会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明申请
    • MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND USE THEREOF
    • 多种抗药性复性蛋白酶抑制剂及其用途
    • WO9967254A3
    • 2000-02-10
    • PCT/US9914120
    • 1999-06-23
    • US HEALTHUNIV ILLINOISERICKSON JOHN WGULNIK SERGEI VGHOSH ARUN KHUSSAIN KHAJA A
    • ERICKSON JOHN WGULNIK SERGEI VGHOSH ARUN KHUSSAIN KHAJA A
    • G01N33/15A61K31/34A61K31/4525A61P31/18A61P37/04A61P43/00C07D493/04C12Q1/02C12Q1/37C07D491/04C07D495/04
    • A61K31/4525A61K31/34C07D493/04C12Q1/025C12Q1/37G01N2333/16G01N2333/8142
    • The present invention generally provides a retroviral protease-inhibiting compound represented by formula (I), or a pharmaceutically acceptable salt, a prodrug, or an ester thereof, wherein A is a group of formula (II), (III), (IV), or (V); R , R , R , R , or R is H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH2, O, S, SO, SO2, amino, amides, carbamates, ureas or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO2; m is from 0 to 6; R is OH, =O (keto), NH2, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO2; wherein the compound inhibits a multidrug-resistant retroviral protease. Optionally, R and R , together the N-W bond of formula (I), comprise a 12- to 18-membered ring. Also provided are pharmaceutical compositions for, and therapeutic methods of, treating a multidrug-resistant retroviral infection in a mammal.
    • 本发明通常提供由式(I)表示的逆转录病毒蛋白酶抑制化合物或其药学上可接受的盐,前药或酯,其中A为式(II),(III),(IV), ,或(V); R 1,R 2,R 3,R 5或R 6是H,或任选取代的和/或含杂原子的烷基,烯基,炔基或环状基团; Y和/或Z是任选被烷基,烯基或炔基取代的CH 2,O,S,SO,SO 2,氨基,酰胺,氨基甲酸酯,脲或硫代羰基衍生物; n为1〜5; X是一个键,任选取代的亚甲基或亚乙基,氨基,O或S; Q是C(O),C(S)或SO 2; m为0〜6; R 4是OH,= O(酮),NH 2或烷基氨基,包括酯,酰胺和其盐; W为C(O),C(S),S(O)或SO 2; 其中所述化合物抑制多药耐药逆转录病毒蛋白酶。 任选地,R 5和R 6一起形成式(I)的N-W键,包含12至18元环。 还提供了用于治疗哺乳动物多药耐药逆转录病毒感染的药物组合物和治疗方法。