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公开(公告)号：US11905284B2
公开(公告)日：2024-02-20
申请号：US17335666
申请日：2021-06-01
Applicant: PFIZER INC.
Inventor： Lei Zhang , Christopher Ryan Butler , Elizabeth Mary Beck , Michael Aaron Brodney , Matthew Frank Brown , Laura Ann McAllister , Erik Alphie LaChapelle , Adam Matthew Gilbert
IPC: C07D471/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , A61K31/437
CPC classification number: C07D471/04 , A61K31/437 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28
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: 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.-
![2-amino-6-methy1-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides](/abs-image/US/2018/07/24/US10028962B2/abs.jpg.150x150.jpg)
2.发明授权公开(公告)号：US10028962B2
公开(公告)日：2018-07-24
申请号：US15629215
申请日：2017-06-21
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D519/00 , C07D513/04 , A61K31/542
CPC classification number: C07D513/04 , A61K31/542 , C07D519/00
Abstract: 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.
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![N-(2-(2-AMINO-6-SUBSTITUTED-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]OXAZIN-8a(8H)-YL)-THIAZOL-4-YL) AMIDES](/abs-image/US/2017/12/28/US20170369506A1/abs.jpg.150x150.jpg)
3.发明申请公开(公告)号：US20170369506A1
公开(公告)日：2017-12-28
申请号：US15678511
申请日：2017-08-16
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill
IPC: C07D498/04 , C07D498/10
CPC classification number: C07D498/04 , C07D498/10
Abstract: 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, 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.
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![2-amino 6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides](/abs-image/US/2017/08/29/US09744173B2/abs.jpg.150x150.jpg)
4.发明授权公开(公告)号：US09744173B2
公开(公告)日：2017-08-29
申请号：US15427350
申请日：2017-02-08
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D519/00 , C07D513/04 , A61K31/542
CPC classification number: A61K31/542 , C07D513/04 , C07D519/00
Abstract: 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.
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![N-[2-(2-Amino-6,6-Disubstituted-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-YL)-1,3-Thiazol-4-YL]Amides](/abs-image/US/2017/03/30/US20170088558A1/abs.jpg.150x150.jpg)
5.发明申请公开(公告)号：US20170088558A1
公开(公告)日：2017-03-30
申请号：US15272501
申请日：2016-09-22
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Patrick Robert Verhoest , Peter Justin Mikochik , John Charles Murray , Xinjun Hou
IPC: C07D513/04 , C07D513/20 , C07D513/10
CPC classification number: C07D513/04 , C07D513/10 , C07D513/20
Abstract: 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.
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Patent Agency Ranking
![N-(2-(2-AMINO-6-SUBSTITUTED-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]OXAZIN-8a(8H)-YL)-THIAZOL-4-YL) AMIDES](/abs-image/US/2017/03/30/US20170088556A1/abs.jpg.150x150.jpg)
6.发明申请公开(公告)号：US20170088556A1
公开(公告)日：2017-03-30
申请号：US15272651
申请日：2016-09-22
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill
IPC: C07D498/04 , C07D498/10
CPC classification number: C07D498/04 , C07D498/10
Abstract: 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, 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.
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![2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,3-Thiazol-4-yl Amides](/abs-image/US/2017/01/12/US20170008911A1/abs.jpg.150x150.jpg)
7.发明申请2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,3-Thiazol-4-yl Amides 审中-公开2-氨基-6-甲基-4,4a，5,6-四氢吡喃并[3,4-d] [1,3]噻唑-8a（8H） - 基] - 噻唑-4-基酰胺公开(公告)号：US20170008911A1
公开(公告)日：2017-01-12
申请号：US15215193
申请日：2016-07-20
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Lei Zhang , Brian Thomas O'Neill , Gabriela Barreiro , Erik Alphie LaChapelle , Bruce Nelsen Rogers
IPC: C07D513/04 , C07D519/00
CPC classification number: A61K31/542 , C07D513/04 , C07D519/00
Abstract: 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.
Abstract translation: 并且变量R1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。
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![Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds](/abs-image/US/2016/01/12/US09233981B1/abs.jpg.150x150.jpg)
8.发明授权Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 有权取代的苯基六氢吡喃并[3,4-d] [1,3]噻嗪-2-胺化合物公开(公告)号：US09233981B1
公开(公告)日：2016-01-12
申请号：US14767414
申请日：2014-02-02
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Brian Thomas O'Neill , Christopher Ryan Butler , Elizabeth Mary Beck
IPC: C07D513/04
CPC classification number: C07D513/04
Abstract: 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, wherein 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.
Abstract translation: 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，其中所述化合物具有式I的结构，其中变量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。
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![Substituted Phenyl Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds](/abs-image/US/2015/12/31/US20150376207A1/abs.jpg.150x150.jpg)
9.发明申请Substituted Phenyl Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds 审中-公开取代苯基六氢吡喃并[3,4-d] [1,3]噻嗪-2-胺化合物公开(公告)号：US20150376207A1
公开(公告)日：2015-12-31
申请号：US14767414
申请日：2014-02-02
Applicant: PFIZER INC.
Inventor： Michael Aaron Brodney , Brian Thomas O'Neill , Christopher Ryan Butler , Elizabeth Mary Beck
IPC: C07D513/04
CPC classification number: C07D513/04
Abstract: 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.
Abstract translation: 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。
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![Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds](/abs-image/US/2014/09/02/US08822456B2/abs.jpg.150x150.jpg)
公开(公告)号：US08822456B2
公开(公告)日：2014-09-02
申请号：US14101462
申请日：2013-12-10
Applicant: Pfizer Inc.
Inventor： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Jennifer Elizabeth Davoren , Brian Thomas O'Neill
IPC: C07D513/04 , A61K31/542
CPC classification number: A61K31/542 , C07D513/04
Abstract: 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.
Abstract translation: 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。
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