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.

公开(公告)号：US20170252352A1

公开(公告)日：2017-09-07

申请号：US15314574

申请日：2015-05-18

Applicant: Pfizer Inc.

Inventor： Eugene Lvovich Piatnitski CHEKLER ,  Adam Matthew GILBERT ,  Rayomand Jal UNWALLA ,  Patrick Robert VERHOEST ,  James Thomas ANDERSON

IPC: A61K31/549 ,  A61K31/433 ,  A61K31/472 ,  A61K45/06 ,  A61K31/397 ,  A61K31/451 ,  A61K31/402 ,  A61K31/4725 ,  A61K31/277

CPC classification number: A61K31/549 ,  A61K31/277 ,  A61K31/397 ,  A61K31/402 ,  A61K31/433 ,  A61K31/451 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: I II III wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or —(CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.