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    • 47. 发明申请
    • TETRA-AZA MACROCYCLES AND METAL COMPLEXES THEREOF
    • TETRA-AZA MACROCYCLES及其金属复合物
    • WO1989001476A1
    • 1989-02-23
    • PCT/GB1988000671
    • 1988-08-12
    • CELLTECH LIMITEDPARKER, DavidMILLICAN, Thomas, Andrew
    • CELLTECH LIMITED
    • C07D257/02
    • C07D401/12A61K47/6887A61K49/0002C07D257/02
    • Tetra-aza macrocycles of formula (1), wherein m and n, which may be the same or different, is each zero or an integer 1, 2, or 3; d is zero or an integer 1 or 2; q is zero or an integer from 1 to 6 inclusive; R , R and R , which may be the same or different, is each a hydrogen atom or an alkyl, alkoxyalkyl, -CO2H, -SO3H, PO3H2 or aryl group; L is a covalent bond or linker group; Z is a hydrogen atom or a reactive functional group, with the proviso that when L is a covalent bond Z is a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and are particularly suitable for coupling to other molecules, such as proteins for use in diagnosis and therapy.
    • 式(1)的四氮杂大环,其中m和n可以相同或不同,分别为零或整数1,2或3; d为零或整数1或2; q为0或1〜6的整数; R 1,R 2和R 3可以相同或不同,分别为氢原子或烷基,烷氧基烷基,-CO 2 H,-SO 3 H,PO 3 H 2或芳基; L是共价键或连接基团; Z是氢原子或反应性官能团,条件是当L是共价键时,Z是反应性官能团; 和金属络合物和/或其盐; 与其制备方法和含有它们的组合物一起描述。 所述化合物可用于成像和治疗异常细胞病症,例如治疗肿瘤,并且特别适用于与其它分子(例如用于诊断和治疗的蛋白质)的偶联。