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1. 发明申请

US20190060293A1 5-PHENYLAZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 审中-公开
公开(公告)号：US20190060293A1
公开(公告)日：2019-02-28
申请号：US16078875
申请日：2017-02-24
申请人： SHIONOGI & CO., LTD.
发明人： Yuusuke TAMURA , Hiroki OZASA
IPC分类号： A61K31/4355 , A61P3/10 , A61K31/5377
CPC分类号： A61K31/4355 , A61K31/444 , A61K31/496 , A61K31/5377 , A61P3/10 , C07D471/04 , C07D519/00 , C07F9/6561 , Y02P20/55
摘要： Provided is a compound which is useful as an AMPK activator. The compound is represented by formula: wherein the symbols are defined in the specification.

2. 发明申请

US20170273955A1 AZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 有权
公开(公告)号：US20170273955A1
公开(公告)日：2017-09-28
申请号：US15505772
申请日：2015-08-26
申请人： Shionogi & Co., Ltd.
发明人： Yuusuke TAMURA , Yu HINATA , Eiichi KOJIMA , Hiroki OZASA
IPC分类号： A61K31/437 , A61K31/10 , A61K31/5377 , A61K31/03 , C07D471/04 , A61K31/343
CPC分类号： A61K31/437 , A61K31/03 , A61K31/10 , A61K31/343 , A61K31/444 , A61K31/5377 , C07D471/04 , C07D519/00
摘要： Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or its pharmaceutically acceptable salt, wherein X is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or substituted or unsubstituted heterocyclyl; R1 is hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted acyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkylsulfonyl, or substituted or unsubstituted alkyloxycarbonyl; R2 is halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; R3 is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; and R4 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

3. 发明申请

US20170253607A1 LONG-ACTING HIV PROTEASE INHIBITOR 审中-公开
公开(公告)号：US20170253607A1
公开(公告)日：2017-09-07
申请号：US15509049
申请日：2015-09-10
申请人： Shionogi & Co., Ltd.
发明人： Takashi KAWASUJI , Hidenori MIKAMIYAMA , Naoyuki SUZUKI , Koji MASUDA , Hideki SUGIMOTO , Azusa OKANO , Miho YOSHIDA , Shuichi SUGIYAMA , Kentarou ASAHI , Iori KOZONO , Keisuke MIYAZAKI , Hiroki OZASA , Masayoshi MIYAGAWA
IPC分类号： C07D493/04 , C07D231/56 , C07D333/72 , C07D519/00
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 the following formula or its pharmaceutically acceptable salt: wherein ring A is R4 is —Y—Z, hydrogen atom, halogen, hydroxy and the like, R5 is hydrogen atom, halogen, hydroxy and the like, R6 is each independently halogen, hydroxy, carboxy and the like, ring A may be substituted with said R6 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, R1 is —Y—Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like, R2 and R3 are each independently —Y—Z or hydrogen atom, provided that at least one of R1, R2, R3 and R4 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—, —NR7—, —C(═O)—, —SO—, —SO2—, —NR7—C(═O)—, —C(═O)—NR7—, —NR7—C(═O)—NR7—, —O—C(═O)—NR7—, —NR7—C(═O)—O—, —SO2—NR7—, —NR7—SO2—, 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, R7 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.

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