公开(公告)号：US20210061923A1

公开(公告)日：2021-03-04

申请号：US17091097

申请日：2020-11-06

Applicant: PFIZER INC.

Inventor： Andreas MADERNA ,  Chakrapani SUBRAMANYAM ,  Lawrence N. TUMEY ,  Zecheng CHEN ,  Jeffrey M. CASAVANT

IPC: C07K16/32 ,  C07D519/00 ,  C07F9/6561 ,  C07K5/062 ,  C07K5/09 ,  C07B59/00 ,  C07K16/28 ,  C07D495/04 ,  A61K47/68 ,  A61K47/65

Abstract: The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: F1-L1-T-L2-F2 where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

公开(公告)号：US20210308276A1

公开(公告)日：2021-10-07

申请号：US16321695

申请日：2017-07-31

Applicant: PFIZER INC.

Inventor： 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: A61K47/68

Abstract: 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 drig conjugates, and the resulting antibody drig conjugates made with components having heteroaryl sulfone-based conjugation handles.

公开(公告)号：US20180362519A1

公开(公告)日：2018-12-20

申请号：US16072291

申请日：2017-01-27

Applicant: PFIZER INC. ,  CovX Technologies Ireland Limited

Inventor： Chakrapani SUBRAMANYAM ,  Lawrence N. TUMEY ,  Longfei XIE ,  Carolyn LEVERETT ,  Beth C. VETELINO ,  Sai Chetan K. SUKURU ,  Sarah HUDSON ,  Venkata Ramana DOPPALAPUDI ,  Abhijit S. BHAT

IPC: C07D417/12 ,  A61K47/65 ,  A61K47/68 ,  A61P35/00 ,  C07D277/56

Abstract: The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

公开(公告)号：US20160271270A1

公开(公告)日：2016-09-22

申请号：US15070549

申请日：2016-03-15

Applicant: Pfizer Inc.

Inventor： Andreas MADERNA ,  Chakrapani SUBRAMANYAM ,  Lawrence N. TUMEY ,  Zecheng CHEN ,  Jeffrey M. CASAVANT

IPC: A61K47/48 ,  C07F9/6561 ,  C07K16/32 ,  C07K5/09 ,  C07B59/00 ,  C07K16/28 ,  C07D519/00 ,  C07K5/062

CPC classification number: C07K16/32 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6849 ,  A61K47/6863 ,  A61K47/6865 ,  A61K47/6869 ,  A61K47/6871 ,  C07B59/002 ,  C07B2200/05 ,  C07D495/04 ,  C07D519/00 ,  C07F9/6561 ,  C07K5/06052 ,  C07K5/0815 ,  C07K16/2803 ,  C07K16/2866

Abstract: The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: F1-L1-T-L2-F2 where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

Abstract translation: 其中F1，L1，T，L2和F2如本文所定义，可用于治疗增殖性疾病，其中本发明的二聚体可用作独立药物，抗体 - 药物共轭物（ADC）中的有效载荷和接头有效载体 可用于生产或管理此类ADC的化合物; 以及包含上述二聚体，连接物有效载体和ADC的组合物，以及使用这些二聚体，连接体有效载体和ADC的方法来治疗包括癌症在内的病理状况。