公开(公告)号：US11602525B2

公开(公告)日：2023-03-14

申请号：US15306481

申请日：2015-04-21

Applicant: RINAT NEUROSCIENCE CORP. ,  PFIZER INC.

Inventor： Pavel Strop ,  Katherine Anne Delaria ,  Magdalena Dorywalska ,  Davide Luciano Foletti ,  Russell George Dushin ,  David Louis Shelton ,  Arvind Rajpal

IPC: A61K31/427 ,  A61K47/68 ,  A61K47/65 ,  C07K16/30 ,  G01N33/574 ,  A61K39/00

Abstract: The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.

公开(公告)号：US10967068B2

公开(公告)日：2021-04-06

申请号：US15504801

申请日：2015-08-14

Applicant: PFIZER INC. ,  RINAT NEUROSCIENCE CORP.

Inventor： Russell George Dushin ,  Pavel Strop ,  Magdalena Grazyna Dorywalska ,  Ludivine Moine

IPC: A61K47/65 ,  A61K47/64 ,  A61K47/68 ,  A61K39/00

Abstract: The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.

公开(公告)号：US08828401B2

公开(公告)日：2014-09-09

申请号：US13670612

申请日：2012-11-07

Applicant: Pfizer Inc.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: C07K7/02 ,  C07K5/02 ,  C07K16/00 ,  A61K47/48

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。

公开(公告)号：US11712480B2

公开(公告)日：2023-08-01

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

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

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

公开(公告)号：US09249186B2

公开(公告)日：2016-02-02

申请号：US14793942

申请日：2015-07-08

Applicant: PFIZER INC.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: C07K7/02 ,  C07K5/02 ,  C07K16/00 ,  C07K7/06

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

公开(公告)号：US09138486B2

公开(公告)日：2015-09-22

申请号：US14322262

申请日：2014-07-02

Applicant: PFIZER INC.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: A61K47/48 ,  A61K38/06 ,  A61K38/08 ,  A61K38/07 ,  C07K7/02 ,  C07K5/083 ,  C07K5/02 ,  C07K16/00

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。