公开(公告)号：US20200262833A1

公开(公告)日：2020-08-20

申请号：US16625202

申请日：2018-06-14

Applicant: Pfizer Inc.

Inventor： Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Christopher Ryan Butler ,  Adam Matthew Gilbert ,  Erik Alphie Lachapelle ,  Laura Ann McAllister ,  Daniel Paul Uccello ,  Lei Zhang

IPC: C07D471/04 ,  A61P25/28 ,  A61P25/30 ,  A61P25/18

Abstract: The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R1)a, (R2)b, (R3)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US10723711B2

公开(公告)日：2020-07-28

申请号：US16547037

申请日：2019-08-21

Applicant: PFIZER INC.

Inventor： Christopher Ryan Butler ,  Laura Ann McAllister ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Adam Matthew Gilbert ,  Christopher John Helal ,  Douglas Scott Johnson ,  Justin Ian Montgomery ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Patrick Robert Verhoest ,  Damien Webb

IPC: C07D295/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D498/10 ,  C07D491/107 ,  C07D401/12 ,  C07D471/10 ,  C07D487/04 ,  C07D211/48 ,  C07D471/08 ,  C07D515/10 ,  C07F9/6561 ,  C07D405/14 ,  C07D413/14 ,  C07D405/12 ,  C07D493/10

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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US20150158864A1

公开(公告)日：2015-06-11

申请号：US14559294

申请日：2014-12-03

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla

IPC: C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07D487/04 ,  C07D471/08

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides 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.

Abstract translation: 本发明提供药学活性吡咯并[2,3-d]嘧啶基和吡咯并[2,3-d]吡啶基丙烯酰胺及其类似物。 这些化合物可用于抑制Janus Kinase（JAK）。 本发明还涉及包含制备这种化合物的方法的组合物，以及用于治疗和预防由JAK介导的病症的方法。

公开(公告)号：US20240190869A1

公开(公告)日：2024-06-13

申请号：US18532547

申请日：2023-12-07

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

Abstract: The present invention provides, in part, compounds of Formula I:




or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US20210309659A1

公开(公告)日：2021-10-07

申请号：US17335666

申请日：2021-06-01

Applicant: PFIZER INC.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61K31/437

Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US09845301B2

公开(公告)日：2017-12-19

申请号：US15221658

申请日：2016-07-28

Applicant: PFIZER INC.

Inventor： Christopher Ryan Butler ,  Laura Ann McAllister ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Adam Matthew Gilbert ,  Christopher John Helal ,  Douglas Scott Johnson ,  Justin Ian Montgomery ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Patrick Robert Verhoest ,  Damien Webb

IPC: C07D295/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D498/10 ,  C07D491/107 ,  C07D401/12 ,  C07D471/10 ,  C07D487/04 ,  C07D211/48 ,  C07D471/08 ,  C07D515/10 ,  C07F9/6561 ,  C07D405/14 ,  C07D413/14 ,  C07D405/12 ,  C07D493/10

CPC classification number: C07D295/14 ,  C07D211/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D493/10 ,  C07D498/10 ,  C07D515/10 ,  C07F9/6561

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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US12077533B2

公开(公告)日：2024-09-03

申请号：US17393463

申请日：2021-08-04

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I Trujillo

IPC: A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC classification number: C07D471/04 ,  A61K31/4523 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure:




or a pharmaceutically acceptable salt thereof, as set forth in the Description.

公开(公告)号：US11712480B2

公开(公告)日：2023-08-01

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: A61K47/54 ,  A61K47/68 ,  C07K4/00 ,  C07K5/02 ,  C07K7/02 ,  A61K47/50 ,  C07K5/062

CPC classification number: A61K47/6855 ,  A61K47/50 ,  A61K47/545 ,  A61K47/6867 ,  C07K4/00 ,  C07K5/0205 ,  C07K5/06052 ,  C07K7/02

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 drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

公开(公告)号：US11198692B2

公开(公告)日：2021-12-14

申请号：US16625202

申请日：2018-06-14

Applicant: Pfizer Inc.

Inventor： Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Christopher Ryan Butler ,  Adam Matthew Gilbert ,  Erik Alphie Lachapelle ,  Laura Ann McAllister ,  Daniel Paul Uccello ,  Lei Zhang

IPC: C07D471/04

Abstract: The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R1)a, (R2)b, (R3)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US11111242B2

公开(公告)日：2021-09-07

申请号：US15446500

申请日：2017-03-01

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo

IPC: A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. 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.