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NEW MAITANINOIDS AND APPLICATION OF MENTATED MAITANINOIDS TO OBTAIN ANTIBODY CONJUGATES

机译:新的类人鞭毛类动物和经指导的类人鞭毛类动物鞭毛在获得抗体结合物中的应用

摘要

The present invention relates to a compound of formula (I) in which ALK is a (C-C) alkylene group; each X and X independently represent one of the following groups: -CH = CH-, -CO-, -CONR-, - NRCO-, -COO-, -OCO-, -OCONR-, -NRCOO-, -NRCONR'-, - NR-, -S (O) (n = 0, 1 or 2) or -O-; R and R ′ are independently H or a (C -C) alkyl group; i is an integer from 1 to 40, preferably from 1 to 20, and more preferably from 1 to 10; j is an integer equal to 1 when X represents -CH = CH-, and 2 when X is -CH = CH-; Z represents a simple bond, -O- or -NH-, and R 5 represents H or (C-C) alkyl, (C-C) cycloalkyl, aryl, heteroaryl or (C-C) heterocycloalkyl group; or Z represents a simple bond and R represents a halogen. The invention relates to the use of the mentioned maytansinoid to obtain conjugates with antibody having affinity for tumor cells.
机译:本发明涉及式(I)的化合物,其中ALK是(C-C)亚烷基。每个X和X独立代表以下组之一:-CH = CH-,-CO-,-CONR-,-NRCO-,-COO-,-OCO-,-OCONR-,-NRCOO-,-NRCONR'- ,-NR-,-S(O)(n = 0、1或2)或-O-; R和R'独立地为H或(C1-C)烷基。 i为1〜40的整数,优选为1〜20的整数,更优选为1〜10的整数。当X表示-CH = CH-时,j是等于1的整数,当X是-CH = CH-时,j是等于2的整数。 Z代表单键,-O-或-NH-,R 5代表H或(C-C)烷基,(C-C)环烷基,芳基,杂芳基或(C-C)杂环烷基; Z表示单键,R表示卤素。本发明涉及上述美登木素生物碱与具有对肿瘤细胞具有亲和力的抗体的缀合物的用途。

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