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1. 发明公开

EP3279187A1 9-MEMBERED FUSED RING DERIVATIVE 有权
标题翻译： 9成员融合环状衍生物
公开(公告)号：EP3279187A1
公开(公告)日：2018-02-07
申请号：EP16772963.1
申请日：2016-03-30
申请人： Shionogi & Co., Ltd.
发明人： OHYABU, Naoki , KURAHASHI, Kana , NISHIURA, Yuji , KATOU, Manabu , MIYAZAKI, Keisuke , SASAKI, Yoshikazu , WADA, Toshihiro , IWATSU, Masafumi
IPC分类号： C07D235/26 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/506 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P25/02 , A61P27/02 , A61P31/00 , A61P35/00 , A61P43/00 , C07D235/28 , C07D401/04
CPC分类号： C07D235/26 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/506 , A61P3/06 , A61P3/08 , A61P9/00 , C07D235/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D493/04
摘要： The purpose of the present invention is to provide novel compounds having ACC2 selective inhibitory activity. In addition, the present invention provides a pharmaceutical composition comprising the compound. A compound of Formula:

or its pharmaceutically acceptable salt,
wherein, R 1 is substituted or unsubstituted fused aromatic heterocyclyl represented by Formula:

wherein,
ring B is 5-membered ring, ring C is 6-membered ring;
ring A is substituted or unsubstituted non-aromatic carbocycle or the like;

-L 1 - is -O-(CR 6 R 7 )m- or the like;
-L 2 - is -O-(CR 6 R 7 )n- or the like;
each R 6 is independently hydrogen or the like;
each R 7 is independently hydrogen or the like;
each m is independently an integer of 0, 1, 2 or 3;
each n is independently an integer of 1, 2 or 3;
R 2 is substituted or unsubstituted alkyl;
R 3 is hydrogen or substituted or unsubstituted alkyl;
R 4 is substituted or unsubstituted alkylcarbonyl or the like.
摘要翻译：本发明的目的是提供具有ACC2选择性抑制活性的新型化合物。此外，本发明提供了包含该化合物的药物组合物。一种下式的化合物或其药学上可接受的盐，其中，R1是取代或未取代的由下式表示的稠合芳族杂环基：其中，环B为5元环，环C为6元环; 环A是取代或未取代的非芳族碳环等; -L 1 - 是-O-（CR 6 R 7）m - 等; -L 2 - 为-O-（CR 6 R 7）n - 等; 每个R6独立地为氢等; 每个R 7独立地为氢等; 每个m独立地为0,1,2或3的整数; 每个n独立地是1,2或3的整数; R2是取代或未取代的烷基; R3是氢或取代或未取代的烷基; R4是取代或未取代的烷基羰基等。

2. 发明公开

EP3670496A3 ACC2 INHIBITORS 审中-公开
公开(公告)号：EP3670496A3
公开(公告)日：2020-09-30
申请号：EP20151537.6
申请日：2014-10-17
申请人： Shionogi & Co., Ltd.
发明人： KOBAYASHI, Naotake , ASAHI, Kentarou , TOMIDA, Yutaka , OHDAN, Masahide , FUMOTO, Masataka , SASAKI, Yoshikazu , KURAHASHI, Kana , INOUE, Takatsugu , URABE, Tomomi , NISHIURA, Yuji , IWATSU, Masafumi , MIYAZAKI, Keisuke , OHYABU, Naoki , WADA, Toshihiro , KATOU, Manabu
IPC分类号： C07C233/18 , A61K31/165 , A61K31/17 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/4725 , A61K31/4965 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/553 , A61P3/04 , A61P3/10 , A61P43/00 , C07C233/31 , C07C275/24 , C07D213/64 , C07D213/69 , C07D231/56
摘要： The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound.
A compound of formula (I):

wherein
R 1 is substituted or unsubstituted fused aromatic heterocyclyl etc.,
ring A is substituted or unsubstituted non-aromatic carbocycle etc.,
-L 1 - is -O-(CR 6 R 7 )m- etc.,
-L 2 - is -O-(CR 6 R 7 )n- etc.,
each R 6 and R 7 are independently hydrogen, halogen etc.,
R 2 is substituted or unsubstituted alkyl,
R 3 is hydrogen or substituted or unsubstituted alkyl,
R 4 is substituted or unsubstituted alkylcarbonyl etc..

