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cytalogy auto smear method

机译:细胞学自动涂片法

摘要

Compounds of formula (I), wherein A' and A'' are independently the same or different group of formula (II) wherein: R' is H, CH 3, C(CH3) 2, -OR a, -N(R a) 2, -N(R a)OR a or -DP; R''' is H or CH 3 ; R a is H, C 1 -C 3 alkyl; D is a bond, alkylene, -C(=O)-, -S(O)- or -S(O) 2 -; P is an optionally substituted, mono or bicyclic carbo- or heterocycle; R'' is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH 2) n DP; M is a bond or -C(=O)N(R''')-; Q is absent, a bond, -CH(OH)- or -CH 2 -; or R'' together with Q, M and R' define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R' is -OR a, -N(R a) 2, -N(R a)OR a or -DP, if M is a bond and Q is absent; X is H, OH, OCH 3 ; Y is H, OH, OCH 3, but X and Y are not both H; Z' and Z'' are independently -(CH 2) m P where P is as defined above; n and m are independently 0, 1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.
机译:式(I)的化合物,其中A'和A''独立地是式(II)的相同或不同基团,其中:R'是H,CH 3,C(CH3)2 --OR a,-N(R a)2,-N(R a)OR a或-DP; R”'为H或CH 3; R a为H,C 1 -C 3烷基; D为键,亚烷基,-C(= O)-,-S(O)-或-S(O)2-; P是任选取代的单或双环碳环或杂环; R”为H,是天然氨基酸,羧乙酰胺或(CH 2)n DP基团中的任何侧链; M为键或-C(= O)N(R''')-; Q不存在,键为-CH(OH)-或-CH 2-;或R”与Q,M和R'一起定义任选取代的5或6元碳环或杂环,其任选地与另外的5或6元碳环或杂环稠合;前提是R'为-OR a,-N(R a)2,-N(R a)OR a或-DP,如果M为键且Q不存在; X为H,OH,OCH 3; Y是H,OH,OCH 3,但是X和Y都不都是H; Z′和Z″独立地为-(CH 2)m P,其中P如上所定义; n和m独立为0、1或2;及其药学上可接受的盐和前药可用作HIV的天冬氨酰蛋白酶抑制剂。它们可以由新型的2,5-二-O-苄基-L-甘露聚糖-1,4:6,3-二内酯中间体以便捷的两步合成法制备。

著录项

  • 公开/公告号KR20010105975A

    专利类型

  • 公开/公告日2001-11-29

    原文格式PDF

  • 申请/专利权人 KIM HAE WON;LEE WON BAE;

    申请/专利号KR20000027131

  • 发明设计人 KIM HAE WON;LEE WON BAE;

    申请日2000-05-19

  • 分类号C12Q1/00;

  • 国家 KR

  • 入库时间 2022-08-22 00:32:07

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