公开(公告)号：EP2128134A1

公开(公告)日：2009-12-02

申请号：EP07830926.7

申请日：2007-10-31

申请人： Shionogi&Co., Ltd.

发明人： ENDOH, Takeshi ,  FUJII, Yasuhiko ,  KOJIMA, Eiichi ,  TADANO, Genta ,  YAMAGUCHI, Naoko ,  ADACHI, Yo ,  TAGASHIRA, Sachie ,  TACHIBANA, Yuki ,  ONODERA, Naohiro

IPC分类号： C07D209/08 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20

CPC分类号： C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20 ,  C07D241/04 ,  C07D243/08 ,  C07D263/32 ,  C07D277/28 ,  C07D295/22 ,  C07D295/26 ,  C07D307/81 ,  C07D307/91

摘要： A compound represented by the general formula (I):

wherein R 1 is

wherein R 26 and R 28 are each independently lower alkyloxy and the like; n 1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula:

wherein R 6 and R 7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R 2 is a hydrogen atom and the like; R 3 is optionally substituted lower alkyl and the like; R 4 is a hydrogen atom; or R 3 and R 4 may be taken together with an adjacent carbon atom to from a ring; R 5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 由通式（I）表示的化合物：其中R 1是其中R 26和R 28各自独立地为低级烷氧基等; n 1为0〜3的整数， Z是可以被选自取代基组a等的取代基中断的任选取代的C 1 -C 5亚炔基; A是由下式表示的基团：其中R 6和R 7各自独立地为低级烷基等; m和n各自独立地为0,1或2; R 2是氢原子等; R 3是任选取代的低级烷基等; R 4是氢原子; 或R 3和R 4可以与相邻的碳原子一起与环一起取代; R 5是羟基等，或光学活性异构体，其药学上可接受的盐或溶剂化物。

公开(公告)号：EP3214076A1

公开(公告)日：2017-09-06

申请号：EP15855481.6

申请日：2015-10-27

申请人： Shionogi & Co., Ltd.

发明人： KOJIMA, Eiichi ,  HINATA, Yu ,  WADA, Toshihiro

IPC分类号： C07D235/26 ,  A61K31/4184 ,  A61K31/437 ,  A61P43/00 ,  C07D471/04 ,  C07D519/00 ,  A61P3/10

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 NR 2 R 3 , SR 7 , SO 2 R 8 , substituted or unsubstituted alkyl, or substituted or unsubstituted alkenyl;
R 2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like;
R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like;
R 7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like;
R 8 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like, provided that R 8 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 -CR 6 =, or -N=;
R 1 is hydrogen, or substituted or unsubstituted alkyl;
R 4 , R 5 and R 6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

摘要翻译： 由下式表示的化合物或其药学上可接受的盐，其中L是NR2R3，SR7，SO2R8，取代或未取代的烷基或取代或未取代的烯基; R2是氢，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等; R3是氢，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等; R7是氢，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等; R8是氢，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等，条件是R8不是未取代的甲基或三氟甲基; Y是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等，条件是Y不是未取代的甲基或未取代的乙基; Z是-CR 6 =或-N =; R1是氢，或取代或未取代的烷基; R4，R5和R6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，取代或未取代的烯基，取代或未取代的炔基等。

公开(公告)号：EP1953145B1

公开(公告)日：2015-11-04

申请号：EP06832946.5

申请日：2006-11-20

申请人： Shionogi & Co., Ltd.

发明人： KUROSE, Noriyuki ,  HAYASHI, Mikayo ,  OGAWA, Tomoyuki ,  MASUDA, Koji ,  KOJIMA, Eiichi

IPC分类号： C07D231/18 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/662 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D231/18 ,  C07D231/20 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12 ,  C07D419/06 ,  C07D471/08 ,  C07D471/10 ,  C07D471/12

公开(公告)号：EP2617722A1

公开(公告)日：2013-07-24

申请号：EP11823623.1

申请日：2011-09-08

申请人： Shionogi & Co., Ltd.