3. 发明公开

EP3670496A2 ACC2 INHIBITORS 审中-公开
公开(公告)号：EP3670496A2
公开(公告)日：2020-06-24
申请号：EP20151537.6
申请日：2014-10-17
申请人： Shionogi & Co., Ltd.
发明人： KOBAYASHI, Naotake , ASAHI, Kentarou , TOMIDA, Yutaka , OHDAN, Masahide , FUMOTO, Masataka , SASAKI, Yoshikazu , KURAHASHI, Kana , INOUE, Takatsugu , URABE, Tomomi , NISHIURA, Yuji , IWATSU, Masafumi , MIYAZAKI, Keisuke , OHYABU, Naoki , WADA, Toshihiro , KATOU, Manabu
IPC分类号： C07C233/18 , A61K31/165 , A61K31/17 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/4725 , A61K31/4965 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/553 , A61P3/04 , A61P3/10 , A61P43/00 , C07C233/31 , C07C275/24 , C07D213/64 , C07D213/69 , C07D231/56
摘要： The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound.
A compound of formula (I):

wherein
R 1 is substituted or unsubstituted fused aromatic heterocyclyl etc.,
ring A is substituted or unsubstituted non-aromatic carbocycle etc.,
-L 1 - is -O-(CR 6 R 7 )m- etc.,
-L 2 - is -O-(CR 6 R 7 )n- etc.,
each R 6 and R 7 are independently hydrogen, halogen etc.,
R 2 is substituted or unsubstituted alkyl,
R 3 is hydrogen or substituted or unsubstituted alkyl,
R 4 is substituted or unsubstituted alkylcarbonyl etc..

4. 发明公开

EP4043463A1 FUSED RING DERIVATIVE HAVING MGAT-2 INHIBITORY ACTIVITY 审中-实审
公开(公告)号：EP4043463A1
公开(公告)日：2022-08-17
申请号：EP22165122.7
申请日：2018-07-13
申请人： Shionogi & Co., Ltd
发明人： NODU, Kouhei , TATENO, Yusuke , MASUDA, Kengo , NISHIURA, Yuji , SASAKI, Yoshikazu , NODU, KouheiHINATA, Yu
IPC分类号： C07D471/04 , A61K31/438 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/527 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D471/10 , C07D491/20 , C07D471/20 , C07D487/10 , C07D491/147
摘要： The present inventon provides the compound represented by the following formula (I):

wherein a moiety represented by formula:

is

or the like;
y is 0 or 1; R 1 is hydrogen or the like; R 2a and R 2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R 3a is hydrogen or the like; R 3b is hydrogen or the like; R 4a is represented by formula:

: L 1 is a single bond or the like; L 2 is -C(=O)- or the like; L 3 is a single bond or the like; R 7 is substituted or unsubstituted alkyl or the like; R 4b is substituted or unsubstituted alkyl or the like; R 4c is each independently halogen or the like.

5. 发明公开

EP3450435A1 5-SUBSTITUTED AZABENZIMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATION ACTION 审中-公开
公开(公告)号：EP3450435A1
公开(公告)日：2019-03-06
申请号：EP17789570.3
申请日：2017-04-26
申请人： Shionogi & Co., Ltd
发明人： TAMURA, Yuusuke , SASAKI, Yoshikazu
IPC分类号： C07D519/00 , A61K31/437 , A61P3/10 , A61P43/00 , C07D471/04
摘要： Provided is a compound which is useful as an AMPK activator. A compound represented by formula:

wherein
L is -NR 1 -, =N-, -O-, -S-, -SO 2 -, -CR 2 R 3 -, or =CR 2 -; dashed line indicates the presence or absence of a bond;
X is -CR 4 R 5 -, or -O-;
Y is substituted or unsubstituted heteroaryl, or substituted or unsubstituted heterocyclyl;
Z is =CR 6 -, or =N-;
R 1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like;
R 2 and R 3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like;
R 4 and R 5 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like;
R 6 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like;
R 7 , R 8 and R 9 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like;
R 10 and R 11 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like; and
R 12 is hydrogen or substituted or unsubstituted alkyl, or its pharmaceutically acceptable salt.

