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1. 发明申请

US20140323722A1 OXADIAZOLE DERIVATIVE HAVING ENDOTHELIAL LIPASE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有内皮脂肪酶抑制活性的氧化氮衍生物
公开(公告)号：US20140323722A1
公开(公告)日：2014-10-30
申请号：US14264857
申请日：2014-04-29
申请人： Shionogi & Co., Ltd.
发明人： Koji MASUDA , Shiro Kida , Naoki Yoshikawa , Manabu Katou , Terukazu Kato , Mado Nakajima , Eiichi Kojima , Mitsuhiro Yonehara
IPC分类号： C07D417/06 , C07D417/14 , C07D413/06
CPC分类号： A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/5377 , C07D413/06 , C07D417/06 , C07D417/14 , C07D513/04
摘要： A compound represented by formula: its pharmaceutically acceptable salt, or a solvate thereof. Ring B is substituted or unsubstituted nitrogen-containing hetero ring, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R2 and R3 taken together may form oxo, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R6 and R7 taken together with the adjacent carbon atom to which they are attached may form a substituted or unsubstituted ring, and n is an integer of 0 to 3.
摘要翻译：由下式表示的化合物：其药学上可接受的盐或其溶剂合物。环B是取代或未取代的含氮杂环，R2和R3各自独立地为氢，卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基或取代或未取代的烷氧基，R2和R3一起可以形成氧代，R4 是由下式表示的基团： - （CR 6 R 7）n -R 8，R 6和R 7各自独立地为氢，卤素，羟基，羧基，取代或未取代的烷基或取代或未取代的烷氧基，R 6和R 7与相邻碳原子一起它们所连接的基团可以形成取代或未取代的环，n为0〜3的整数。

2. 发明授权

US09890119B2 Indole and azaindole derivative having AMPK-activating activity 有权
公开(公告)号：US09890119B2
公开(公告)日：2018-02-13
申请号：US14413337
申请日：2014-02-26
申请人： SHIONOGI & CO., LTD.
发明人： Yuusuke Tamura , Eiichi Kojima , Hidaka Ikemoto , Yu Hinata
IPC分类号： A61K31/5377 , A61K31/4045 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D493/04 , C07D209/34 , C07D209/42 , C07D519/00 , C07H17/02
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═ or —N═; 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; and R4, R7 and R8 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocyclyl.

3. 发明申请

US20150203450A1 INDOLE AND AZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 有权
标题翻译：具有AMPK活化活性的吲哚和吖啶衍生物
公开(公告)号：US20150203450A1
公开(公告)日：2015-07-23
申请号：US14413337
申请日：2014-02-26
申请人： SHIONOGI & CO., LTD
发明人： Yuusuke Tamura , Eiichi Kojima , Hidaka Ikemoto , Yu Hinata
IPC分类号： C07D209/34 , C07D471/04 , C07D405/12 , C07D493/04 , C07D519/00
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： Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or its pharmaceutically acceptable salt, wherein Y 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; T is —CR7═ or —N═; U is —CR8═ or —N═; R2 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; R3 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; and R4, R7 and R8 are each independently hydrogen, 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.
摘要翻译：公开了可用作AMPK活化剂的化合物。取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基，取代或未取代的环烯基，或取代或未取代的杂环基; T为-CR7 =或-N =; U为-CR8 =或-N =; 取代或未取代的酰基，取代或未取代的氨基甲酰基，取代或未取代的烷硫基，取代或未取代的烷基亚磺酰基，取代或未取代的烷基磺酰基，或取代或未取代的烷基磺酰基，未取代的烷氧基羰基; 取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基，取代或未取代的环烯基，取代或未取代的杂环基等; 取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基取代或未取代的环烯基，取代或未取代的杂环基等。

4. 发明授权

US10093670B2 Azabenzimidazole derivative having AMPK-activating activity 有权
公开(公告)号：US10093670B2
公开(公告)日：2018-10-09
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 , C07D519/00 , C07D451/06
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.

5. 发明授权

US11685740B2 Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same 有权
公开(公告)号：US11685740B2
公开(公告)日：2023-06-27
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 , A61P25/24 , A61P25/28 , A61P25/04
CPC分类号： C07D487/04 , A61P25/04 , A61P25/28 , C07D471/04 , C07D473/18 , C07D498/04
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.

6. 发明授权

US11066409B2 Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same 有权
公开(公告)号：US11066409B2
公开(公告)日：2021-07-20
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 , 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. The compound represented by Formula (I): wherein the symbols are defined in the specification, or a pharmaceutically acceptable salt thereof.

7. 发明授权

US10123994B2 Heterocyclic derivative having AMPK-activating activity 有权
公开(公告)号：US10123994B2
公开(公告)日：2018-11-13
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 , A61K31/382 , A61K31/34 , A61K31/5375 , A61K31/415
摘要： A compound of formula: or its pharmaceutically acceptable salt. L is NR2R3, SR7, SO2R8, alkyl, or alkenyl; R2 is hydrogen, alkyl, alkenyl, or alkynyl; R3 is hydrogen, alkyl, alkenyl, alkynyl; R7 is hydrogen, alkyl, alkenyl, or alkynyl; R8 is hydrogen, alkyl, alkenyl, or alkynyl, provided that R8 is not unsubstituted methyl or trifluoromethyl; Y is alkyl, alkenyl, alkynyl, aryl, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR6═, or —N═; R1 is hydrogen, or alkyl; R4, R5 and R6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, alkyl, alkenyl, or alkynyl.

8. 发明授权

US09980948B2 Azaindole derivative having AMPK-activating activity 有权
公开(公告)号：US09980948B2
公开(公告)日：2018-05-29
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： C07D401/02 , C07D401/10 , C07D401/14 , A61K31/437 , A61K31/4353 , A61K31/444 , A61K31/5377 , C07D471/04 , C07D519/00 , A61K31/03 , A61K31/10 , 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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