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公开(公告)号:US20170233371A1
公开(公告)日:2017-08-17
申请号:US15497862
申请日:2017-04-26
Applicant: Pfizer Inc.
Inventor: Mark Edward Schnute , Gõran Mattias Wennerstål , James Robert Blinn , Neelu Kaila , James Richard Kiefer, Jr. , Scot Richard Mente , Ravi G. Kurumbail , Marvin Jay Meyers , Atli Thorarensen , Li Xing , Christoph Wolfgang Zapf , Edouard Zamaratski , Andrew Christopher Flick , Peter Jones
IPC: C07D401/14 , C07D413/14 , C07D405/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D403/04 , C07D401/04 , C07D417/14
CPC classification number: C07D401/14 , A61K31/454 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5355 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , Y02A50/406 , A61K2300/00
Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
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公开(公告)号:US20160052930A1
公开(公告)日:2016-02-25
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
IPC: C07D487/08 , C07D519/00 , A61K45/06 , C07D401/14 , C07D405/14 , A61K31/506 , C07D403/14
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 a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. 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:US20160046597A1
公开(公告)日:2016-02-18
申请号:US14448220
申请日:2014-07-31
Applicant: PFIZER INC.
Inventor: Mark Edward Schnute , Göran Mattias Wennerstål , James Robert Blinn , Neelu Kaila , James Richard Kiefer, JR. , Scot Richard Mente , Ravi G. Kurumbail , Marvin Jay Meyers , Atli Thorarensen , Li Xing , Christoph Wolfgang Zapf , Edouard Zamaratski , Andrew Christopher Flick , Peter Jones
IPC: C07D401/04 , C07D413/14 , C07D403/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D401/14 , C07D405/14
CPC classification number: C07D401/14 , A61K31/454 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5355 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , Y02A50/406 , A61K2300/00
Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
Abstract translation: 本发明提供化合物,药物组合物,抑制受试者的RORγ活性和/或减少IL-17的量的方法,以及使用这些化合物和药物组合物治疗各种医学病症的方法。
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公开(公告)号:US11197867B2
公开(公告)日:2021-12-14
申请号:US16920027
申请日:2020-07-02
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 , A61K31/55 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D487/08 , C07D519/00
Abstract: A compound compound having the structure: or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. 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:US10980815B2
公开(公告)日:2021-04-20
申请号:US16580667
申请日:2019-09-24
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 , A61K31/55 , 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:US20190202798A1
公开(公告)日:2019-07-04
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
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 cases 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:US20190144429A1
公开(公告)日:2019-05-16
申请号:US16261689
申请日:2019-01-30
Applicant: Pfizer Inc.
Inventor: Mark Edward Schnute , Gõran Mattias Wennerstål , James Robert Blinn , Neelu Kaila , James Richard Kiefer, JR. , Scot Richard Mente , Ravi G. Kurumbail , Marvin Jay Meyers , Atli Thorarensen , Li Xing , Christoph Wolfgang Zapf , Edouard Zamaratski , Andrew Christopher Flick , Peter Jones
IPC: C07D401/14 , C07D405/14 , C07D413/14 , C07D403/04 , C07D487/04 , C07D471/04 , C07D417/14 , C07D413/04 , C07D407/14 , C07D401/04 , A61K31/5355 , A61K31/519 , A61K31/506 , A61K31/497 , A61K31/454
Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
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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:US20200039960A1
公开(公告)日:2020-02-06
申请号:US16656702
申请日:2019-10-18
Applicant: Pfizer Inc.
Inventor: Mark Edward Schnute , Göran Mattias Wennerstål , James Robert Blinn , Neelu Kaila , James Richard Kiefer, Jr. , Scot Richard Mente , Ravi G. Kurumbail , Marvin Jay Meyers , Atli Thorarensen , Li Xing , Christoph Wolfgang Zapf , Edouard Zamaratski , Andrew Christopher Flick , Peter Jones
IPC: C07D401/14 , C07D413/14 , A61K31/454 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5355 , C07D407/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D401/04 , C07D403/04 , C07D405/14
Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
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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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