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    • 4. 发明授权
    • Hepatitis C inhibitor tri-peptides
    • 丙型肝炎抑制剂三肽
    • US06323180B1
    • 2001-11-27
    • US09368866
    • 1999-08-05
    • Montse Llinas-BrunetMurray D. BaileyDale CameronElise GhiroNathalie GoudreauMarc-André PoupartJean RancourtYoula S. TsantrizosAnne-Marie FaucherTeddy HalmosDominik M. WernicBruno Simoneau
    • Montse Llinas-BrunetMurray D. BaileyDale CameronElise GhiroNathalie GoudreauMarc-André PoupartJean RancourtYoula S. TsantrizosAnne-Marie FaucherTeddy HalmosDominik M. WernicBruno Simoneau
    • A61K3800
    • C12P13/02A61K38/21A61K45/06C07D207/16C07D401/12C07D403/12C07D403/14C07D405/14C07D409/14C07D417/14C07K5/0806C07K5/0808C07K5/081C07K5/0812C12P41/005A61K2300/00
    • 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.
    • 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。