公开(公告)号：US10385036B2

公开(公告)日：2019-08-20

申请号：US15547228

申请日：2016-01-29

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand J. Unwalla

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides sulfonamide-substituted indoles and Methods of Use Thereof-substituted pyrrolopyridines, pharmaceutical compositions thereof methods of modulating RORy activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such indoles and pharmaceutical compositions thereof.

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：US09670201B2

公开(公告)日：2017-06-06

申请号：US14864840

申请日：2015-09-24

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Göran Mattias Wennerstål ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang

IPC: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  C07D471/04 ,  C07D401/14

CPC classification number: C07D471/04 ,  C07D401/14

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

公开(公告)号：US09663526B2

公开(公告)日：2017-05-30

申请号：US14829753

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Andrew Fensome ,  Ariamala Gopalsamy ,  Brian S. Gerstenberger ,  Ivan Viktorovich Efremov ,  Zhao-Kui Wan ,  Betsy Pierce ,  Jean-Baptiste Telliez ,  John I. Trujillo ,  Liying Zhang ,  Li Xing ,  Eddine Saiah

IPC: A61K31/506 ,  C07D487/08 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D519/00

CPC classification number: A61K31/55 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D519/00

Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C═O, —SO2—, etc.; A′ is selected from the group consisting of a bond, C═O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1′ are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.