Doronina, Svetlana O.,Senter, Peter D.,Toki, Brian E.,Ebens, Allen J.,Kline, Toni Beth,Polakis, Paul,Sliwkowski, Mark X.,Spencer, Susan D.
申请号：
ES10175437
公开号：
ES2579836T3
申请日:
2004.11.05
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound of antibody-drug comprising an antibody covalently attached to one or more drug moieties, the compound having the Formula Ic: Formula ** ** or a pharmaceutically acceptable salt thereof, wherein: Ab is an antibody that binds to one or more tumor-associated antigens (1) - (8): (1) CD79b (CD79B, CD79 ß, IGB (beta associated with immunoglobulin), B29) (2) MUC16 (3) ETBR (Endothelin receptor type B) (4) Napi3b (NAPI-3B, NPTIIb, Slc34a2, family 34 solute vehicle (sodium phosphate), conveyor 3b sodium phosphate dependent type II, member 2) (5) IRTA2 (associated Translocation 2 receptor immunoglobulin superfamily a course immunoreceptor with possible roles in the development and lymphomagenesis B lymphocyte deregulation of genes by translocation occurs in some B cell malignancies) (6) PSCA hlg (2700050C12Rik genes, C530008O16Rik, RIKEN cDNA 2700050C12, RIKEN cDNA 270005OC12) (7) STEAP1 (six transmembrane epithelial antigen of prostate domains) (8) MPF (MPF, MSLN, SMR, megakaryocyte potentiating factor, mesothelin) A frame is a unit, a is 0 or 1, each -W- is independently an Amino Acid unit, w is an integer ranging from 0 to 12, Y is a spacer unit, and y is 0, 1 or 2. where p varies from 1 to 20, and D is a drug moiety selected from formulas DE and DF: ** ** Formula in which the wavy line of DE and DF indicates the covalent attachment site to a, w or Y, and independently at each location: R2 is selected from the group consisting of H and C1-C8 alkyl R3 is selected from the group consisting of H, C1-C8 alkyl, C3-C8 carbocycle, aryl, alkaryl C1-C8, C1-C8 alkyl- (C3-C8 carbocycle), C3-C8 heterocycle and alkyl C1- C8 (C3-C8 heterocycle) R4 is selected from the group consisting of H, C1-C8 alkyl, C3-C8 carbocycle, aryl, alkaryl C1-C8, C1-C8 alkyl- (C3-C8 carbocycle), C3-C8 heterocycle and C1 -C8- (C3-C8 heterocycle) R5 is selected from the group consisting of H and methyl Or R4 and R5 together form a carbocyclic ring and have the formula - (CRaRb) n- wherein Ra and Rb
