发明名称 ACTINIUM-225 COMPLEXES AND CONJUGATES FOR RADIOIMMUNOTHERAPY
摘要 Actinium-225 (225Ac) complexes with functionalized chelants of the formula ( I) wherein: each Q is independently hydrogen or (CHR5)pCO2R; Q1 is hydrogen or (CHR5)wCO2R; each R independently is hydrogen, benzyl or C1-C4 alkyl; with t he proviso that at least two of the sum of Q and Q1 must be other than hydrogen ; each R5 independently is hydrogen; C1-C4 alkyl or (C1-C2 alkyl)phenyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon-carbon bond; n is 0 or 1; m is an integer from 0 t o 10 inclusive; p is 1 or 2; r is 0 or 1; w is 0 or 1; with the proviso that n is only 1 when X and/or Y form an additional carbon to carbon bond, and the sum of r and w is 0 or 1; L is a linker/spacer group covalently bonded to, a nd replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula (1) wherein s is a n integer of 0 or 1; t is an integer of 0 to 20 inclusive; R1 is an electrophilic or nucleophilic moiety which allows for covalent attachment to an antibody or fragment thereof, or synthetic linker which can be attached t o an antibody or fragment thereof, or precursor thereof; and Cyc represents a cyclic aliphatic moiety, aromatic moiety, aliphatic heterocyclic moiety, or aromatic heterocyclic moiety, each of said moieties optionally substituted with one or more groups which do not interfere with binding to an antibody o r antibody fragment; with the proviso that when s, t, m, r, and n are 0, then R1 is other than carboxyl; their pharmaceutically acceptable salts, their conjugates and the use thereof for radioimmunotherapy is disclosed.
申请公布号 CA2381123(A1) 申请公布日期 2001.09.13
申请号 CA20012381123 申请日期 2001.02.23
申请人 MA, DANGSHE 发明人 MA, DANGSHE;FRANK, R. KEITH;SCHEINBERG, DAVID A.;SIMON, JAIME;KIEFER, GARRY E.;MCDEVITT, MICHAEL R.;GULYAS, GYONGYI
分类号 A61K51/04;A61K51/10;(IPC1-7):A61K51/04 主分类号 A61K51/04
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