公开(公告)号：US20200262833A1

公开(公告)日：2020-08-20

申请号：US16625202

申请日：2018-06-14

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04 ,  A61P25/28 ,  A61P25/30 ,  A61P25/18

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)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

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：US09428523B2

公开(公告)日：2016-08-30

申请号：US15019342

申请日：2016-02-09

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Gabriela Barreiro ,  Erik Alphie LaChapelle ,  Bruce Nelsen Rogers

IPC分类号： C07D513/04 ,  C07D519/00

CPC分类号： A61K31/542 ,  C07D513/04 ,  C07D519/00

摘要： The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09198917B2

公开(公告)日：2015-12-01

申请号：US14695920

申请日：2015-04-24

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC分类号： C07D513/04 ,  A61K31/542

CPC分类号： A61K31/542 ,  C07D513/04

摘要： The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09192612B2

公开(公告)日：2015-11-24

申请号：US14694288

申请日：2015-04-23

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC分类号： A61K31/542 ,  C07D513/04

CPC分类号： A61K31/542 ,  C07D513/04

摘要： The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20150224110A1

公开(公告)日：2015-08-13

申请号：US14694288

申请日：2015-04-23

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Erik Alphie LaChapelle ,  Brian Thomas O'Neill

IPC分类号： A61K31/542

CPC分类号： A61K31/542 ,  C07D513/04

摘要： The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 本发明涉及所公开的化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有式I的结构，并且变量R1和R2如说明书中所定义。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20140323474A1

公开(公告)日：2014-10-30

申请号：US14325409

申请日：2014-07-08

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC分类号： C07D513/04

CPC分类号： A61K31/542 ,  C07D513/04

摘要： The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 本发明提供式I化合物及其互变异构体，以及化合物和互变异构体的药学上可接受的盐，其中化合物具有其中变量R1，R2，R3，R4和x如说明书中所定义的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20130296308A1

公开(公告)日：2013-11-07

申请号：US13886405

申请日：2013-05-03

申请人： PFIZER INC.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Jennifer Elizabeth Davoren ,  Brian Thomas O'Neill

IPC分类号： C07D513/04

CPC分类号： C07D513/04 ,  A61K31/542

摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20240190869A1

公开(公告)日：2024-06-13

申请号：US18532547

申请日：2023-12-07

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 ,  A61K31/437 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC分类号： C07D471/04 ,  A61K31/437 ,  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：US20210309659A1

公开(公告)日：2021-10-07

申请号：US17335666

申请日：2021-06-01

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

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.