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COMPOUNDS FOR INHIBITION OF CHYMOTRYPSIN-LIKE ACTIVITY OF THE 20S PROTEASOME

机译:抑制20S蛋白质类胰蛋白酶样活性的化合物

摘要

A compound having a structure of formula I or a pharmaceutically acceptablesalt thereof,(see formula I)wherein X is O; Y is NH, N-alkyl, or O; Z is O or C(R9)2; R1, R2, R3, and R4are all hydrogen;each R5, R6, R7, R8, and R9 is independently selected from hydrogen, C1-6alkyl,C1-6hydroxyalkyl, C1-6alkoxyalkyl, aryl, and C1-6aralkyl, each of which isoptionallysubstituted with a group selected from alkyl, amide, amine, carboxylic acid orapharmaceutically acceptable salt thereof, carboxyl ester, thiol, andthioether; m is an integerfrom 0 to 2; and n is an integer from 0 to 2. The invention also relates touses of suchcompounds for the inhibition of chymotrypsin-like activity of a 20S-proteasome.
机译:具有式I结构或可药用的化合物盐(参见公式I)其中X是O; Y是NH,N-烷基或O; Z为O或C(R9)2; R1,R2,R3和R4都是氢每个R5,R6,R7,R8和R9独立地选自氢,C1-6烷基C 1-6羟烷基,C 1-6烷氧基烷基,芳基和C 1-6芳烷基,各自为可选地被选自烷基,酰胺,胺,羧酸或一种其药学上可接受的盐,羧基酯,硫醇和硫醚m是整数从0到2; n是0至2的整数。本发明还涉及这样的用途抑制20S-的胰凝乳蛋白酶样活性的化合物蛋白酶体。

著录项

  • 公开/公告号CA2589765C

    专利类型

  • 公开/公告日2015-06-30

    原文格式PDF

  • 申请/专利权人 PROTEOLIX INC.;

    申请/专利号CA20052589765

  • 发明设计人 SMYTH MARK S.;LAIDIG GUY J.;

    申请日2005-08-08

  • 分类号C07K5/087;A61K38/06;A61K38/07;C07K5/02;C07K5/103;

  • 国家 CA

  • 入库时间 2022-08-21 15:11:46

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