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BENZISOXAZOLE COMPOUND

外国特許コード F200010053
整理番号 6121
掲載日 2020年5月15日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2019JP018082
国際公開番号 WO 2019208812
国際出願日 平成31年4月26日(2019.4.26)
国際公開日 令和元年10月31日(2019.10.31)
優先権データ
  • 特願2018-086929 (2018.4.27) JP
発明の名称 (英語) BENZISOXAZOLE COMPOUND
発明の概要(英語) A compound represented by general formula (1), a salt thereof, or a prodrug thereof is provided as a compound effective in the prevention and/or treatment of fibrosis. (In the formula, A is an optionally substituted benzene ring; B is an optionally substituted aryl or an optionally substituted heteroaryl; X is an oxygen atom or a sulfur atom; Y is a nitrogen atom or a carbon atom; and R1 each independently are lower alkyls, or two R1 may bond to each other to form a spiro ring or a cross-linked structure, or two R1 may bond to each other to form a saturated fused heterocycle together with the carbon atom and nitrogen atom that constitute the Y-containing ring, where p is 0, 1, or 2, or, alternatively, (R1)p is oxo.)
従来技術、競合技術の概要(英語) BACKGROUND ART
Organ or tissue fibrosis is, such as an organ for some reason, an invasion or damaged at the time of repair or as defense mechanisms, the extracellular matrix in an organ caused by the excessively accumulated. And the extracellular matrix, to a material surrounding the cells of the tissue, as major ones, collagen, elastin fibrous proteins, proteoglycans and the like of the glycoconjugates, and fibronectin, laminin such as a glycoprotein and the like. Due to damage of organs such as the degree of invasion or if a minor failure, repair scars do not remain, such as an organ is recovered to normal. However, due to damage of organs such as the degree of invasion or large or persist failure, repair scar fibrosis is an obstacle to the original function of the organ or the like. Furthermore, it causes a vicious circle occurs new fibrosis are formed. Ultimately cause failure of the organ or the like, in the worst case, leading to death.
TRP(Transient receptor potential) gene, year 1989 of the photoreceptor response mutants Drosophila was identified as the causative gene. Subsequent studies, the protein encoded by the TRP homology with protein found in many cases a mammal, the cation in the cell membrane essentially functions as a channel. TRP is an immense diversity channel functional forms such as a super family of, TRPA,TRPV,TRPM,TRPC classified into a group. TRPC (TRP classic or TRP canonical) group is further classified into sub-groups TRPC1-C7.
TRPC3 deficient mice induced cardiac fibrosis load pressure resistance to be shown, and in the mouse administered Pyr3 TRPC3 channel inhibitors of cardiac fibrosis induced pressure load can be suppressed to a known strong (non-patent document 1, 2). Also, bleomycin induced lung fibrosis TRPC6 deficient mice on one side and by renal interstitial fibrosis obstruction resistance to (non-patent document 3, 4) shown, and the channel of the inhibitor Pyr2 TRPC3 TRPC6 (BTP2) by the administration of, on one side of the obstruction by the renal interstitial fibrosis mouse be suppressed.
Therefore, the channel or adjusting the channel activity TRPC6 TRPC3 (hereinafter, TRPC3 adjustment, sometimes referred to as adjusted TRPC6) or inhibit (hereinafter, TRPC3 inhibition, sometimes referred to as inhibition TRPC6) is, lung, heart, kidney or liver organ, tissue fibrosis is useful as a (non-patent document 1-5), in addition, muscle atrophy Amyotrophic Lateral Sclerosis (ALS) and, muscular dystrophy, ulcerative colitis, Crohn's disease, nonalcoholic steatohepatitis (NASH) non-, neurodegenerative diseases such as Williams syndrome, muscle degenerative diseases, inflammatory diseases and the like are also considered to be valid (non-patent document 6-12).
And/or inhibitory effect TRPC3 TRPC6, Pyr2(BTP2), Pyr3,Pyr4,GSK2332255B,GSK2833503A,SAR7334 and the like as the compound have been reported (Non-Patent Document 13-18).
  • 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
  • OSAKA UNIVERSITY
  • KYOTO UNIVERSITY
  • NATIONAL INSTITUTES OF NATURAL SCIENCES
  • 発明者(英語)
  • NAGATA, Ryu
  • MORI, Yasuo
  • MORI, Masayuki
  • NISHIDA, Motohiro
  • TOMITA, Takuro
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 DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS 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 ST TD TG
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