 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），它们都是任选的单 - ，二 - 或三 - 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。

公开(公告)号：USRE41356E1

公开(公告)日：2010-05-25

申请号：US12118926

申请日：2008-05-12

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K31/40 ,  C07D207/00 ,  C07D295/00

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, diastereolsomers 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—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; carboyl; 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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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R4-SO2的磺酰基; R5是H或C1-6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; 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），它们都是任选的单 - ，二 - 或三 - 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; 羰基 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。

公开(公告)号：US06534523B1

公开(公告)日：2003-03-18

申请号：US10091293

申请日：2002-03-05

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K3147

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 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—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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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。

公开(公告)号：USRE42164E1

公开(公告)日：2011-02-22

申请号：US12119609

申请日：2008-05-13

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K31/40 ,  A61K31/47 ,  C07D215/16 ,  C07D207/12

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 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—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）化合物的外消旋体，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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R4-SO2的磺酰基; R5是H或C1-6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; 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），它们都是任选的单 - ，二 - 或三 - 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。

公开(公告)号：US06410531B1

公开(公告)日：2002-06-25

申请号：US09849057

申请日：2001-05-04

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K3535

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 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—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 C26 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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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 26炔基，全部被卤素取代; 或其药学上可接受的盐或酯。

公开(公告)号：US06329417B1

公开(公告)日：2001-12-11

申请号：US09703751

申请日：2000-11-01

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K3140

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, diastereolsomers 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—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; carboyl; 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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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; 羰基 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。

公开(公告)号：US06329379B1

公开(公告)日：2001-12-11

申请号：US09675398

申请日：2000-09-29

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Elise Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K31505

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 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—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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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。

公开(公告)号：US06420380B2

公开(公告)日：2002-07-16

申请号：US09827976

申请日：2001-04-06

申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Ellse Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Dale R. Cameron ,  Ellse Ghiro ,  Nathalie Goudreau ,  Marc-Andre Poupart ,  Jean Rancourt ,  Youla S. Tsantrizos ,  Anne-Marie Faucher ,  Teddy Halmos ,  Dominik M. Wernic

IPC分类号： A61K3144

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 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—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，非对映异构体和光学异构体：其中B是H，C6或C10芳基，C7-16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; 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。

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。

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。