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    Hepatitis C inhibitor peptides
    11.
    发明授权
    Hepatitis C inhibitor peptides 有权
    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。

    Hepatitis C inhibitor peptide analogues
    15.
    发明授权
    Hepatitis C inhibitor peptide analogues 有权
    丙型肝炎抑制肽类似物

    公开(公告)号：US6143715A

    公开(公告)日：2000-11-07

    申请号：US131433

    申请日：1998-08-10

    申请人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Teddy Halmos ,  Marc-Andre Poupart ,  Youla Tsantrizos

    发明人： Montse Llinas-Brunet ,  Murray D. Bailey ,  Teddy Halmos ,  Marc-Andre Poupart ,  Youla Tsantrizos

    IPC分类号： A61K45/00 ,  A61K31/13 ,  A61K31/7056 ,  A61K38/00 ,  A61K38/21 ,  A61P31/14 ,  C07K7/06 ,  C07K14/18 ,  A61K38/04 ,  C07K5/00

    CPC分类号： C07K7/06 ,  C07K14/005 ,  A61K38/00 ,  C12N2770/24222

    摘要： Compound of formula (I) active against the Hepatitis C virus: ##STR1## wherein B is an acyl derivative; a is 0 or 1; R.sub.6, when present, is carboxy(lower)alkyl; b is 0 or 1; R.sub.5, when present, is C.sub.1-6 alkyl, or carboxy (lower)alkyl; Y is H or C.sub.1-6 alkyl; R.sub.4 is C.sub.1-10 alkyl; R.sub.3 is C.sub.1-10 alkyl; W is --NH--CH(R.sub.2)--C(O)--, wherein R.sub.2 is C.sub.1-6 alkyl; C.sub.6 or C.sub.10 aryl; C.sub.7-16 aralkyl; or carboxy (lower)alkyl; or W is a proline derivative; Q is a group of the formula --Z(R.sub.1)--C(O)--R.sub.13, wherein Z is CH or N; R.sub.1 is C.sub.1-6 alkyl or C.sub.1-6 alkenyl both optionally substituted with thio or halo,; and R.sub.13 is an activated carbonyl substituent, or Q is a phosphonate group of the formula --CH(R.sub.1)--P(O)R.sub.15 R.sub.16 wherein R.sub.15 and R.sub.16 are independently C.sub.6-20 aryloxy; and R.sub.1 is as defined above.

    摘要翻译： 对丙型肝炎病毒有活性的式（I）化合物：其中B为酰基衍生物; a是0或1; 当存在时，R 6为羧基（低级）烷基; b为0或1; 当存在时，R 5为C 1-6烷基或羧基（低级）烷基; Y是H或C 1-6烷基; R4是C1-10烷基; R3是C1-10烷基; W是-NH-CH（R 2）-C（O） - ，其中R 2是C 1-6烷基; C6或C10芳基; C7-16芳烷基; 或羧基（低级）烷基; 或W是脯氨酸衍生物; Q是式-Z（R1）-C（O）-R13的基团，其中Z是CH或N; R1是任选被硫或卤代取代的C 1-6烷基或C 1-6烯基; 并且R 13是活化的羰基取代基，或Q是式-CH（R 1）-P（O）R 15 R 16的膦酸酯基团，其中R 15和R 16独立地是C 6-20芳氧基; 并且R 1如上所定义。