发明人： TONOGAKI, Keisuke ,  INO, Akira ,  KOJIMA, Eiichi ,  KATOU, Manabu ,  IWATSU, Masafumi ,  TANAKA, Nobuyuki ,  FUJIOKA, Masahiko

IPC分类号： C07D471/04 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/52 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P43/00 ,  C07D473/00 ,  C07D495/04

CPC分类号： C07D471/04 ,  C07D473/00 ,  C07D473/06 ,  C07D473/28 ,  C07D473/30 ,  C07D487/04 ,  C07D491/048 ,  C07D491/08 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

摘要： Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula:

its pharmaceutically acceptable salt, or a solvate thereof,
wherein
a group represented by the formula:

is a group represented by the formula:

R 1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like;
m is an integer of 0 to 3;
R 2 is hydrogen, or substituted or unsubstituted alkyl;
X is -O-; and
Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

摘要翻译： 公开了可用作AMPK活化剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中由下式表示的基团是由下式表示的基团：R 1各自独立地为卤素，羟基，氰基，硝基，羧基，取代或 未取代的烷基，取代或未取代的链烯基等; m为0〜3的整数。 R 2是氢或取代或未取代的烷基; X为-O- 和Y是取代或未取代的芳基，或取代或未取代的杂芳基。

公开(公告)号：EP1953145A1

公开(公告)日：2008-08-06

申请号：EP06832946.5

申请日：2006-11-20

申请人： Shionogi & Co., Ltd.

发明人： KUROSE, Noriyuki ,  HAYASHI, Mikayo ,  OGAWA, Tomoyuki ,  MASUDA, Koji ,  KOJIMA, Eiichi

IPC分类号： C07D231/18 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/662 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D231/18 ,  C07D231/20 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12 ,  C07D419/06 ,  C07D471/08 ,  C07D471/10 ,  C07D471/12

摘要： Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor.
A compound represented by the formula:

a pharmaceutically acceptable salt or solvate thereof,
wherein
R 1 is optionally substituted alkyl or the like,
one of R 2 and R 4 is a group of formula: -Y-R 5 ,
wherein Y is -O- or the like,
R 5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like,
the other of R 2 and R 4 is hydrogen or optionally substituted alkyl,
R 3 is a group of formula: -C(=O)-Z-R 6 ,
wherein Z is -NR 7 - or -NR 7 -W-,
R 6 is optionally substituted cycloalkyl or the like,
R 7 is hydrogen or optionally substituted alkyl,
W is optionally substituted alkylene,
X is =N- or the like,
with the proviso that compounds wherein R 2 is 2-(morphorino)ethoxy, R 3 is N-(1-adamantyl)carbamoyl and R 1 is benzyl are excluded.

摘要翻译： 公开了可用作I 11 2羟基类固醇脱氢酶抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或溶剂合物，其中R 1是任选取代的烷基等，R 2和R 4之一是式-YR 5的基团，其中Y是-O-或 R 5为取代烷基（取代基为任选取代的环烷基等），任选取代的支链烷基等，R 2和R 4中的另一个为氢或任意取代的烷基，R 3为式 ：-C（= O）-ZR 6，其中Z为-NR 7 - 或-NR 7 -W-，R 6为任选取代的环烷基等，R 7为氢或任选取代的烷基，W为任选取代的亚烷基 ，X为= N-等，条件是其中R 2为2-（吗啉基）乙氧基，R 3为N-（1-金刚烷基）氨基甲酰基且R 1为苄基的化合物除外。

公开(公告)号：EP3187498A1

公开(公告)日：2017-07-05

申请号：EP15836882.9

申请日：2015-08-26

申请人： Shionogi & Co., Ltd.

