公开(公告)号：EP3290424A1

公开(公告)日：2018-03-07

申请号：EP16786500.5

申请日：2016-04-27

申请人： Shionogi & Co., Ltd

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： C07D498/14 ,  C07D513/14 ,  C07D491/22 ,  C07D471/14 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/53 ,  A61P31/16

CPC分类号： C07D498/14 ,  A61K31/53 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K31/675 ,  A61P31/16 ,  C07C2601/08 ,  C07C2601/16 ,  C07D471/14 ,  C07D471/20 ,  C07D491/22 ,  C07D513/14 ,  C07D519/00 ,  C07F7/1804 ,  C07F9/6561

摘要： The present inventon provides the following compounds having anti-viral activity.

A 1 is CR 1A R 1B , S or O;
A 2 is CR 2A R 2B , S or O;
A 3 is CR 3A R 3B , S or O;
A 4 is CR 4A R 4B , S or O;
the number of hetero atoms among atoms constituting the ring which consists of A 1 , A 2 , A 3 , A 4 , nitrogen atom adjacent to A 1 and carbon atom adjacent to A 1 , is 1 or 2;
R 1A and R 1B are each independently hydrogen, halogen, alkyl, or the like;
R 2A and R 2B are each independently hydrogen, halogen, alkyl, or the like;
R 3A and R 3B are each independently hydrogen, halogen, alkyl, or the like;
R 4A and R 4B are each independently hydrogen, halogen, alkyl, or the like;
R 3A and R 3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle;
X is CH 2 , S or O;
R 1 is each independently halogen, hydroxy, or the like;
m is any integer of 0 to 2; and
n is any integer of 1 to 2.

摘要翻译： 本发明提供了具有抗病毒活性的下列化合物。 A1是CR1AR1B，S或O; A2是CR2AR2B，S或O; A3是CR3AR3B，S或O; A4是CR4AR4B，S或O; 构成由A1，A2，A3，A4，与A1相邻的氮原子和与A1相邻的碳原子构成的环的原子中的杂原子数为1或2; R1A和R1B各自独立地为氢，卤素，烷基等; R2A和R2B各自独立地为氢，卤素，烷基等; R3A和R3B各自独立地为氢，卤素，烷基等; R4A和R4B各自独立地为氢，卤素，烷基等; R3A和R3B可以一起形成非芳族碳环或非芳族杂环; X是CH2，S或O; R1各自独立地为卤素，羟基等; m是0至2的任何整数; 并且n是1至2的任何整数。

公开(公告)号：EP3498281A1

公开(公告)日：2019-06-19

申请号：EP17839530.7

申请日：2017-08-09

申请人： Shionogi & Co., Ltd.

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： A61K31/5383 ,  A61P31/12 ,  A61P31/16 ,  A61P43/00

摘要： The present invention provides a pharmaceutical composition containing the following compound having antiviral action:

P is hydrogen or a group to form a prodrug.

公开(公告)号：EP4238960A8

公开(公告)日：2023-11-22

申请号：EP21886259.7

申请日：2021-10-27

申请人： Shionogi & Co., Ltd. ,  UBE Corporation

发明人： OKANO, Azusa ,  TATENO, Yusuke ,  NODU, Kouhei ,  SUZUKI, Shinji ,  AKIYAMA, Toshiyuki ,  MATOYAMA, Masaaki ,  AKAZA, Hiroto ,  FUKUDA, Takashi

IPC分类号： C07D20060101

摘要： The present invention provides a compound represented by formula (I) :

wherein the dashed line indicates the presence or absence of a bond; R 1 is carboxy or the like; L is substituted or unsubstituted non-aromatic carbocyclyldiyl or the like; R 2 is substituted or unsubstituted alkyl; R 3 is a hydrogen atom or the like; X is =CR X -or =N-; Y is =CR Y - or =N-; U is -CR U = or -N=; V is -CR V = or -N=; W is =CR W - or =N-; Z A is -C= or -N-; Z B is -CR 5 R 6 - or the like; Z C is -CR 7 R 8 - or the like; R X , R Y , R V and R W are each independently a hydrogen atom or the like; R U is a hydrogen atom or the like; R 5 and R 6 are each independently a hydrogen atom or the like; R 7 and R 8 are each independently a hydrogen atom or the like; R 4 is substituted or unsubstituted alkyloxy or the like,
or a pharmaceutically acceptable salt thereof, having an antiviral activity; and a pharmaceutical composition comprising the same.

