公开(公告)号：EP2025676A1

公开(公告)日：2009-02-18

申请号：EP07767066.9

申请日：2007-06-08

申请人： Ube Industries, Ltd. ,  SANTEN PHARMACEUTICAL CO., LTD.

发明人： HAGIHARA, Masahiko ,  TSUZAKI, Yasunori ,  KOMORI, Ken-ichi ,  NISHIDA, Hiroshi ,  KIDO, Kazutaka ,  FUJIMOTO, Tomokazu ,  MATSUGI, Takeshi ,  SHIMAZAKI, Atsushi

IPC分类号： C07D401/04 ,  A61K31/416 ,  A61K31/4439 ,  A61P1/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P15/06 ,  A61P19/10 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P29/00 ,  A61P31/04 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D231/56

CPC分类号： C07D231/56 ,  C07D401/04

摘要： An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; R 1 and R 2 represent halogen, H, OH, alkoxy, cycloalkyloxy, aryloxy, alkyl, cycloalkyl or the like; R 3 represents halogen, H or the like; R 4 and R 5 represent halogen, H or the like; R 6 and R 7 represent H, alkyl or the like; and m, n, p and q represent an integer of 0 to 3. In this connection, each group may have a substituent.

摘要翻译： 本发明的目的是在侧链中产生具有螺环结构的新颖的吲唑衍生物，其可用作药物，并找到衍生物的新的药理活性。 本发明化合物由通式[I]表示，具有优异的Rho激酶抑制活性。 在该式中，环X表示苯环或吡啶环; R 1和R 2表示卤素，H，OH，烷氧基，环烷氧基，芳氧基，烷基，环烷基等; R 3表示卤素，H等; R 4和R 5表示卤素，H等; R 6和R 7表示H，烷基等; m，n，p和q表示0〜3的整数。就此而言，各基团可以具有取代基。

公开(公告)号：EP2578219B1

公开(公告)日：2014-10-01

申请号：EP11786710.1

申请日：2011-05-26

申请人： Ube Industries, Ltd.

发明人： HAGIHARA, Masahiko ,  KOMORI, Ken-ichi ,  SUNAMOTO, Hidetoshi ,  NISHIDA, Hiroshi ,  TSUZAKI, Yasunori ,  TAKAMA, Akira ,  KIDO, Kazutaka ,  FUJIMOTO, Tomokazu ,  MATSUGI, Takeshi

IPC分类号： A61K31/4439 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P7/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P27/04 ,  A61P27/06

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/10 ,  C07D405/14

公开(公告)号：EP3333163A1

公开(公告)日：2018-06-13

申请号：EP16833140.3

申请日：2016-08-05

申请人： UBE Industries, Ltd.

发明人： KOMORI, Ken-ichi ,  NINOMIYA, Akishi ,  USHIYAMA, Shigeru ,  SHINOHARA, Masaru ,  ITO, Koji ,  KAWAGUCHI, Tetsuo ,  TOKUNAGA, Yasunori ,  KAWADA, Hiroyoshi ,  YAMADA, Haruka ,  SHIRAISHI, Yusuke ,  KOJIMA, Masahiro ,  ITO, Masaaki ,  KIMURA, Tomio

IPC分类号： C07D401/04 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  A61P3/10 ,  A61P13/12 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07F7/18

CPC分类号： A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07F7/18 ,  Y02P20/55

摘要： The present invention provides a compound of general formula (I) (wherein, R 1 , X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.

公开(公告)号：EP3705471A1

公开(公告)日：2020-09-09

申请号：EP18872421.5

申请日：2018-11-02

申请人： UBE Industries, Ltd.

