会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明申请
    • CYCLIN GROOVE INHIBITORS
    • CYCLIN GROVE抑制剂
    • WO2005042565A3
    • 2005-08-11
    • PCT/GB2004004454
    • 2004-10-21
    • CYCLACEL LTDANDREWS MARTIN J IMCINNES CAMPBELLKONTOPIDIS GEORGEFISCHER PETER M
    • ANDREWS MARTIN J IMCINNES CAMPBELLKONTOPIDIS GEORGEFISCHER PETER M
    • A61K38/00C07K14/47G01N33/50G01N33/68C07K5/00C07K5/02C07K7/00C07K7/02G01N33/574G06F19/00
    • C07K14/4738A61K38/00G01N33/5011G01N33/6872G01N2333/4739G01N2333/91205G01N2500/02
    • The present invention relates to a compound of formula (I), or a variant thereof, A - (B)m - C - (D)n- E, wherein m and n are each independently 0 or 1 and A, B, C, D and E are each independently linked to the respective adjacent residue by a linker group independently selected from carboxamide, reduced carboxamide, sulfonamide, imine, semicarbazone, oxime and ethanolamine; A is (i) a natural or unnatural amino acid residue having a side chain comprising at least one H-bond acceptor moiety and at least one H-bond donor moiety, or a derivative thereof; or (ii) R(CO), wherein R is a C1-C24 hydrocarbyl group comprising at least one H-bond acceptor moiety and optionally one or more H-bond donor moieties, and where R optionally contains one or more heteroatoms selected from S, O, and N, and is optionally substituted by one or more substituents selected from halogen, OMe, CN, CF3, and NO2; each of B and D is independently an amino acid residue selected from arginine, 4-(guanidinyl)phenylalanine (4-(Gu)Phe), piperidinylglycine (PipGly), piperidinylalanine (PipAla), pyridinylalanine, histamine, N,N-(dimethyl) lysine (DMLys), citrulline, glutamine, serine, lysine, asparagine, isoleucine and alanine, or a derivative thereof; C is NH-X-CO, where X is a C1-C4 alkylene group substituted by a straight-chain or branched C1-C6 alkylene group, said C1-C6 alkylene group optionally containing a H-bond donor or H-bond acceptor moiety; E is (i) a natural or unnatural amino acid residue having an aryl or heteroaryl side chain, or a derivative thereof; or (ii) NHR', where R' is a C1-C24 hydrocarbyl group, optionally containing one or more heteroatoms selected from N, O, and S, and optionally comprising one or more H-bond acceptor or donor moieties; said hydrocarbyl group further comprising a pendent C4-C12 aryl or heteroaryl group, which itself may be optionally substituted by one or more substituents selected from a H-bond donor moiety, a H-bond acceptor moiety, a halogen, Me, Et, Pr, CF3, CN and NO2; wherein at least one of A and E is other than a natural or unnatural amino acid residue when A, B, C, D and E are each linked to the respective adjacent residue by a carboxamide group.
    • 本发明涉及式(I)化合物或其变体,A - (B)m -C-(D)n-E,其中m和n各自独立地为0或1,A,B,C D和E各自独立地通过独立地选自羧酰胺,还原羧酰胺,磺酰胺,亚胺,缩氨基脲,肟和乙醇胺的连接基团相应地相邻的相邻残基连接。 A是(i)具有侧链的天然或非天然氨基酸残基,所述侧链包含至少一个H键受体部分和至少一个H键供体部分或其衍生物; 或(ii)R(CO),其中R是包含至少一个H键受体部分和任选的一个或多个H键供体部分的C 1 -C 24烃基,并且其中R任选地含有一个或多个选自S ,O和N,并且任选地被一个或多个选自卤素,OMe,CN,CF 3和NO 2的取代基取代; B和D中的每一个独立地为选自精氨酸,4-(胍基)苯丙氨酸(4-(Gu)Phe),哌啶基甘氨酸(PipGly),哌啶基丙氨酸(PipAla),吡啶丙氨酸,组胺,N,N- )赖氨酸(DMLys),瓜氨酸,谷氨酰胺,丝氨酸,赖氨酸,天冬酰胺,异亮氨酸和丙氨酸或其衍生物; C是NH-X-CO,其中X是被直链或支链C1-C6亚烷基取代的C1-C4亚烷基,所述C1-C6亚烷基任选地含有H-键供体或H-键受体部分 ; E是(i)具有芳基或杂芳基侧链的天然或非天然氨基酸残基或其衍生物; 或(ii)NHR',其中R'是C 1 -C 24烃基,任选地含有一个或多个选自N,O和S的杂原子,并任选地包含一个或多个H键受体或供体部分; 所述烃基还包含悬挂的C 4 -C 12芳基或杂芳基,其本身可以任选地被一个或多个选自H键供体部分,H-键受体部分,卤素,Me,Et,Pr ,CF3,CN和NO2; 其中当A,B,C,D和E各自通过羧酰胺基团连接到相应的相邻残基时,A和E中的至少一个不是天然或非天然氨基酸残基。