公开(公告)号：EP4238960A1

公开(公告)日：2023-09-06

申请号：EP21886259.7

申请日：2021-10-27

申请人： Shionogi & Co., Ltd ,  UBE Corporation

发明人： OKANO, Azusa ,  TATENO, Yusuke ,  NODU, Kouhei ,  SUZUKI, Shinji ,  AKIYAMA, Toshiyuki ,  MATOYAMA, Masaaki ,  AKAZA, Hiroto ,  FUKUDA, Takashi

IPC分类号： C07D20060101

摘要： The present invention provides a compound represented by formula (I) :

wherein the dashed line indicates the presence or absence of a bond; R 1 is carboxy or the like; L is substituted or unsubstituted non-aromatic carbocyclyldiyl or the like; R 2 is substituted or unsubstituted alkyl; R 3 is a hydrogen atom or the like; X is =CR X -or =N-; Y is =CR Y - or =N-; U is -CR U = or -N=; V is -CR V = or -N=; W is =CR W - or =N-; Z A is -C= or -N-; Z B is -CR 5 R 6 - or the like; Z C is -CR 7 R 8 - or the like; R X , R Y , R V and R W are each independently a hydrogen atom or the like; R U is a hydrogen atom or the like; R 5 and R 6 are each independently a hydrogen atom or the like; R 7 and R 8 are each independently a hydrogen atom or the like; R 4 is substituted or unsubstituted alkyloxy or the like,
or a pharmaceutically acceptable salt thereof, having an antiviral activity; and a pharmaceutical composition comprising the same.

公开(公告)号：EP4424314A2

公开(公告)日：2024-09-04

申请号：EP24172424.4

申请日：2016-04-27

申请人： Shionogi & Co., Ltd

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： A61K31/5383

CPC分类号： A61K9/0014 ,  A61K9/0019 ,  A61K9/0056 ,  A61K9/0075 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/1611 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/7038 ,  A61K47/06 ,  A61K47/26 ,  A61P31/00 ,  A61P31/16 ,  C07D498/14 ,  C07F7/1804 ,  C07F9/6561

摘要： The present inventon provides the following compounds having anti-viral activity.

A1 is CR1A R1B, S or O;
A2 is CR2A R2B, S or O;
A3 is CR3AR3B, S or O;
A4 is CR4AR4B, S or O;
the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2;
R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like;
R3A and R3B are each independently hydrogen, halogen, alkyl, or the like;
R4A and R4B are each independently hydrogen, halogen, alkyl, or the like;
R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle;
X is CH2, S or O;
R1 is each independently halogen, hydroxy, or the like;
m is any integer of 0 to 2; and
n is any integer of 1 to 2.

公开(公告)号：EP4219508A1

公开(公告)日：2023-08-02

申请号：EP23150186.7

申请日：2016-04-27

申请人： Shionogi & Co., Ltd

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： C07D498/14 ,  A61P31/16 ,  A61K31/5383

摘要： The present inventon provides the following compounds having anti-viral activity.

A 1 is CR 1A R 1B , S or O;
A 2 is CR 2A R 2B , S or O;
A 3 is CR 3A R 3B , S or O;
A 4 is CR 4A R 4B , S or O;
the number of hetero atoms among atoms constituting the ring which consists of A 1 , A 2 , A 3 , A 4 , nitrogen atom adjacent to A 1 and carbon atom adjacent to A 1 , is 1 or 2;
R 1A and R 1B are each independently hydrogen, halogen, alkyl, or the like;
R 2A and R 2B are each independently hydrogen, halogen, alkyl, or the like;
R 3A and R 3B are each independently hydrogen, halogen, alkyl, or the like;
R 4A and R 4B are each independently hydrogen, halogen, alkyl, or the like;
R 3A and R 3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle;
X is CH 2 , S or O;
R 1 is each independently halogen, hydroxy, or the like;
m is any integer of 0 to 2; and
n is any integer of 1 to 2.

公开(公告)号：EP3428170A1

公开(公告)日：2019-01-16

申请号：EP18189193.8

申请日：2016-04-27

申请人： SHIONOGI & CO., LTD

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： C07D498/14 ,  A61P31/16 ,  A61K31/5383

摘要： The present inventon provides the following compounds having anti-viral activity.

