公开(公告)号：US11905284B2

公开(公告)日：2024-02-20

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

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：US20230192654A1

公开(公告)日：2023-06-22

申请号：US17969479

申请日：2022-10-19

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 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

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

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：US11198692B2

公开(公告)日：2021-12-14

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

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：US20180002331A1

公开(公告)日：2018-01-04

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

CPC分类号： C07D471/04

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：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.

公开(公告)号：US09845301B2

公开(公告)日：2017-12-19

申请号：US15221658

申请日：2016-07-28

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

CPC分类号： 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

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：US11524954B2

公开(公告)日：2022-12-13

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 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107

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：US20210309669A1

公开(公告)日：2021-10-07

申请号：US17260247

申请日：2019-07-10

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Laura Ann McAllister ,  Steven Victor O'Neil

IPC分类号： C07D491/107

摘要： The present invention provides, in part, a compound selected from the group consisting of: 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl (3R)-3-[(cyclopropylsulfonyl)amino]-1-oxa-8-azaspiro[4.5]decane-8-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate; 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-1; and 1,1,1,3,3,3-hexafluoropropan-2-yl 3-{[(cyclopropylmethyl)sulfonyl]amino}-1-oxa-9-azaspiro[5.5]undecane-9-carboxylate, ENT-2, 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, steatohepatitis [e.g. nonalcoholic Steatohepatitis (NASH)], stroke, or cancer.

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.