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1. 发明公开

EP3192794A1 SUSTAINED HIV PROTEASE INHIBITOR 审中-公开
标题翻译：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。

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