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    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：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。

    Hepatitis C inhibitor tri-peptides
    7.
    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

    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。

    Hepatitis C inhibitor tri-peptides
    8.
    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

    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。

    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：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。

    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：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。