公开(公告)号：US10723711B2

公开(公告)日：2020-07-28

申请号：US16547037

申请日：2019-08-21

申请人： PFIZER INC.

发明人： 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分类号： 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

摘要： 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：US08933095B2

公开(公告)日：2015-01-13

申请号：US14068707

申请日：2013-10-31

申请人： Pfizer Inc.

发明人： Amy Beth Dounay ,  Laura Ann McAllister ,  Vinod Dipak Parikh ,  Suobao Rong ,  Patrick Robert Verhoest

IPC分类号： C07D235/02 ,  C07D403/00 ,  C07D231/56 ,  C07D487/00 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.

摘要翻译： 式I化合物：其中X，Y，Z，R 1，R 2，R 3，R 4如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其他精神病学，神经变性和/ 或哺乳动物包括人类的神经障碍。

公开(公告)号：US20230192690A1

公开(公告)日：2023-06-22

申请号：US18112156

申请日：2023-02-21

申请人： PFIZER INC.

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

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

CPC分类号： C07D471/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61K31/437

摘要： 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：US20210024497A1

公开(公告)日：2021-01-28

申请号：US17040479

申请日：2019-03-25

申请人： Pfizer Inc.

发明人： 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分类号： C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D413/14

摘要： 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：US10858373B2

公开(公告)日：2020-12-08

申请号：US16429678

申请日：2019-06-03

申请人： Pfizer Inc.

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

IPC分类号： C07D513/10 ,  A61P37/00 ,  C07D401/12 ,  C07D471/10 ,  C07D493/10 ,  C07D498/10 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  C07D221/20

摘要： The present invention provides, in part, heterocyclic spiro 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：US20200207762A1

公开(公告)日：2020-07-02

申请号：US16797966

申请日：2020-02-21

申请人： Pfizer Inc.

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

IPC分类号： C07D471/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P25/00

摘要： 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：US10604519B2

公开(公告)日：2020-03-31

申请号：US15637071

申请日：2017-06-29

申请人： Pfizer Inc.

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

IPC分类号： C07D471/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

摘要： 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：US10428034B2

公开(公告)日：2019-10-01

申请号：US15808242

申请日：2017-11-09

申请人： PFIZER INC.

发明人： 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分类号： 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

摘要： 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：US20190292203A1

公开(公告)日：2019-09-26

申请号：US16429678

申请日：2019-06-03

申请人： Pfizer Inc.

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

IPC分类号： C07D513/10 ,  A61P37/00 ,  C07D498/10 ,  C07D493/10 ,  C07D471/10 ,  A61P3/00 ,  C07D221/20 ,  A61P35/00 ,  A61P25/00 ,  A61P9/00 ,  C07D401/12

摘要： The present invention provides, in part, heterocyclic spiro 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：US10329308B2

公开(公告)日：2019-06-25

申请号：US15874987

申请日：2018-01-19

申请人： PFIZER INC.

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

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

摘要： 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.