公开(公告)号：US10738063B2

公开(公告)日：2020-08-11

申请号：US16427627

申请日：2019-05-31

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Matthew Merrill Hayward

IPC: C07D498/04 ,  C07D519/00

Abstract: The present invention is directed to PDE4B inhibitors of Formula I: (I) or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R2, R3, and R4 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

公开(公告)号：US20190322674A1

公开(公告)日：2019-10-24

申请号：US16455020

申请日：2019-06-27

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

公开(公告)号：US20190263816A1

公开(公告)日：2019-08-29

申请号：US15736942

申请日：2016-06-09

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Ramalakshmi Yegna Chandrasekaran

IPC: C07D471/14 ,  C07D491/147 ,  C07D513/14 ,  C07D519/00 ,  C07D491/22

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

公开(公告)号：US20180346475A1

公开(公告)日：2018-12-06

申请号：US16056968

申请日：2018-08-07

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

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：US09296761B2

公开(公告)日：2016-03-29

申请号：US14829842

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  A61K31/53 ,  A61K31/4353

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

公开(公告)号：US09145427B2

公开(公告)日：2015-09-29

申请号：US14549871

申请日：2014-11-21

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Byrce Tuttle ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/53 ,  A61K31/4353 ,  A61P9/12 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

Abstract translation: 本发明涉及如下式I所述的新一类三嗪衍生物，其中A，X，R 1，R 2，R 3和R 4如本文所定义，以及该化合物作为PDE10抑制剂的用途。

公开(公告)号：US20150080401A1

公开(公告)日：2015-03-19

申请号：US14549871

申请日：2014-11-21

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

公开(公告)号：US12049465B2

公开(公告)日：2024-07-30

申请号：US17886807

申请日：2022-08-12

Applicant: PFIZER INC.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Ramalakshmi Yegna Chandrasekaran

IPC: C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/22 ,  C07D513/14 ,  C07D519/00

CPC classification number: C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/22 ,  C07D513/14 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

公开(公告)号：US20230192654A1

公开(公告)日：2023-06-22

申请号：US17969479

申请日：2022-10-19

Applicant: PFIZER, INC.

Inventor： Lei Zhang ,  Erik Alphie LaChapelle ,  Christopher Ryan Butler ,  Natasha Mariam Kablaoui ,  Michael Aaron Brodney ,  Laura Ann McAllister ,  Qingyi Yang ,  Christopher John Helal ,  Damien Webb

IPC: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

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: X1, X2, R1, R2, m and n 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, Parkinson's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.