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    • 6. 发明申请
    • CYCLOPEPTIDE DERIVATIVES
    • CYCLO肽衍生物
    • WO1997014716A1
    • 1997-04-24
    • PCT/EP1996004462
    • 1996-10-14
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGJONCZYK, AlfredGOODMAN, Simon, LawrenceDIEFENBACH, BeateSUTTER, ArneKESSLER, Horst
    • MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
    • C07K14/75
    • C07K7/64A61K38/00C07K14/75Y02P20/55
    • The invention relates to compounds of the formula (I) R -Q -X-Q -R , in which: Q , Q , each independent of one another, are missing or are -NH-(CH2)n-CO-; R , R , each independent of one another, are missing or are cyclo-(Arg-Gly-Asp-Z), wherein Z is missing in the side chain of Q or Q or if Q and/or Q are missing, is bound to X, at least one of the groups R or R always having to be included; X is -CO-R -CO-, and if R -Q - or R -Q - are missing is R , R , R , Het-CO or a fluorescent pigment residue linked through a -CONH-, -COO-, -NH-C(=S)-NH-, -NH-C(=O)-NH-, -SO2NH- or -NHCO- bond; and Z, R , R , R , R , Het and n have the meanings given in claim 1. The invention also relates to the salts of said compounds. Said compounds and their salts can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, angiogenic diseases and in tumour therapy.
    • 式(I)R <1> -Q <1> -XQ <2> -R <2>其中Q <1>,Q <2>各自独立地不存在或-NH-(CH 2)N-CO-的化合物 ,R <1>,R <2>不存在各自独立地为或环 - (Arg - 甘氨酸 - 天冬氨酸-Z),其中Z在侧链至Q <1>或Q <2>,或者,如果Q <1>,和 /或Q <2>不存在,键合至X,并且其中R中的至少一个<1>或R <2>必须始终包含的,X是-CO-R <18> - CO-和如果R <1 > -Q <1> - 或R <2> -Q <2> - 缺失 - [R <10>,R <13>,R <16>中,Het-CO,或经由-CONH-,-COO - , - NH-C(= S)-NH-,-NH-C(= O)-NH - , - SO 2 NH-或-NHCO-键连接的荧光染料基团,和Z,R <10>,R <13>, [R <16>,R <18>中,Het和n具有权利要求1中给出的含义和它们的盐可以用作整联蛋白抑制剂,特别是用于循环,血栓形成障碍,心肌梗死,冠状动脉心脏疾病,动脉硬化症的预防和治疗, 血管生成病症和在肿瘤治疗中使用。