公开(公告)号：US11712480B2

公开(公告)日：2023-08-01

申请号：US16321695

申请日：2017-07-31

申请人： PFIZER INC.

发明人： Russell George Dushin ,  Daniel P. Uccello ,  Jeremy Starr ,  Ye Che ,  Mark Flanagan ,  Jeffrey M. Casavant ,  Christopher John O'Donnell ,  Gary Frederick Filzen ,  Jennifer Young ,  Joseph A. Abramite ,  Lawrence N. Tumey ,  Ludivine Moine ,  Adam Matthew Gilbert ,  Lee R. Roberts

IPC分类号： A61K47/54 ,  A61K47/68 ,  C07K4/00 ,  C07K5/02 ,  C07K7/02 ,  A61K47/50 ,  C07K5/062

CPC分类号： A61K47/6855 ,  A61K47/50 ,  A61K47/545 ,  A61K47/6867 ,  C07K4/00 ,  C07K5/0205 ,  C07K5/06052 ,  C07K7/02

摘要： The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula:




(wherein R1, R2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

公开(公告)号：US11993625B2

公开(公告)日：2024-05-28

申请号：US16477290

申请日：2018-01-10

申请人： PFIZER INC.

发明人： Omar Khaled Ahmad ,  Stephen Paul Brown ,  Kenneth John Dirico ,  Russell Dushin ,  Gary Frederick Filzen ,  Sujiet Puthenveetil ,  Pavel Strop ,  Chakrapani Subramanyam ,  Lawrence N. Tumey

IPC分类号： C07H15/26 ,  A61K47/68 ,  A61P35/00 ,  A61K45/06

CPC分类号： C07H15/26 ,  A61K47/6807 ,  A61P35/00 ,  A61K45/06

摘要： The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.