Title:
NOVEL NF-κB INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2019/059132
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a novel NF-κB inhibitor which has a more effective and higher bioavailability and is more suitable for clinical application. More specifically, the purpose of the present invention is to find a non-epoxy compound which recognizes a domain including Cys-38 of RelA and neighboring amino acid sequences, and which has an NF-κB inhibitory efficacy and can be used for clinical application. The present invention provides a novel jietacin derivative having an excellent NF-κB inhibitory activity. In other words, the present invention provides an azoxy motif as a class of NF-κB inhibitors having a novel and useful backbone. More specifically, the present invention relates to a compound represented by the following general formula, an NF-κB inhibitor containing said compound as an active ingredient, and the like.
Inventors:
OMURA SATOSHI (JP)
SUNAZUKA TOSHIAKI (JP)
HIROSE TOMOYASU (JP)
SUGAWARA AKIHIRO (JP)
NOGUCHI YOSHIHIKO (JP)
HORIE RYOICHI (JP)
WATANABE MARIKO (JP)
SUNAZUKA TOSHIAKI (JP)
HIROSE TOMOYASU (JP)
SUGAWARA AKIHIRO (JP)
NOGUCHI YOSHIHIKO (JP)
HORIE RYOICHI (JP)
WATANABE MARIKO (JP)
Application Number:
PCT/JP2018/034254
Publication Date:
March 28, 2019
Filing Date:
September 14, 2018
Export Citation:
Assignee:
THE KITASATO INST (JP)
International Classes:
C07C291/08; A61K31/131; A61K31/4192; A61K31/4439; A61P29/00; A61P35/00; A61P37/06; C07D249/04; C07D401/04; C07K14/435
Foreign References:
| JPH01211557A | 1989-08-24 | |||
| CN107501131A | 2017-12-22 |
Other References:
TSUZUKI,K. ET AL., THE JOURNAL OF ANTIBIOTICS, vol. 44, no. 7, 1991, pages 774 - 784
SUGAWARA, A. ET AL.: "Jietacins with potent nematocidal activity; efficient isolation of novel analogs and divergent total synthesis of jietacin A, B, C, and D", TETRAHEDRON, vol. 71, 2015, pages 2149 - 2157, XP029145143
DATABASE Registry [o] 7 April 1989 (1989-04-07), retrieved from STN Database accession no. RN 119947-18-1
DATABASE Registry [o] 7 April 1989 (1989-04-07), retrieved from STN Database accession no. RN 119947-17-0
DATABASE Registry [o] 12 January 1990 (1990-01-12), retrieved from STN Database accession no. RN 124657-83-6
DATABASE Registry [o] 3 March 1985 (1985-03-03), retrieved from STN Database accession no. RN 95048-37-6
SGWARA, AKIMASA ET AL.,: "27PA-am054", LECTURE ABSTRACTS OF 137TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1 February 2017 (2017-02-01)
SUGAWARA,A. ET AL.: "Jietacins, azoxy antibiotics with potent nematocidal activity: Design, synthesis, and biological evaluation against parasitic nematodes", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 145, 28 December 2017 (2017-12-28), pages 524 - 538, XP055584914
SUGAWARA, A. ET AL.: "Jietacins with potent nematocidal activity; efficient isolation of novel analogs and divergent total synthesis of jietacin A, B, C, and D", TETRAHEDRON, vol. 71, 2015, pages 2149 - 2157, XP029145143
DATABASE Registry [o] 7 April 1989 (1989-04-07), retrieved from STN Database accession no. RN 119947-18-1
DATABASE Registry [o] 7 April 1989 (1989-04-07), retrieved from STN Database accession no. RN 119947-17-0
DATABASE Registry [o] 12 January 1990 (1990-01-12), retrieved from STN Database accession no. RN 124657-83-6
DATABASE Registry [o] 3 March 1985 (1985-03-03), retrieved from STN Database accession no. RN 95048-37-6
SGWARA, AKIMASA ET AL.,: "27PA-am054", LECTURE ABSTRACTS OF 137TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1 February 2017 (2017-02-01)
SUGAWARA,A. ET AL.: "Jietacins, azoxy antibiotics with potent nematocidal activity: Design, synthesis, and biological evaluation against parasitic nematodes", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 145, 28 December 2017 (2017-12-28), pages 524 - 538, XP055584914
Attorney, Agent or Firm:
NAKATANI Tomoko (JP)
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