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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.
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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/2016/06/02/US20160152637A1/abs.jpg.150x150.jpg)
12.发明申请公开(公告)号：US20160152637A1
公开(公告)日：2016-06-02
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.
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![Alkyl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds](/abs-image/US/2015/08/27/US20150239908A1/abs.jpg.150x150.jpg)
13.发明申请Alkyl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds 审中-公开烷基取代的六氢吡喃并[3,4-d] [1,3]噻嗪-2-胺化合物公开(公告)号：US20150239908A1
公开(公告)日：2015-08-27
申请号：US14429215
申请日：2013-09-09
申请人： PFIZER INC.
发明人： Michael Aaron Brodney , Elizabeth Mary Beck , Christopher Ryan Butler , Jennifer Elizabeth Davoren
IPC分类号： C07D513/04
CPC分类号： C07D513/04
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.
摘要翻译： 公开了化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有如说明书中定义的式I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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![Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds](/abs-image/US/2015/06/02/US09045499B2/abs.jpg.150x150.jpg)
14.发明授权Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 有权杂芳基取代的六氢吡喃并[3,4-d] [1,3]噻嗪-2-胺化合物公开(公告)号：US09045499B2
公开(公告)日：2015-06-02
申请号：US14464935
申请日：2014-08-21
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： C07D513/04 , 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。
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![Heteroaryl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds](/abs-image/US/2014/12/11/US20140364426A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140364426A1
公开(公告)日：2014-12-11
申请号：US14464935
申请日：2014-08-21
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： 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.
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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
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.-
![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)
17.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
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： C07D519/00 , C07D513/04 , A61K31/542
CPC分类号： C07D513/04 , A61K31/542 , 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.
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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)
18.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
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： C07D519/00 , C07D513/04 , A61K31/542
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.
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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)
19.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
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.
摘要翻译： 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)
20.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
申请人： Pfizer Inc.
IPC分类号： C07D513/04
CPC分类号： 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, 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.
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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