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.

公开(公告)号：US20180148432A1

公开(公告)日：2018-05-31

申请号：US15820679

申请日：2017-11-22

申请人： Pfizer Inc.

发明人： Natasha Mariam Kablaoui ,  Michael Eric Green ,  Justin Ian Montgomery ,  Michael Aaron Brodney ,  Patrick Robert Verhoest ,  Gregory Wayne Kauffman ,  Danica Antonia Rankic ,  Scot Richard Mente ,  Bruce Nelsen Rogers ,  Kapildev Kashmirilal Arora ,  Matthew Francis Dunn

IPC分类号： C07D403/04 ,  C07D417/04 ,  A61P25/00 ,  C07D231/20 ,  C07D413/04

CPC分类号： C07D403/04 ,  A61P25/00 ,  C07B2200/13 ,  C07D231/20 ,  C07D413/04 ,  C07D417/04

摘要： The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R9, X, m and n are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating kappa opioid (κ-opioid) associated disorders including, e.g., a neurological disorder, or psychiatric disorder such as a neurocognitive disorder, substance abuse disorder, depressive disorder, anxiety disorder, trauma and stressor related disorder and feeding and eating disorder.

公开(公告)号：US09850232B2

公开(公告)日：2017-12-26

申请号：US15077229

申请日：2016-03-22

申请人： PFIZER INC.

发明人： David Lawrence Firman Gray ,  Lei Zhang ,  Michael Aaron Brodney ,  Michael Eric Green ,  Chakrapani Subramanyam

IPC分类号： C07D403/12 ,  C07D471/04 ,  C07D401/12

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D471/04

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 D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

公开(公告)号：US09822097B2

公开(公告)日：2017-11-21

申请号：US15349075

申请日：2016-11-11

申请人： PFIZER INC.

发明人： Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Michael Eric Green ,  Jaclyn Louise Henderson ,  Chewah Lee ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Lei Zhang

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/501 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

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 D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.

公开(公告)号：US20170305931A1

公开(公告)日：2017-10-26

申请号：US15646572

申请日：2017-07-11

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC分类号： C07D513/04 ,  C07D513/20 ,  C07D513/10

CPC分类号： C07D513/04 ,  C07D513/10 ,  C07D513/20

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, R2 and R3 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：US09751895B2

公开(公告)日：2017-09-05

申请号：US15272501

申请日：2016-09-22

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Peter Justin Mikochik ,  John Charles Murray ,  Xinjun Hou

IPC分类号： C07D513/04 ,  C07D513/10 ,  C07D513/20

CPC分类号： C07D513/04 ,  C07D513/10 ,  C07D513/20

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, R2 and R3 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：US09745317B2

公开(公告)日：2017-08-29

申请号：US15305384

申请日：2015-04-14

申请人： PFIZER INC.

发明人： David Lawrence Firman Gray ,  Lei Zhang ,  Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Ivan Viktorovich Efremov ,  Michael Eric Green ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers

IPC分类号： C07D491/048 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

CPC分类号： C07D491/048 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

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 D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.