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1. 发明申请

US20200048257A1 BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
公开(公告)号：US20200048257A1
公开(公告)日：2020-02-13
申请号：US16340467
申请日：2017-10-16
申请人： Shionogi & Co., Ltd.
发明人： Koji MASUDA , Shuichi SUGIYAMA , Toru YAMADA , Eiichi KOJIMA , Tomoyuki OGAWA , Naotake KOBAYASHI , Hiroyuki KAI
IPC分类号： C07D487/04 , C07D498/04 , C07D471/04 , C07D473/18
摘要： Provided are a novel compound having an antagonistic activity for the P2X7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X7 receptor. The compound represented by Formula (I): wherein the symbols are defined in the specification, or a pharmaceutically acceptable salt thereof.

2. 发明申请

US20210317125A1 BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 有权
公开(公告)号：US20210317125A1
公开(公告)日：2021-10-14
申请号：US17349042
申请日：2021-06-16
申请人： Shionogi & Co., Ltd.
发明人： Koji MASUDA , Shuichi SUGIYAMA , Toru YAMADA , Eiichi KOJIMA , Tomoyuki OGAWA , Naotake KOBAYASHI , Hiroyuki KAI
IPC分类号： C07D487/04 , C07D471/04 , C07D473/18 , C07D498/04 , A61P25/04
摘要： Provided are a novel compound having an antagonistic activity for the P2X7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X7 receptor. A compound represented by Formula (I): wherein Z1 is C(R4) or the like; R4 is a hydrogen atom or the like; Z2 is C(R5a)(R5a′) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R5a′ is absent; R5a and R5a′ are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y1 is O or the like; R2a is a group represented by the formula: —(C(R2a′)(R2b′))n—R1; R2b is a hydrogen atom or the like; R2a′ and R2b′ is each independently a hydrogen atom or the like; R1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R7a) or the like; R7a is a hydrogen atom or the like; R3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.

3. 发明申请

US20170107219A1 AZABENZIMIDAZOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 审中-公开
公开(公告)号：US20170107219A1
公开(公告)日：2017-04-20
申请号：US15390933
申请日：2016-12-27
申请人： Shionogi & Co., Ltd.
发明人： Eiichi KOJIMA , Keisuke Tonogaki , Nobuyuki Tanaka , Manabu Katou , Akira Ino , Masafumi Iwatsu , Masahiko Fujioka , Yu Hinata , Naoki Ohyabu
IPC分类号： C07D471/04 , C07F9/6561
CPC分类号： C07D471/04 , C07D451/06 , C07D519/00 , C07F9/6561
摘要： Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(═O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.

4. 发明申请

US20180141906A1 INDOLE AND AZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 审中-公开
公开(公告)号：US20180141906A1
公开(公告)日：2018-05-24
申请号：US15876535
申请日：2018-01-22
申请人： SHIONOGI & CO. , LTD.
发明人： Yuusuke TAMURA , Eiichi KOJIMA , Yu HINATA
IPC分类号： C07D209/34 , A61K31/5377 , C07D405/12 , C07D471/04 , C07D493/04 , A61K31/4045 , C07D519/00 , C07H17/02 , C07D403/12 , C07D413/12 , C07D209/42
CPC分类号： C07D209/34 , A61K31/4045 , A61K31/5377 , C07D209/42 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D493/04 , C07D519/00 , C07H17/02
摘要： A compound is represented by formula: or its pharmaceutically acceptable salt, wherein Y is substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocyclyl; T is —CR7═; U is —CR8═ or —N═; R2 is hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, alkenyl, acyl, carbamoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, or alkyloxycarbonyl; R3 is halogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl; R4 and R8 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocyclyl; and R7 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl, alkyloxy, aryloxy, heteroaryloxy, cycloalkyloxy, cycloalkenyloxy, heterocyclyloxy, alkylthio, arylthio, heteroarylthio, cycloalkylthio, cycloalkenylthio, heterocyclylthio, alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, cycloalkylsulfonyl, cycloalkenylsulfonyl, heterocyclylsulfonyl, acyl, carbamoyl, sulfamoyl, or amino.

5. 发明申请

US20170333398A1 HETEROCYCLIC DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 审中-公开
公开(公告)号：US20170333398A1
公开(公告)日：2017-11-23
申请号：US15522504
申请日：2015-10-27
申请人： SHIONOGI & CO., LTD.
发明人： Eiichi KOJIMA , Yu HINATA , Toshihiro WADA
IPC分类号： A61K31/4188 , C07D419/14 , A61K31/415 , A61K31/382 , A61K31/5375 , A61K31/34
CPC分类号： A61K31/4188 , A61K31/34 , A61K31/382 , A61K31/415 , A61K31/4184 , A61K31/437 , A61K31/5375 , A61P3/00 , A61P3/10 , A61P9/12 , C07D235/26 , C07D419/14 , C07D471/04 , C07D493/04 , C07D519/00
摘要： A compound represented by formula: or its pharmaceutically acceptable salt, wherein L is NR2R3, SR7, SO2R8, substituted or unsubstituted alkyl, or substituted or unsubstituted alkenyl; R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R8 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like, provided that R8 is not unsubstituted methyl or trifluoromethyl; Y is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or the like, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR6═, or —N═; R1 is hydrogen, or substituted or unsubstituted alkyl; R4, R5 and R6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

6. 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.

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