TOP > 外国特許検索 > TGF-Β SIGNAL TRANSDUCTION INHIBITOR

TGF-Β SIGNAL TRANSDUCTION INHIBITOR

外国特許コード F120006681
整理番号 2789
掲載日 2012年5月24日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2011JP053428
国際公開番号 WO 2011102436
国際出願日 平成23年2月17日(2011.2.17)
国際公開日 平成23年8月25日(2011.8.25)
優先権データ
  • 特願2010-032810 (2010.2.17) JP
発明の名称 (英語) TGF-Β SIGNAL TRANSDUCTION INHIBITOR
発明の概要(英語) A compound represented by formula (I) or a pharmacologically acceptable salt thereof; and use of the compound or the pharmacologically acceptable salt thereof in the prevention or treatment of TGF-β-related diseases. [In the formula, Y represents a hydrogen atom or the like; R2 represents a group represented by formula (a) or the like; R3 represents -NR8-R9- or the like; R4, R5, R6 and R7 are the same as or different from one another and independently represent a hydrogen atom or the like; and X represents a group represented by formula (b) or the like.]
従来技術、競合技術の概要(英語) BACKGROUND ART
Transforming Growth Factor (TGF) - is β, or promote cell growth or inhibition thereof, cell differentiation, such as occurrence of a cytokine involved in various physiological phenomena in. In addition, is pathological, cancer, cirrhosis, renal failure (glomerulonephritis), such as rheumatoid arthritis and arteriosclerosis, organ fibrosis is deeply be due to the onset of the disease has been known (non-patent document 1).
On the constituent amino acids homology is observed, TGF-β is, bone morphogenic protein, such as TGF-β superfamily and activin to form. TGF-β superfamily members, after both as a precursor, pre-body, followed by sequence-body can be removed by proteolytic enzymes, having a molecular weight of about 12kDa generated as a mature protein. One of such a monomer is 2, can be covalently linked by disulfide bridges, a dimer of a molecular weight of approximately 25kDa (non-patent document 2) is generated.
Human TGF-β 3 is three isoforms (TGF-β1, and TGF-β3 TGF-β2) is present, in a tissue specific (non-patent document 2) expressing. Each TGF-β isoform of the signal, information transmitted via the transmission paths, each exhibit physiological activity. That is, the serine/TGF-β receptor type II TGF-β-oxide enzyme and binds to the receptor, 2 receptor molecule type II, type I TGF-β 2 receptor molecules/Alk-5 receptors composed of a complex is formed after, TGF-β type II receptors I receptor/Alk-5 phosphorylate serine residues and activate. Type I TGF-β receptor II receptor/Alk-5 also in the same manner as an enzyme serine/ oxide, activated receptor/Alk-5 I is, present in the cytoplasm of the Smad3 transcription factor or Smad2 phosphorylation of serine residues. Smad2 Or Smad3 is phosphorylated, and Smad4 form a complex in the cytoplasm, then, proceeds to the nucleus, the involvement of a fibrosis of the target gene and the promoter region of the deep collagen present in the target sequence called CAGAbox, induce transcript expression of a target gene together with a co-activator (non-patent document 1, 3, 4).
TGF-β is a disease state caused by the action of as a measure for improving, the binding of TGF-β receptor, neutralizing antibodies, soluble receptors or inhibited by the compounds or low-molecular, caused by the binding of TGF-β phosphorylation of the receptor enzyme activity such as inhibitors of the low-molecular compound has been attempted is, novel TGF-β signal transduction inhibitors are developed for development (non-patent document 5).
On the other hand, the non-patent document 6, inhibit secreted Frezzled-Related Protein I (sFRP-1), modulate Wnt signaling, is piperidinyl substituted N - - sulfonamides disclosed (non-patent document 6).
  • 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 University
  • 発明者(英語)
  • KAKEYA, Hideaki
  • HATTORI, Akira
  • TAKASU, Yasuaki
  • FUJII, Nobutaka
  • OISHI, Shinya
  • KOJIMA, Soichi
  • HARA, Mitsuko
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH 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 IS JP KE KG KM 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 PE PG PH PL PT RO RS RU 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 SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ MD 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 ML MR NE SN TD TG
ライセンスをご希望の方、特許の内容に興味を持たれた方は、下記までご連絡ください。

PAGE TOP

close
close
close
close
close
close