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    E2F ACTIVITY INHIBITORY COMPOUNDS
    3.
    发明公开
    E2F ACTIVITY INHIBITORY COMPOUNDS 失效
    E2FAKTIVITÄTHEMMUNGSVERBINDUNGEN

    公开(公告)号：EP0963999A1

    公开(公告)日：1999-12-15

    申请号：EP97941259.0

    申请日：1997-09-26

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： SHIBATA, Kenji ,  YAMASAKI, Motoo ,  YOSHIDA, Tetsuo ,  MIZUKAMI, Tamio

    IPC分类号： C07K14/47 ,  A61K38/17

    CPC分类号： C07K14/4705 ,  A61K38/00

    摘要： Compounds represented by the general formula (I): R 1 -A-R 2 or pharmacologically acceptable salts thereof wherein R 1 represents (un)substituted alkanoyl, (un)substituted aroyl, (un)substituted heteroarylcarbonyl, (un)substituted alkoxycarbonyl, (un)substituted aryloxycarbonyl, (un)substituted heteroaryloxycarbonyl, or hydrogen; R 2 represents hydroxy, (un)substituted alkoxy or (un)substituted amino; and A represents a partial peptide sequence comprising at least 12 consecutive amino acid residues in the sequence of a dimer forming or DNA binding region of each member of E2F family.

    摘要翻译： 由通式（I）表示的化合物：R 1 -AR 2或其药理学上可接受的盐，其中R 1表示（un）取代的烷酰基，（un）取代的芳酰基，（未）取代的杂芳基羰基，（un ）取代的烷氧基羰基，（取代的）取代的芳氧基羰基，（取代的）取代的杂芳氧基羰基或氢; R 2表示羟基，（未）取代的烷氧基或（取代的）取代的氨基; 并且A表示在E2F家族的每个成员的二聚体形成或DNA结合区的序列中包含至少12个连续的氨基酸残基的部分肽序列。

    PEPTIDES HAVING CYCLIC STRUCTURES AND EXERTING P53 PROTEIN ACTIVTY-RESTORING EFFECT ON P53 PROTEIN MUTANTS
    4.
    发明公开
    PEPTIDES HAVING CYCLIC STRUCTURES AND EXERTING P53 PROTEIN ACTIVTY-RESTORING EFFECT ON P53 PROTEIN MUTANTS 失效
    具有环状结构突变型P53蛋白的活性可恢复肽。

    公开(公告)号：EP0989136A1

    公开(公告)日：2000-03-29

    申请号：EP98919612.6

    申请日：1998-05-15

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： SHIBATA, Kenji ,  YAMASAKI, Motoo ,  YOSHIDA, Tetsuo ,  MIZUKAMI, Tamio ,  SHINKAI, Akeo ,  ANAZAWA, Hideharu

    IPC分类号： C07K14/82

    CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K7/52 ,  C07K7/64 ,  C07K14/4746

    摘要： Peptides having cyclic structures represented by the following general formula(I): R 1 (X 1 ) n1 (X 2 ) n2 (X 3 ) n3 (X 4 ) n4 (X 5 ) n5 (X 6 ) n6 (X 7 ) n7 (X 8 ) n8 (X 9 ) n9 (X 10 ) n10 (x 11 )n 11 (X 12 ) n12 (X 13 ) n13 (X 14 ) n14 (X 15 ) n15 (X 16 ) n16 (X 17 ) n17 R2 and exerting the effect of restoring a P53 protein activity on P53 protein mutants or pharmacologically acceptable salts thereof. In said formula (I) X i means an arbitrary member selected from among X 1 to X 17 while n i means an arbitrary member selected from among n 1 to n 17 (provided that i is an integer of from 1 to 17), then X i represents an amino acid residue or an organic acid residue; a functional group in a residue X p selected among X 1 to X 11 (provided that p is an integer of from 1 to 11) and a functional group X q selected from among X 8 to X 17 (provided that q is an integer of from 8 to 17 and larger than p) form a cyclic structure having a crosslinkage selected from among S-S, S-CH 2 -S, S-CH 2 -C 6 H 4 ,-CH 2 -S, S-CH 2 -CO, CO-NH, NH-CO, O-CO or CO-O; R 1 represents optionally substituted alkanoyl, etc.; and R 2 represents optionally substitued alkoxy, etc.

    摘要翻译： [R <1））））：具有由下述通式（I）表示的环状结构的肽 ））））（X <8>））））N <11）））） ））） R2和施加P53蛋白突变体或其药理学上可接受的盐还原P53蛋白活性的效果。 在所述式（I）中X的装置从X <1>到X <17>而Ñ装置从N中<1>选择到n的任意构件（提供<17>中选择的任意构件做 i是从1到17的整数），则X的 darstellt在氨基酸残基或有机残基; 在残基X

    的官能团中选择的X <1>至X <11>（提供确实p是从1到11的整数）和选自X <8>到所选择的官能团X X <17>（提供确实q是8至17中的整数，大于p）形成具有从SS，S-CH2-S，S-CH2-C6H4，CH2-S中选择的交联的环状结构， S-CH2-CO，CO-NH，NH-CO，O-CO或CO-O; [R <1> darstellt OPTIONALLY substituiertem烷酰基等; 且R <2> darstellt任意取代的烷氧基等