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：US20190002466A1

公开(公告)日：2019-01-03

申请号：US15569874

申请日：2016-04-19

Applicant: Pfizer Inc.

Inventor： Atli THORARENSEN ,  Matthew Frank BROWN ,  Agustin CASIMIRO-GARCIA ,  Ye CHE ,  Mark Edward FLANAGAN ,  Adam Matthew GILBERT ,  Matthew Merrill HAYWARD ,  Jean-Baptiste TELLIEZ ,  Rayomand Jal UNWALLA ,  John I. TRUJILLO ,  Sidney Xi LIANG

IPC: C07D487/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.