6. 发明公开

EP3059225A1 NOVEL ALKYLENE DERIVATIVE 审中-公开
标题翻译： NEUARTIGE ALKYLENDERIVATE
公开(公告)号：EP3059225A1
公开(公告)日：2016-08-24
申请号：EP14853664.2
申请日：2014-10-17
申请人： Shionogi & Co., Ltd.
发明人： KOBAYASHI, Naotake , ASAHI, Kentarou , TOMIDA, Yutaka , OHDAN, Masahide , FUMOTO, Masataka , SASAKI, Yoshikazu , KURAHASHI, Kana , INOUE, Takatsugu , URABE, Tomomi , NISHIURA, Yuji , IWATSU, Masafumi , MIYAZAKI, Keisuke , OHYABU, Naoki , WADA, Toshihiro , KATOU, Manabu
IPC分类号： C07C233/18 , A61K31/165 , A61K31/17 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/4725 , A61K31/4965 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/553 , A61P3/04 , A61P3/10 , A61P43/00 , C07C233/31 , C07C275/24 , C07D213/64 , C07D213/69 , C07D231/56
CPC分类号： C07C233/22 , C07C233/18 , C07C233/31 , C07C275/10 , C07C2601/02 , C07D213/64 , C07D213/69 , C07D231/56 , C07D239/80 , C07D241/18 , C07D261/20 , C07D263/56 , C07D267/14 , C07D277/20 , C07D277/34 , C07D277/64 , C07D277/68 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12
摘要： The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound.
A compound of formula (I):

wherein R 1 is substituted or unsubstituted fused aromatic heterocyclyl etc., ring A is substituted or unsubstituted non-aromatic carbocycle etc.,
-L 1 - is -O-(CR 6 R 7 )m- etc.,
-L 2 - is -O-(CR 6 R 7 )n- etc.,
each R 6 and R 7 are independently hydrogen, halogen etc.,
R 2 is substituted or unsubstituted alkyl,
R 3 is hydrogen or substituted or unsubstituted alkyl,
R 4 is substituted or unsubstituted alkylcarbonyl etc..
摘要翻译：本发明的目的是提供具有ACC2抑制活性的新型化合物。此外，本发明的目的是提供一种包含该化合物的药物组合物。式（I）的化合物：其中R 1是取代或未取代的稠合芳族杂环基等，环A是取代或未取代的非芳族碳环等，-L 1 - 是-O-（CR 6 R 7）m- 等等，-L 2 - 为-O-（CR 6 R 7）n - 等，每个R 6和R 7独立地为氢，卤素等，R 2为取代或未取代的烷基，R 3为氢或取代或未取代的烷基，R 4为取代或未取代的烷基羰基等。

7. 发明公开

EP3395798A1 NON-AROMATIC HETEROCYCLIC DERIVATIVE HAVING MGAT2 INHIBITORY ACTIVITY 审中-公开
公开(公告)号：EP3395798A1
公开(公告)日：2018-10-31
申请号：EP16878728.1
申请日：2016-12-21
申请人： Shionogi & Co., Ltd
发明人： NISHIURA, Yuji , KURAHASHI, Kana , OHYABU, Naoki , SASAKI, Yoshikazu
IPC分类号： C07D211/86 , A61K31/435 , A61K31/444 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： A61K31/444 , A61K31/435 , A61K31/4439 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07D211/86 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to a compound represented by Formula (I):

wherein X is, for example, C(=O); Z is, for example, C(=O); L is, for example, a single bond; A is, for example, aromatic carbocycle; R is, for example, R 6 or B; R 2 is, for example, hydrogen; R 3 is, for example, substituted or unsubstituted alkyl; R 4a is, for example, hydrogen; R 4b is, for example, hydrogen; R 5 is, for example, halogen; R 6 is, for example, halogen; R 7a is, for example, hydrogen; R 7b is, for example, hydrogen; R 8 is, for example, hydrogen; R 9 is, for example, hydrogen; m is 0 to 5; n is 0 to 5; and p is 1 to 6, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

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