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    SUSTAINED HIV PROTEASE INHIBITOR
    9.
    发明公开
    SUSTAINED HIV PROTEASE INHIBITOR 审中-公开
    持久的HIV蛋白酶抑制剂

    公开(公告)号：EP3192794A1

    公开(公告)日：2017-07-19

    申请号：EP15839901.4

    申请日：2015-09-10

    申请人： Shionogi & Co., Ltd.

    发明人： KAWASUJI, Takashi ,  MIKAMIYAMA, Hidenori ,  SUZUKI, Naoyuki ,  MASUDA, Koji ,  SUGIMOTO, Hideki ,  OKANO, Azusa ,  YOSHIDA, Miho ,  SUGIYAMA, Shuichi ,  ASAHI, Kentarou ,  KOZONO, Iori ,  MIYAZAKI, Keisuke ,  OZASA, Hiroki ,  MIYAGAWA, Masayoshi

    IPC分类号： C07D409/12 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/416 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4525 ,  A61P31/18 ,  A61P43/00 ,  C07D493/04 ,  C12N9/99

    CPC分类号： C07D493/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/416 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4525 ,  A61P31/18 ,  C07D231/56 ,  C07D333/72 ,  C07D409/12 ,  C07D519/00 ,  C12N9/99

    摘要： 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.

    摘要翻译： 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。