申请人:Adamo Roberto
公开号:US20140141034A1
公开(公告)日:2014-05-22
A process is provided for preparing a conjugate of Formula (I-A) or (I) comprising a polypeptide containing n number of tyrosine units, where n is an integer greater than or equal to 1, dispersed within the amino acid chain
having and amino terminus end (A
1
) and an acid terminus end (A
2
) of the protein or polypeptide and having a weight average molecular weight equal to or greater than 10,000 Daltons (10 kDa), wherein the conjugate comprises a number m of tyrosine conjugates (modified tyrosine residues) as depicted in Formula (I-A) or (I), where m is at least one and is less than or equal to n:
where X, Lg, L and R are as defined herein.
提供了一种制备公式(I-A)或(I)的共轭物的方法,其中包含n个酪氨酸单元的多肽,其中n是大于或等于1的整数,分散在具有氨基端末(A1)和酸端末(A2)的氨基酸链中,并且具有平均分子量大于或等于10,000道尔顿(10 kDa)的蛋白质或多肽,其中共轭物包括如公式(I-A)或(I)所示的m个酪氨酸共轭物(修饰的酪氨酸残基),其中m至少为1且小于或等于n:其中X,Lg,L和R如此处所定义。