公开(公告)号：US20160090381A1

公开(公告)日：2016-03-31

申请号：US14864840

申请日：2015-09-24

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D401/14

摘要： 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.

摘要翻译： 本发明提供甲基 - 和三氟甲基取代的吡咯并吡啶，其药物组合物，调节受试者的RORγ活性和/或减少IL-17的量的方法，以及使用这种吡咯并吡啶治疗各种医学病症的方法及其药物组合物。

公开(公告)号：US20230339960A1

公开(公告)日：2023-10-26

申请号：US18342977

申请日：2023-06-28

申请人： Pfizer Inc.

发明人： 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分类号： C07D491/056 ,  C07F7/18 ,  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 ,  A61K31/40

CPC分类号： C07D491/056 ,  C07F7/1804 ,  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 ,  A61K31/40

摘要： 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. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

公开(公告)号：US20180170928A1

公开(公告)日：2018-06-21

申请号：US15889296

申请日：2018-02-06

申请人： Pfizer Inc.

发明人： 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

IPC分类号： C07D471/04 ,  C07D401/14

CPC分类号： C07D471/04 ,  C07D401/14

摘要： 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：US20170233390A1

公开(公告)日：2017-08-17

申请号：US15581310

申请日：2017-04-28

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D401/14

摘要： 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：US20190092750A1

公开(公告)日：2019-03-28

申请号：US16206166

申请日：2018-11-30

申请人： PFIZER INC.

发明人： KATHERINE LIN LEE ,  CHRISTOPHE PHILIPPE ALLAIS ,  CHRISTOPH MARTIN DEHNHARDT ,  LORI KRIM GAVRIN ,  SEUNGIL HAN ,  DAVID HEPWORTH ,  ARTHUR LEE ,  FRANK ELDRIDGE LOVERING ,  JOHN PAUL MATHIAS ,  DAFYDD RHYS OWEN ,  NIKOLAOS PAPAIOANNOU ,  EDDINE SAIAH ,  JOSEPH WALTER STROHBACH ,  JOHN DAVID TRZUPEK ,  STEPHEN WAYNE WRIGHT ,  CHRISTOPH WOLFGANG ZAPF

IPC分类号： C07D401/12 ,  C07D413/04 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K45/06 ,  C07D401/14 ,  C07D207/273 ,  C07D491/18 ,  C07D471/04 ,  C07D413/14 ,  A61K31/4015

摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula 1a, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20180244646A1

公开(公告)日：2018-08-30

申请号：US15754650

申请日：2016-08-16

申请人： PFIZER INC.

发明人： KATHERINE LIN LEE ,  CHRISTOPHE PHILIPPE ALLAIS ,  CHRISTOPH MARTIN DEHNHARDT ,  LORI KRIM GAVRIN ,  SEUNGIL HAN ,  DAVID HEPWORTH ,  ARTHUR LEE ,  FRANK ELDRIDGE LOVERING ,  JOHN PAUL MATHIAS ,  DAFYDD RHYS OWEN ,  NIKOLAOS PAPAIOANNOU ,  EDDINE SAIAH ,  JOSEPH WALTER STROHBACH ,  JOHN DAVID TRZUPEK ,  STEPHEN WAYNE WRIGHT ,  CHRISTOPH WOLFGANG ZAPF

IPC分类号： C07D401/12 ,  A61K31/4709 ,  C07D413/14 ,  A61K31/4725 ,  A61K45/06 ,  C07D401/14 ,  C07D413/04 ,  C07D207/273 ,  A61K31/4015 ,  C07D491/18 ,  A61K31/4745 ,  C07D471/04 ,  A61K31/4375

CPC分类号： C07D401/12 ,  A61K31/4015 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K45/06 ,  C07D207/273 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D491/18

摘要： 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.