发明人： YAMADA, Haruka ,  KOMORI, Ken-ichi ,  SHIRAISHI, Yusuke ,  UMEZAKI, Satoshi ,  KINOSHITA, Naoya ,  ITO, Koji ,  KANDA, Tomoko ,  YONEDA, Kenji ,  TOKUNAGA, Yasunori ,  KIMURA, Tomio

IPC分类号： C07C307/06 ,  A61K31/357 ,  A61P3/04 ,  C07C279/18 ,  C07D321/00

摘要： The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I):

[wherein: A 1 and A 2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A 1 to A 2 ] or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP2468729A1

公开(公告)日：2012-06-27

申请号：EP12160543.0

申请日：2004-10-15

申请人： UBE INDUSTRIES, LTD. ,  Santen Pharmaceutical Co., Ltd

发明人： HAGIHARA, Masahiko ,  KOMORI, Ken-ichi ,  SUNAMOTO, Hidetoshi ,  NISHIDA, Hiroshi ,  MATSUGI, Takeshi ,  NAKAJIMA, Tadashi ,  HATANO, Masakazu ,  KIDO, Kazutaka ,  HARA, Hideaki

IPC分类号： C07D231/56 ,  C07D401/04 ,  A61K31/416 ,  A61K31/4439 ,  A61P27/06 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： The invention relates to compounds of formula (I):

in which R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the description. These compounds are useful as Rho kinase inhibitors.

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，R 3，R 4，R 5和X如说明书中所定义。 这些化合物可用作Rho激酶抑制剂。

公开(公告)号：EP3978073A1

公开(公告)日：2022-04-06

申请号：EP20815167.0

申请日：2020-05-29

申请人： Ube Industries, Ltd.

发明人： KOMORI, Ken-ichi ,  NISHIYAMA, Hayato ,  KINOSHITA, Naoya ,  WADA, Yukinori ,  MORISHITA, Kousuke ,  NINOMIYA, Akishi ,  SHIRAISHI, Yuusuke ,  ONUMA, Kazuhiro ,  OGI, Sayaka ,  KAWADA, Hiroyoshi ,  KIMURA, Tomio

IPC分类号： A61P13/12 ,  A61P43/00 ,  C07D413/10 ,  C07D498/04 ,  A61K31/553

摘要： The present invention provides a compound having Keap1 inhibitory effects and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following general formula (I):

[wherein the symbols have the same meanings as those described in the description] or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.

公开(公告)号：EP2468729B1

公开(公告)日：2013-12-25

申请号：EP12160543.0

申请日：2004-10-15

申请人： Ube Industries, Ltd.

发明人： HAGIHARA, Masahiko ,  KOMORI, Ken-ichi ,  SUNAMOTO, Hidetoshi ,  NISHIDA, Hiroshi ,  MATSUGI, Takeshi ,  NAKAJIMA, Tadashi ,  HATANO, Masakazu ,  KIDO, Kazutaka ,  HARA, Hideaki

IPC分类号： C07D231/56 ,  C07D401/04 ,  A61K31/416 ,  A61K31/4439 ,  A61P27/06 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

摘要： An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; R 1 and R 2 are H or alkyl; R 3 and R 4 are halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R 5 is halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted.

公开(公告)号：EP2578219A1

公开(公告)日：2013-04-10

申请号：EP11786710.1

申请日：2011-05-26

申请人： Ube Industries, Ltd.

发明人： HAGIHARA, Masahiko ,  KOMORI, Ken-ichi ,  SUNAMOTO, Hidetoshi ,  NISHIDA, Hiroshi ,  TSUZAKI, Yasunori ,  TAKAMA, Akira ,  KIDO, Kazutaka ,  FUJIMOTO, Tomokazu ,  MATSUGI, Takeshi

IPC分类号： A61K31/4439 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P7/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P27/04 ,  A61P27/06

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/10 ,  C07D405/14

摘要： A compound represented by formula (1) or salt thereof and a production intermediate thereof are created. The compound exhibited an excellent antioxidation action in a microsome lipid peroxidation measuring system using a rat liver microsome. Therefore, the compound or salt thereof is useful as an antioxidant. The present invention also provides use of a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof for production of an antioxidant.

摘要翻译： 由式（1）或其盐和一种生产中间表示的化合物或其被创建。 化合物显示在微粒体脂质过氧化的测量系统使用大鼠肝微粒优良的抗氧化作用。 因此，该化合物或其盐是作为抗氧化剂是有用的。 本发明因此提供了式（1）或用于生产抗氧化剂的药学上可接受的盐表示的化合物。