Hepatitis C inhibitor tri-peptides
    1.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE41894E1

    公开(公告)日:2010-10-26

    申请号:US12042627

    申请日:2008-03-05

    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。

    Hepatitis C inhibitor tri-peptides
    2.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE41356E1

    公开(公告)日:2010-05-25

    申请号:US12118926

    申请日:2008-05-12

    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。

    Hepatitis C inhibitor tri-peptides
    3.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06534523B1

    公开(公告)日:2003-03-18

    申请号:US10091293

    申请日:2002-03-05

    IPC分类号: A61K3147

    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。

    Hepatitis C inhibitor tri-peptides
    4.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE42164E1

    公开(公告)日:2011-02-22

    申请号:US12119609

    申请日:2008-05-13

    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。

    Hepatitis C inhibitor tri-peptides
    5.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06410531B1

    公开(公告)日:2002-06-25

    申请号:US09849057

    申请日:2001-05-04

    IPC分类号: A61K3535

    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。

    Hepatitis C inhibitor tri-pepitides
    6.
    发明授权
    Hepatitis C inhibitor tri-pepitides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06329417B1

    公开(公告)日:2001-12-11

    申请号:US09703751

    申请日:2000-11-01

    IPC分类号: A61K3140

    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。

    Hepatitis C inhibitor tri-peptides
    7.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06329379B1

    公开(公告)日:2001-12-11

    申请号:US09675398

    申请日:2000-09-29

    IPC分类号: A61K31505

    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。

    Hepatitis C inhibitor tri-peptides
    9.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06420380B2

    公开(公告)日:2002-07-16

    申请号:US09827976

    申请日:2001-04-06

    IPC分类号: A61K3144

    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。

    Hepatitis C inhibitor tri-peptides
    10.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    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

    IPC分类号: A61K3800

    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。