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PEPTIDIC COMPOUND AND USE OF SAME

Foreign code F110005444
File No. S2009-0905-C0
Posted date Sep 6, 2011
Country WIPO
International application number 2010JP062514
International publication number WO 2011/013612
Date of international filing Jul 26, 2010
Date of international publication Feb 3, 2011
Priority data
  • P2009-178168 (Jul 30, 2009) JP
Title PEPTIDIC COMPOUND AND USE OF SAME
Abstract Disclosed is a novel compound having an antitumor/anticancer effect. Specifically disclosed is a compound represented by formula (I), a derivative thereof or a salt of the same. In formula (I), R1 represents an alkyl group, an alkenyl group, a cycloalkyl group, an amino group, a monoalkylamino group, a dialkylamino group, an aryl group, a heteroaryl group, an aralkyl group or an alkoxy group; R2 represents an optionally substituted amino group or an optionally substituted nitrogen-containing heterocyclic group; and R3 represents hydrogen, halogen, alkyl, methoxy, cyano, trifluoromethyl, acetylamino or amino. In formula (I), N-Me-Ala may be substituted by N-Me-Gly, N-Me-Ser, N-Me-Thr, Ala, Gly, Ser or Thr; N-Me-Phe may be substituted by Phe, Tyr or N-Me-Tyr; and D-Leu may be substituted by L-Leu.
Scope of claims (In Japanese)
【請求項1】下記式(I)
【化学式1】(式中、R1はアルキル基、アルケニル基、シクロアルキル基、アミノ基、モノアルキルアミノ基、ジアルキルアミノ基、アリール基、ヘテロアリール基、アラルキル基またはアルコキシ基を示す。
 R2は、置換基を有していてもよいアミノ基または置換基を有していてもよい含窒素複素環基を示す。
 R3は水素、ハロゲン、アルキル、メトキシ、シアノ、トリフルオロメチル、アセチルアミノまたはアミノを示す。
 但し、式(I)のAlaは、N-Me-Gly、N-Me-Ser、N-Me-Thr、N-Me-Ala、Gly、SerもしくはThrで置換されていてもよい。
 N-Me-Pheは、Phe,Tyr、N-Me-Tyrで置換されていてもよい。
 D-LeuはL-Leuで置換されていてもよい。)
で表される化合物又はその誘導体もしくはその塩。

【請求項2】 R2は、NR4R5(R4,R5は、同一又は異なって水素原子、アルキル基またはシクロアルキル基を示す。)、
【化学式2】(式中、R6は、R7-CO-もしくはそのヒドラジド、R7-CH(OR8)-(R7はアルキル、アリールもしくはアラルキル基を示す。R8は水素、アルキル基、アリール基、アラルキル基またはアシル基を示す。)を示す。)
で表される、請求項1に記載の化合物又はその誘導体もしくはその塩。

【請求項3】下記式1
【化学式3】で表される請求項1に記載の化合物又はその誘導体もしくはその塩。

【請求項4】請求項1~3のいずれかに記載の化合物又はその誘導体もしくはその塩を有効成分とする抗癌剤。

【請求項5】請求項1~3のいずれかに記載の化合物又はその誘導体を有効成分とするERK選択的なリン酸化阻害剤。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • KEIO UNIVERSITY
  • Inventor
  • SUENAGA, Kiyotake
  • TERUYA, Toshiaki
  • SASAKI, Hiroaki
IPC(International Patent Classification)
Specified countries AE(UTILITY MODEL),AG,AL(UTILITY MODEL),AM(PROVISIONAL PATENT)(UTILITY MODEL),AO(UTILITY MODEL),AT(UTILITY MODEL),AU,AZ(UTILITY MODEL),BA,BB,BG(UTILITY MODEL),BH(UTILITY MODEL),BR(UTILITY MODEL),BW,BY(UTILITY MODEL),BZ(UTILITY MODEL),CA,CH,CL(UTILITY MODEL),CN(UTILITY MODEL),CO(UTILITY MODEL),CR(UTILITY MODEL),CU(INVENTOR'S CERTIFICATE),CZ(UTILITY MODEL),DE(UTILITY MODEL),DK(UTILITY MODEL),DM,DO(UTILITY MODEL),DZ,EC(UTILITY MODEL),EE(UTILITY MODEL),EG(UTILITY MODEL),ES(UTILITY MODEL),FI(UTILITY MODEL),GB,GD,GE(UTILITY MODEL),GH(UTILITY CERTIFICATE),GM,GT(UTILITY MODEL),HN(UTILITY MODEL),HR(CONSENSUAL PATENT),HU(UTILITY MODEL),ID,IL,IN,IS,JP(UTILITY MODEL),KE(UTILITY MODEL),KG(UTILITY MODEL),KM,KN,KP(INVENTOR'S CERTIFICATE)(UTILITY MODEL),KR(UTILITY MODEL),KZ(PROVISIONAL PATENT)(UTILITY MODEL),LA,LC,LK,LR,LS(UTILITY MODEL),LT,LU,LY,MA,MD(UTILITY MODEL),ME,MG,MK,MN,MW,MX(UTILITY MODEL),MY(UTILITY-INNOVATION),MZ(UTILITY MODEL),NA,NG,NI(UTILITY MODEL),NO,NZ,OM(UTILITY MODEL),PE(UTILITY MODEL),PG,PH(UTILITY MODEL),PL(UTILITY MODEL),PT(UTILITY MODEL),RO,RS(PETTY PATENT),RU(UTILITY MODEL),SC,SD,SE,SG,SK(UTILITY MODEL),SL(UTILITY MODEL),SM,ST,SV(UTILITY MODEL),SY,TH(PETTY PATENT),TJ(UTILITY MODEL),TM(PROVISIONAL PATENT),TN,TR(UTILITY MODEL),TT(UTILITY CERTIFICATE),TZ,UA(UTILITY MODEL),UG(UTILITY CERTIFICATE),US,UZ(UTILITY MODEL),VC(UTILITY CERTIFICATE),VN(PATENT FOR UTILITY SOLUTION),ZA,ZM,ZW,EP(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,SE,SI,SK,SM,TR),OA(BF(UTILITY MODEL),BJ(UTILITY MODEL),CF(UTILITY MODEL),CG(UTILITY MODEL),CI(UTILITY MODEL),CM(UTILITY MODEL),GA(UTILITY MODEL),GN(UTILITY MODEL),GQ(UTILITY MODEL),GW(UTILITY MODEL),ML(UTILITY MODEL),MR(UTILITY MODEL),NE(UTILITY MODEL),SN(UTILITY MODEL),TD(UTILITY MODEL),TG(UTILITY MODEL)),AP(BW(UTILITY MODEL),GH(UTILITY MODEL),GM(UTILITY MODEL),KE(UTILITY MODEL),LR(UTILITY MODEL),LS(UTILITY MODEL),MW(UTILITY MODEL),MZ(UTILITY MODEL),NA(UTILITY MODEL),SD(UTILITY MODEL),SL(UTILITY MODEL),SZ(UTILITY MODEL),TZ(UTILITY MODEL),UG(UTILITY MODEL),ZM(UTILITY MODEL),ZW(UTILITY MODEL)),EA(AM,AZ,BY,KG,KZ,MD,RU,TJ,TM)
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