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公开(公告)号:US11702424B2
公开(公告)日:2023-07-18
申请号:US16996117
申请日:2020-08-18
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D491/056 , C07F7/18 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07C69/94 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/40 , C07D207/08 , C07D207/267
CPC classification number: C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.-
公开(公告)号:US20210002251A1
公开(公告)日:2021-01-07
申请号:US17025026
申请日:2020-09-18
Applicant: Pfizer Inc.
Inventor: John Robert Springer , Balekudru Devadas , Danny James Garland , Margaret Lanahan Grapperhaus , Seungil Han , Susan Landis Hockerman , Robert Owen Hughes , Eddine Saiah , Mark Edward Schnute , Shaun Raj Selness , Daniel Patrick Walker , Zhao-Kui Wan , Li Xing , Christoph Wolfgang Zapf , Michelle Ann Schmidt
IPC: C07D401/04
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
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公开(公告)号:US20200377511A1
公开(公告)日:2020-12-03
申请号:US16996117
申请日:2020-08-18
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D491/056 , C07F7/18 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07C69/94 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/40 , C07D207/08 , C07D207/267
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, 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:US10463675B2
公开(公告)日:2019-11-05
申请号:US15585626
申请日:2017-05-03
Applicant: Pfizer Inc.
Inventor: Andrew Fensome , Ariamala Gopalsamy , Brian S. Gerstenberger , Ivan Viktorovich Efremov , Zhao-Kui Wan , Betsy Pierce , Jean-Baptiste Telliez , John I. Trujillo , Liying Zhang , Li Xing , Eddine Saiah
IPC: C07D487/08 , A61K31/55 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D519/00
Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C═O, —SO2—, etc.; A′ is selected from the group consisting of a bond, C═O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1′ are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
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公开(公告)号:US10329302B2
公开(公告)日:2019-06-25
申请号:US15862691
申请日:2018-01-05
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D401/04 , A61K31/47 , C07D491/056 , C07F7/18 , A61K31/4015 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07C69/94 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/40 , C07D207/08 , C07D207/267
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, 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:US10266513B2
公开(公告)日:2019-04-23
申请号:US15624969
申请日:2017-06-16
Applicant: Pfizer Inc.
Inventor: John Robert Springer , Balekudru Devadas , Danny James Garland , Margaret Lanahan Grapperhaus , Seungil Han , Susan Landis Hockerman , Robert Owen Hughes , Eddine Saiah , Mark Edward Schnute , Shaun Raj Selness , Daniel Patrick Walker , Zhao-Kui Wan , Li Xing , Christoph Wolfgang Zapf , Michelle Ann Schmidt
IPC: C07D403/04 , C07D401/04
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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公开(公告)号:US09879022B2
公开(公告)日:2018-01-30
申请号:US15232892
申请日:2016-08-10
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D491/056 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , A61K31/47 , A61K31/517 , A61K31/4015 , A61K31/4709 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D413/12 , C07D417/12 , C07D487/04 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07C69/94 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , C07F7/18 , A61K31/40 , C07D207/08 , C07D207/267
CPC classification number: C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, 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:US09663526B2
公开(公告)日:2017-05-30
申请号:US14829753
申请日:2015-08-19
Applicant: Pfizer Inc.
Inventor: Andrew Fensome , Ariamala Gopalsamy , Brian S. Gerstenberger , Ivan Viktorovich Efremov , Zhao-Kui Wan , Betsy Pierce , Jean-Baptiste Telliez , John I. Trujillo , Liying Zhang , Li Xing , Eddine Saiah
IPC: A61K31/506 , C07D487/08 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D519/00
CPC classification number: A61K31/55 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D487/08 , C07D519/00
Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C═O, —SO2—, etc.; A′ is selected from the group consisting of a bond, C═O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1′ are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
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公开(公告)号:US10815213B2
公开(公告)日:2020-10-27
申请号:US16296319
申请日:2019-03-08
Applicant: Pfizer Inc.
Inventor: John Robert Springer , Balekudru Devadas , Danny James Garland , Margaret Lanahan Grapperhaus , Seungil Han , Susan Landis Hockerman , Robert Owen Hughes , Eddine Saiah , Mark Edward Schnute , Shaun Raj Selness , Daniel Patrick Walker , Zhao-Kui Wan , Li Xing , Christoph Wolfgang Zapf , Michelle Ann Schmidt
IPC: C07D401/04 , C07D401/14 , A61K31/4155 , A61K31/454 , A61P29/00 , A61P35/00
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
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公开(公告)号:US10793579B2
公开(公告)日:2020-10-06
申请号:US16411679
申请日:2019-05-14
Applicant: Pfizer Inc.
Inventor: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC: C07D401/14 , A61K31/47 , A61K31/4709 , A61K31/4725 , C07D491/056 , C07F7/18 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07C69/94 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/4015 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/40 , C07D207/08 , C07D207/267
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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