公开(公告)号：US10336748B2

公开(公告)日：2019-07-02

申请号：US15546887

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: C07D471/04

Abstract: The present invention provides methoxy-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：US20190150401A1

公开(公告)日：2019-05-23

申请号：US16268857

申请日：2019-02-06

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 Jal Unwalla

IPC: A01K5/01 ,  B65D77/20 ,  B65D25/04 ,  B65D1/34 ,  A01K7/00 ,  B65D25/18 ,  A23K20/00 ,  A23K50/48 ,  B65D1/36

CPC classification number: A01K5/0121 ,  A01K7/00 ,  A23K20/00 ,  A23K50/48 ,  B65D1/34 ,  B65D1/36 ,  B65D25/04 ,  B65D25/18 ,  B65D77/2024 ,  B65D85/70 ,  B65D2577/205 ,  C07D401/14 ,  C07D471/04

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：US10227346B2

公开(公告)日：2019-03-12

申请号：US15889296

申请日：2018-02-06

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 Jal Unwalla

IPC: A61K31/437 ,  A61K31/4353 ,  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：US20180002330A1

公开(公告)日：2018-01-04

申请号：US15546887

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: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides methoxy-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：US09856263B2

公开(公告)日：2018-01-02

申请号：US15305390

申请日：2015-04-15

Applicant: PFIZER INC.

Inventor： David Lawrence Firman Gray ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  Scot Richard Mente ,  Chakrapani Subramanyam

IPC: C07D487/04 ,  C07D519/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D519/00

Abstract: The present invention provides, in part, compounds of Formula (I): and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

公开(公告)号：US20170233371A1

公开(公告)日：2017-08-17

申请号：US15497862

申请日：2017-04-26

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Gõran 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 ,  C07D413/14 ,  C07D405/14 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/04 ,  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：US09617275B2

公开(公告)日：2017-04-11

申请号：US14820611

申请日：2015-08-07

Applicant: PFIZER INC.

Inventor： Jotham Wadsworth Coe ,  John Arthur Allen ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Edward Raymond Guilmette ,  Anthony Richard Harris ,  Chris John Helal ,  Jaclyn Louise Henderson ,  Scot Richard Mente ,  Deane Milford Nason ,  Steven Victor O'Neil ,  Chakrapani Subramanyam ,  Wenjian Xu

IPC: C07D491/048 ,  C07D491/04 ,  C07D495/04 ,  C07D519/04 ,  C07D519/00

CPC classification number: A61K31/53 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D519/04

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

公开(公告)号：US20160046597A1

公开(公告)日：2016-02-18

申请号：US14448220

申请日：2014-07-31

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: C07D401/04 ,  C07D413/14 ,  C07D403/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14

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.

Abstract translation: 本发明提供化合物，药物组合物，抑制受试者的RORγ活性和/或减少IL-17的量的方法，以及使用这些化合物和药物组合物治疗各种医学病症的方法。

公开(公告)号：US20200039960A1

公开(公告)日：2020-02-06

申请号：US16656702

申请日：2019-10-18

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

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：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.