发明人： TAMURA, Yuusuke ,  HINATA, Yu ,  KOJIMA, Eiichi ,  OZASA, Hiroki

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P43/00 ,  C07D519/00

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;
R 1 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;
R 2 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;
R 3 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
R 4 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

摘要翻译： 公开了用作AMPK激活剂的化合物。 由下式表示的化合物或其药学上可接受的盐，其中X是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， 或取代或未取代的杂环基; R1是氢，卤素，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的链烯基，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， 未取代的烷氧基羰基; R2是卤素，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; R3是卤素，羟基，氰基，硝基，羧基，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， 杂环基等; 和R4是氢，卤素，羟基，氰基，硝基，羧基，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等。

公开(公告)号：EP2617722B1

公开(公告)日：2016-03-23

申请号：EP11823623.1

申请日：2011-09-08

申请人： Shionogi & Co., Ltd.

发明人： TONOGAKI, Keisuke ,  INO, Akira ,  KOJIMA, Eiichi ,  KATOU, Manabu ,  IWATSU, Masafumi ,  TANAKA, Nobuyuki ,  FUJIOKA, Masahiko

IPC分类号： C07D471/04 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/52 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P43/00 ,  C07D473/00 ,  C07D495/04 ,  C07D491/08 ,  C07D473/06 ,  C07D473/28 ,  C07D473/30 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  C07D491/048

CPC分类号： C07D471/04 ,  C07D473/00 ,  C07D473/06 ,  C07D473/28 ,  C07D473/30 ,  C07D487/04 ,  C07D491/048 ,  C07D491/08 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

公开(公告)号：EP2963013A1

公开(公告)日：2016-01-06

申请号：EP14756889.3

申请日：2014-02-26

申请人： Shionogi & Co., Ltd.

发明人： TAMURA, Yuusuke ,  KOJIMA, Eiichi ,  IKEMOTO, Hidaka ,  HINATA, Yu

IPC分类号： C07D209/42 ,  A61K31/4045 ,  A61K31/5377 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/50 ,  A61P7/00 ,  A61P9/12 ,  A61P43/00 ,  C07D405/12 ,  C07D471/04 ,  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 -CR 7 = or -N=;
U is -CR 8 = or -N=;
R 2 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;
R 3 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
R 4 , R 7 and R 8 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是-CR 7 =或-N =; U是-CR 8 =或-N =; R 2为氢，卤素，氰基，硝基，羧基，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; R 4，R 7和R 8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，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， 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。

公开(公告)号：EP2514749B1

公开(公告)日：2015-02-25

申请号：EP10837586.6

申请日：2010-12-14

申请人： Shionogi & Co., Ltd.

发明人： MASUDA, Koji ,  KIDA, Shiro ,  YOSHIKAWA, Naoki ,  KATOU, Manabu ,  KATO, Terukazu ,  NAKAJIMA, Mado ,  KOJIMA, Eiichi ,  YONEHARA, Mitsuhiro

IPC分类号： C07D413/06 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P43/00 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

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

公开(公告)号：EP3527568A1

公开(公告)日：2019-08-21

申请号：EP17863024.0

申请日：2017-10-16

申请人： Shionogi & Co., Ltd

发明人： MASUDA, Koji ,  SUGIYAMA, Shuichi ,  YAMADA, Toru ,  KOJIMA, Eiichi ,  OGAWA, Tomoyuki ,  KOBAYASHI, Naotake ,  KAI, Hiroyuki

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5383 ,  A61P43/00 ,  C07D487/04 ,  C07D498/04

摘要： Provided are a novel compound having an antagonistic activity for the P2X 7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X 7 receptor. A compound represented by Formula (I):

wherein Z 1 is C(R 4 ) or the like; R 4 is a hydrogen atom or the like; Z 2 is C(R 5a )(R 5a' ) 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 R 5a' is absent; R 5a and R 5a' are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y 1 is O or the like; R 2a is a group represented by the formula: -(C(R 2a' )(R 2b' )) n -R 1 ; R 2b is a hydrogen atom or the like; R 2a' and R 2b' is each independently a hydrogen atom or the like; R 1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R 7a ) or the like; R 7a is a hydrogen atom or the like; R 3 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.