公开(公告)号：US10428034B2

公开(公告)日：2019-10-01

申请号：US15808242

申请日：2017-11-09

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：US10329308B2

公开(公告)日：2019-06-25

申请号：US15874987

申请日：2018-01-19

Applicant: PFIZER INC.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Christopher John Helal ,  Steven Victor O'Neil ,  Patrick Robert Verhoest

IPC: C07D513/10 ,  C07D221/20 ,  C07D295/185 ,  C07D401/08 ,  C07D401/12 ,  C07D491/10

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, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US10077269B2

公开(公告)日：2018-09-18

申请号：US15426423

申请日：2017-02-07

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：US20230146535A1

公开(公告)日：2023-05-11

申请号：US17964491

申请日：2022-10-12

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

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

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：US11524954B2

公开(公告)日：2022-12-13

申请号：US17040479

申请日：2019-03-25

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

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.

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：US20190300546A1

公开(公告)日：2019-10-03

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：US10131669B2

公开(公告)日：2018-11-20

申请号：US15327814

申请日：2015-07-10

Applicant: Pfizer Inc.

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

IPC: C07D487/04 ,  A61K31/519

Abstract: The present invention is directed to pyrazolopyrimine compounds or pharmaceutically acceptable salts which are inhibitors of PDE4 isozymes, especially with a binding affinity for PDE4B isoform, and compositions thereof.

公开(公告)号：US20170204099A1

公开(公告)日：2017-07-20

申请号：US15327814

申请日：2015-07-10

Applicant: Pfizer Inc.

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

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R3, and b 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：US09200000B2

公开(公告)日：2015-12-01

申请号：US14069640

申请日：2013-11-01

Applicant: Pfizer Inc.

Inventor： Christopher John Helal ,  Thomas Allen Chappie ,  John Michael Humphrey ,  Patrick Robert Verhoest ,  Eddie Yang

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.

Abstract translation: 本发明涉及式的化合物及其药学上可接受的盐，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物的用途，作为治疗疾病的方法或 选自哺乳动物中的中枢神经系统疾病，认知障碍，精神分裂症，痴呆等紊乱的病症。