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LSD1-SELECTIVE INHIBITOR HAVING LYSINE STRUCTURE UPDATE

外国特許コード F180009657
整理番号 3965
掲載日 2018年11月21日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2013JP082011
国際公開番号 WO 2014084298
国際出願日 平成25年11月28日(2013.11.28)
国際公開日 平成26年6月5日(2014.6.5)
優先権データ
  • 特願2012-260222 (2012.11.28) JP
発明の名称 (英語) LSD1-SELECTIVE INHIBITOR HAVING LYSINE STRUCTURE UPDATE
発明の概要(英語) The present invention mainly addresses the problem of providing a novel compound having a LSD1-selective inhibitory activity and also having an anti―tumor/anti-cancer activity, an anti-virus activity and the like. As a means for solving the problem, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided. [In the formula, R1 to R5, A, and *1 to *3 are as defined in the description.]
従来技術、競合技術の概要(英語) BACKGROUND ART
Specific amino acid residues of the quality of a methylated core histone proteins, made by modifications such as acetylation, changes the chromatin structure of chromosomes, which has an important function in gene regulation has been recently revealed. Is Lysine-specific histone demethylase 1(LSD1), quality of core histone proteins 4 histone H3 monomethylated lysine residue by way of the second (H3K4me1) and (H3K4me2) demethylation of the dimethylated body which catalyzes the reaction, a histone demethylating enzyme (non-patent document 1).
LSD1 Can be suppressed by the RNAi function, cell proliferation is inhibited in cancer cells has been reported. Further, the trans-2 - phenylcyclopropyl amine LSD1 described later can be used as inhibitors, may be effective in the treatment of leukemia has been reported.
LSD1 A compound capable to inhibit the function of as, nialamide (tranylcypromine) and trans-2 - phenylcyclopropyl amine known (non-patent document 1, 2). However, these compounds are, low inhibitory activity against LSD1, and LSD1 are highly homologous to further monoamine oxidase (MAO) for also inhibit compound, not with respect to the selective inhibitors of LSD1. MAO (in humans, MAO-A and MAO-B) is, in the adjustment of the important neurotransmitter, or nialamide tranisylpromine clinical application as an inhibitor to LSD1 there is a possibility of an adverse effect is difficult to increase.
Non-patent document 3 and Patent Document 1 is, in the function of the LSD1 can inhibit the disclosed phenylcyclopropyl amine derivatives. However, the compound is is provided with a high selectivity for LSD1, LSD1 inhibitory activity and cell proliferation activity of cancer cells, particularly human insufficient active with respect to the cancer cells.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • KYOTO PREFECTURAL PUBLIC UNIVERSITY CORPORATION
  • PUBLIC UNIVERSITY CORPORATION NAGOYA CITY UNIVERSITY
  • EDUCATIONAL CORPORATION KANSAI BUNRI SOUGOUGAKUEN
  • FRONTIER PHARMA INC.
  • KYOTO UNIVERSITY
  • 発明者(英語)
  • SUZUKI, Takayoshi
  • ITOH, Yukihiro
  • OGASAWARA, Daisuke
  • MIYATA, Naoki
  • MIZUKAMI, Tamio
  • SASAKI, Ryuzo
  • TAKAORI, Akifumi
  • KAWAHARA, Masahiro
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN TD TG
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