发明名称 |
STABILITY-MODULATING LINKER USED WITH ANTIBODY DRUG CONJUGATE |
摘要 |
PROBLEM TO BE SOLVED: To provide an antibody drug conjugate (ADC) in which stable characteristics are modified by the portion for modulation on a linker of ADC.SOLUTION: The invention provides an ADC using a linker represented by formula (I). [M is a stability modulation group; P is a peptide sequence comprising one or more glutamine residues; Q is a glutamine residue in P; E is each independently -C(R1)2-, -O-C(R1)2-C(R1)2- (if r is 2 or more) or -C(R1)2-C(R1)2-O- (if s is 1 or more); R1 is H, an alkyl of straight/branched chain of C1-6, an alkenyl of straight/branched chain of C2-6, or an alkynyl of straight/branched chain of C2-C6; X and Y are amino acids; Z is a spacer element; m is 0-5; n is 1-5; p is 0-2; q is 0-10; r is 0-2; s is 0-2; q+r+s≥2; and D is a cytotoxic agent.]SELECTED DRAWING: None |
申请公布号 |
JP2016050204(A) |
申请公布日期 |
2016.04.11 |
申请号 |
JP20150166643 |
申请日期 |
2015.08.26 |
申请人 |
PFIZER INC;RINAT NEUROSCIENCE CORP |
发明人 |
RUSSELL GEORGE DUSHIN;PAVEL STROP;MAGDALENA GRAZYNA DORYWALSKA;LUDIVINE MOINE |
分类号 |
C07K7/00;A61K31/09;A61K31/395;A61K31/4745;A61K31/537;A61K31/704;A61K39/395;A61K45/00;A61K47/48;A61P35/00;A61P37/06 |
主分类号 |
C07K7/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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