公开(公告)号：US10329302B2

公开(公告)日：2019-06-25

申请号：US15862691

申请日：2018-01-05

Applicant: Pfizer Inc.

Inventor： John David Trzupek ,  Katherine Lin Lee ,  Mark Edward Bunnage ,  Seungil Han ,  David Hepworth ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Nikolaos Papaioannou ,  Betsy Susan Pierce ,  Joseph Walter Strohbach ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf ,  Lori Krim Gavrin ,  Arthur Lee ,  David Randolph Anderson ,  Kevin Joseph Curran ,  Christoph Martin Dehnhardt ,  Eddine Saiah ,  Joel Adam Goldberg ,  Xiaolun Wang ,  Horng-Chih Huang ,  Richard Vargas ,  Michael Dennis Lowe ,  Akshay Patny

IPC: C07D401/04 ,  A61K31/47 ,  C07D491/056 ,  C07F7/18 ,  A61K31/4015 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D207/26 ,  C07D215/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07C69/94 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D207/273 ,  C07D498/04 ,  C07D209/52 ,  A61K31/40 ,  C07D207/08 ,  C07D207/267

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US10266513B2

公开(公告)日：2019-04-23

申请号：US15624969

申请日：2017-06-16

Applicant: Pfizer Inc.

Inventor： John Robert Springer ,  Balekudru Devadas ,  Danny James Garland ,  Margaret Lanahan Grapperhaus ,  Seungil Han ,  Susan Landis Hockerman ,  Robert Owen Hughes ,  Eddine Saiah ,  Mark Edward Schnute ,  Shaun Raj Selness ,  Daniel Patrick Walker ,  Zhao-Kui Wan ,  Li Xing ,  Christoph Wolfgang Zapf ,  Michelle Ann Schmidt

IPC: C07D403/04 ,  C07D401/04

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

公开(公告)号：US20180282304A1

公开(公告)日：2018-10-04

申请号：US16008419

申请日：2018-06-14

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Göran Mattias Wennerstål ,  James Robert Blinn ,  Neelu Kaila ,  James Richard Kiefer, JR. ,  Scot Richard Mente ,  Ravi G. Kurumbail ,  Marvin Jay Meyers ,  Atli Thorarensen ,  Li Xing ,  Christoph Wolfgang Zapf ,  Edouard Zamaratski ,  Andrew Christopher Flick ,  Peter Jones

IPC: C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D401/04 ,  C07D407/14 ,  C07D413/04 ,  C07D405/14 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14

Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.

公开(公告)号：US20180086736A1

公开(公告)日：2018-03-29

申请号：US15834545

申请日：2017-12-07

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Göran Mattias Wennerstål ,  James Robert Blinn ,  Neelu Kaila ,  James Richard Kiefer, JR. ,  Scot Richard Mente ,  Ravi G. Kurumbail ,  Marvin Jay Meyers ,  Atli Thorarensen ,  Li Xing ,  Christoph Wolfgang Zapf ,  Edouard Zamaratski ,  Andrew Christopher Flick ,  Peter Jones

IPC: C07D401/14 ,  C07D487/04 ,  C07D413/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D401/04 ,  C07D407/14 ,  C07D413/04 ,  C07D405/14 ,  C07D403/04 ,  C07D471/04 ,  C07D417/14

CPC classification number: C07D401/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  Y02A50/406 ,  A61K2300/00

Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.

公开(公告)号：US09879022B2

公开(公告)日：2018-01-30

申请号：US15232892

申请日：2016-08-10

Applicant: Pfizer Inc.

Inventor： John David Trzupek ,  Katherine Lin Lee ,  Mark Edward Bunnage ,  Seungil Han ,  David Hepworth ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Nikolaos Papaioannou ,  Betsy Susan Pierce ,  Joseph Walter Strohbach ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf ,  Lori Krim Gavrin ,  Arthur Lee ,  David Randolph Anderson ,  Kevin Joseph Curran ,  Christoph Martin Dehnhardt ,  Eddine Saiah ,  Joel Adam Goldberg ,  Xiaolun Wang ,  Horng-Chih Huang ,  Richard Vargas ,  Michael Dennis Lowe ,  Akshay Patny

IPC: C07D491/056 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/14 ,  A61K31/47 ,  A61K31/517 ,  A61K31/4015 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D207/26 ,  C07D215/48 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07C69/94 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D207/273 ,  C07D498/04 ,  C07D209/52 ,  C07F7/18 ,  A61K31/40 ,  C07D207/08 ,  C07D207/267

CPC classification number: C07D491/056 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07C69/94 ,  C07D207/08 ,  C07D207/26 ,  C07D207/267 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04 ,  C07F7/1804

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.