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    • 1. 发明公开
    • SUSTAINED HIV PROTEASE INHIBITOR
    • 持久的HIV蛋白酶抑制剂
    • EP3192794A1
    • 2017-07-19
    • EP15839901.4
    • 2015-09-10
    • Shionogi & Co., Ltd.
    • KAWASUJI, TakashiMIKAMIYAMA, HidenoriSUZUKI, NaoyukiMASUDA, KojiSUGIMOTO, HidekiOKANO, AzusaYOSHIDA, MihoSUGIYAMA, ShuichiASAHI, KentarouKOZONO, IoriMIYAZAKI, KeisukeOZASA, HirokiMIYAGAWA, Masayoshi
    • C07D409/12A61K31/381A61K31/397A61K31/40A61K31/416A61K31/427A61K31/428A61K31/4436A61K31/4525A61P31/18A61P43/00C07D493/04C12N9/99
    • C07D493/04A61K31/381A61K31/397A61K31/40A61K31/416A61K31/427A61K31/428A61K31/4436A61K31/4525A61P31/18C07D231/56C07D333/72C07D409/12C07D519/00C12N9/99
    • The present invention provides useful compounds for HIV protease inhibitor. A compound represented by formula or its pharmaceutically acceptable salt Formula:

      wherein ring A is

      R 4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like,
      R 5 is hydrogen atom, halogen, hydroxy and the like,
      R 6 is each independently halogen, hydroxy, carboxy and the like,
      ring A may be substituted with said R 6 at any substitutable position(s),
      a is an integer of 0 to 7,
      ring B is substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl,
      ring C is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl,
      R 1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like,
      R 2 and R 3 are each independently -Y-Z or hydrogen atom,
      provided that at least one of R 1 , R 2 , R 3 and R 4 is a group represented by formula: -Y-Z,
      Y is a bond, or a spacer of any combination selected from the group consisting of -O-, -S-, -NR 7 -, -C(=O)-, -SO-, -SO 2 -, -NR 7 -C(=O)-, -C(=O)-NR 7 -, -NR 7 -C(=O)-NR 7 -, -NR 7 -C(=O)-O-, -SO 2 -NR 7 -, -NR 7 -SO 2 -, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted aromatic carbocyclediyl, substituted or unsubstituted non-aromatic carbocyclediyl, substituted or unsubstituted aromatic heterocyclediyl and substituted or unsubstituted non-aromatic heterocyclediyl,
      R 7 are each independently hydrogen atom, hydroxy, carboxy and the like, and
      Z is substituted aromatic carbocyclyl, substituted non-aromatic carbocyclyl, substituted aromatic heterocyclyl or substituted non-aromatic heterocyclyl.
    • 本发明提供了用于HIV蛋白酶抑制剂的有用化合物。 由式或其药学上可接受的盐表示的化合物或其药学上可接受的盐式:其中环A为R 4为-YZ,氢原子,卤素,羟基等,R 5为氢原子,卤素,羟基等,R 6各自独立地为卤素,羟基 ,羧基等,环A可以在任何可取代的位置被所述R6取代,a是0-7的整数,环B是取代或未取代的芳族碳环基或取代或未取代的芳族杂环基,环C是 取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环基或取代或未取代的非芳族杂环基,R1是-YZ,取代或未取代的烷基,取代或未取代的烯基, 例如,R2和R3各自独立地是-YZ或氢原子,条件是R1,R2,R3和R4中的至少一个是由式-YZ表示的基团, Y是键,或选自-O - , - S - , - NR 7 - , - C(= O) - , - SO - , - SO 2 - , - NR 7 -C (= O)-NR 7 - , - NR 7 -C(= O)-NR 7 - , - NR 7 -C(= O)-O - , - SO 2 -NR 7 - ,取代或未取代的亚烷基,取代或未取代的亚烯基,取代或未取代的亚炔基,取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环二基和取代或未取代的非芳族杂环二基, ,羟基,羧基等,Z是取代的芳族碳环基,取代的非芳族碳环基,取代的芳族杂环基或取代的非芳族杂环基。