首页> 外国专利> LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PSMA-EXPRESSING CANCERS

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PSMA-EXPRESSING CANCERS

机译：前列腺特异性膜抗原（PSMA）的标签抑制剂，它们作为成像剂和药物制剂用于治疗PSMA表达癌的抑制剂

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摘要

The present invention relates to a compound of formula (1) (I), wherein Y³ is O or S, wherein s, t, u and w are 0 or 1, wherein i is an integer of from 1 to 3, wherein j is an integer of from 3 to 5, and wherein Z¹, Z²and Z³ are selected from the group consisting of CO ₂ H, -SO ₂ H, -SO 3 H, -OSO 3 H, and -0P0₃H₂, R ¹ is -CH ₃ or H, X is selected from the group consisting of alkylaryl, aryl, alkylheteroaryl and heteroaryl, Y ¹ and Y ² are selected from the group consisting of aryl, alkylaryl, cycloalkyl, heterocycloalkyl, heteroaryl and alkylheteroaryl, and wherein A is a chelator residue having a structure selected from the group consisting of (la), (lb) and (lc), wherein R ², R ³, R ⁴ and R ⁵ are selected from the group consisting of H, - CH ₂ -COOH and -CH ₂ -C(=0)-NH ₂ or wherein R ² and R ⁴ form a -(CH ₂ ) _n- bridge with n being an integer of from 1 to 3, wherein n is preferably 2, and wherein r, v and q are 0 or 1, with the proviso that in case u and w are 0, q and v are 0, and (A) wherein u and w are 1, or (B) wherein u is 0 and w is 1, and wherein A is selected from (la) or (lb), or (C) wherein A is not The compound is disclosed for use in the treatment of PSMA- expressing cancer.

机译：本发明涉及式（1）（I）的化合物，其中Y ^{3 为O或S，其中s，t，u和w为0或1，其中i为整数从1到3，其中j是3到5的整数，并且其中Z ^{1 ，Z ^{2 和Z ^{3 选自由CO _{2 H，-SO _{2 H，-SO 3 H，-OSO 3 H和-0P0 _{3 H <组成的组Sub> 2 ，R ^{1 为-CH _{3 或H，X选自烷基芳基，芳基，烷基杂芳基和杂芳基，Y ^{1 和Y ^{2 选自芳基，烷基芳基，环烷基，杂环烷基，杂芳基和烷基杂芳基，其中A是具有选自以下的结构的螯合剂残基：（1a），（1b）和（1c）中的其中R ^{2 ，R ^{3 ，R ^{4 和R ^{5 < / Sup>选自H，-CH _{2 -COOH和-CH _{2 -C（= 0）-NH _{2 或rein R ^{2 和R ^{4 形成-（CH _{2 ）_{n -桥，其中n为整数从1到3，其中n优选为2，并且其中r，v和q为0或1，前提是在u和w为0的情况下，q和v为0，以及（A）其中u和w为1或（B），其中u为0，w为1，并且其中A选自（la）或（lb），或（C）其中A不为所述化合物。公开了该化合物用于治疗PSMA表达癌症。}}}}}}}}}}}}}}}}}}}}}}

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公开/公告号WO2020065045A1

专利类型
公开/公告日2020-04-02

原文格式PDF
申请/专利权人 UNIVERSITÄT HEIDELBERG;DEUTSCHES KREBSFORSCHUNGSZENTRUM;
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申请/专利号WO2019EP76267
发明设计人 HABERKORN UWE;DOS SANTOS JOSÉ CARLOS;MIER WALTER;KRATOCHWIL CLEMENS;BAUDER-WUEST ULRIKE;KOPKA KLAUS;SCHÄFER MARTIN;
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申请日2019-09-27
分类号A61K51/04;
国家 WO
入库时间 2022-08-21 11:12:20

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