公开(公告)号：EP4458348A2

公开(公告)日：2024-11-06

申请号：EP24190015.8

申请日：2017-08-09

申请人： Shionogi & Co., Ltd

发明人： KAWAI, Makoto ,  TOMITA, Kenji ,  AKIYAMA, Toshiyuki ,  OKANO, Azusa ,  MIYAGAWA, Masayoshi

IPC分类号： A61K9/06

摘要： The present invention provides a pharmaceutical composition containing the following compound having antiviral action:

P is hydrogen or a group to form a prodrug;
A 1 is CR 1 A R 1 B , S or O;
A 2 is CR 2 A R 2 B , S or O;
A 3 is CR 3 A R 3 B , S or O;
A 4 is each independently CR 4 A R 4 B , S or O;
the number of hetero atoms among atoms constituting the ring which consists of A 1 ,
A 2 , A 3 , A 4 , nitrogen atom adjacent to A 1 and carbon atom adjacent to A 4 , is 1 or 2;
R 1 A and R 1 B are each independently hydrogen, halogen, alkyl, or the like;
R 2 A and R 2 B are each independently hydrogen, halogen, alkyl, or the like;
R 3 A and R 3 B are each independently hydrogen, halogen, alkyl, or the like;
R 4 A and R 4 B are each independently hydrogen, halogen, alkyl, or the like;
R 3 A and R 3 B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle;
R 1 is fluorine;
m is any integer of 1 to 2; and
n is any integer of 1 to 2.

公开(公告)号：EP3192794A1

公开(公告)日：2017-07-19

申请号：EP15839901.4

申请日：2015-09-10

申请人： Shionogi & Co., Ltd.

发明人： KAWASUJI, Takashi ,  MIKAMIYAMA, Hidenori ,  SUZUKI, Naoyuki ,  MASUDA, Koji ,  SUGIMOTO, Hideki ,  OKANO, Azusa ,  YOSHIDA, Miho ,  SUGIYAMA, Shuichi ,  ASAHI, Kentarou ,  KOZONO, Iori ,  MIYAZAKI, Keisuke ,  OZASA, Hiroki ,  MIYAGAWA, Masayoshi

IPC分类号： C07D409/12 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/416 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4525 ,  A61P31/18 ,  A61P43/00 ,  C07D493/04 ,  C12N9/99

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 formula or its pharmaceutically acceptable salt Formula:

wherein ring A is

R 4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like,
R 5 is hydrogen atom, halogen, hydroxy and the like,
R 6 is each independently halogen, hydroxy, carboxy and the like,
ring A may be substituted with said R 6 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,
R 1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like,
R 2 and R 3 are each independently -Y-Z or hydrogen atom,
provided that at least one of R 1 , R 2 , R 3 and R 4 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-, -NR 7 -, -C(=O)-, -SO-, -SO 2 -, -NR 7 -C(=O)-, -C(=O)-NR 7 -, -NR 7 -C(=O)-NR 7 -, -NR 7 -C(=O)-O-, -SO 2 -NR 7 -, -NR 7 -SO 2 -, 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,
R 7 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.

摘要翻译： 本发明提供了用于HIV蛋白酶抑制剂的有用化合物。 由式或其药学上可接受的盐表示的化合物或其药学上可接受的盐式：其中环A为R 4为-YZ，氢原子，卤素，羟基等，R 5为氢原子，卤素，羟基等，R 6各自独立地为卤素，羟基 ，羧基等，环A可以在任何可取代的位置被所述R6取代，a是0-7的整数，环B是取代或未取代的芳族碳环基或取代或未取代的芳族杂环基，环C是 取代或未取代的芳族碳环基，取代或未取代的非芳族碳环基，取代或未取代的芳族杂环基或取代或未取代的非芳族杂环基，R1是-YZ，取代或未取代的烷基，取代或未取代的烯基， 例如，R2和R3各自独立地是-YZ或氢原子，条件是R1，R2，R3和R4中的至少一个是由式-YZ表示的基团， Y是键，或选自-O - ， - S - ， - NR 7 - ， - C（= O） - ， - SO - ， - SO 2 - ， - NR 7 -C （= O）-NR 7 - ， - NR 7 -C（= O）-NR 7 - ， - NR 7 -C（= O）-O - ， - SO 2 -NR 7 - ，取代或未取代的亚烷基，取代或未取代的亚烯基，取代或未取代的亚炔基，取代或未取代的芳族碳环基，取代或未取代的非芳族碳环基，取代或未取代的芳族杂环二基和取代或未取代的非芳族杂环二基， ，羟基，羧基等，Z是取代的芳族碳环基，取代的非芳族碳环基，取代的芳族杂环基或取代的非芳族杂环基。