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公开(公告)号：US09890152B2
公开(公告)日：2018-02-13
申请号：US14745159
申请日：2015-06-19
Applicant: Genentech, Inc.
Inventor： Marian C. Bryan , Bryan Chan , Emily Hanan , Timothy Heffron , Hans Purkey , Richard Leonard Elliott , Robert Heald , Jamie Knight , Michael Lainchbury , Eileen M. Seward
IPC: C07D471/04 , C07D498/10 , A61K31/506 , A61K31/5377 , C07D498/08 , A61K31/541 , A61K31/538 , C07D491/107 , C07D519/00 , A61K31/5355 , A61K45/06
CPC classification number: C07D471/04 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K45/06 , C07D491/107 , C07D498/08 , C07D498/10 , C07D519/00
Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
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2.发明申请
公开(公告)号：US20160060262A1
公开(公告)日：2016-03-03
申请号：US14928973
申请日：2015-10-30
Applicant: Genentech, Inc.
Inventor： Joseph P. Lyssikatos , Lewis J. Gazzard , Emily Hanan , Samuel S. Kintz , Hans Edward Purkey
IPC: C07D471/04 , C07D417/04 , C07D401/14 , C07D405/12 , C07D413/12 , C07D217/22 , C07D401/12
CPC classification number: C07D471/04 , A61K31/47 , A61K31/4725 , C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/04
Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
Abstract translation: 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。
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公开(公告)号：US20220389020A1
公开(公告)日：2022-12-08
申请号：US17648045
申请日：2022-01-14
Applicant: Genentech, Inc.
Inventor： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark E. Zak , Aihe Zhou , Bing-Yan Zhu , Christopher Hurley
IPC: C07D487/04 , A61P17/06 , A61P35/02 , A61K31/519 , A61P29/00
Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
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公开(公告)号：US20180327420A1
公开(公告)日：2018-11-15
申请号：US16044862
申请日：2018-07-25
Applicant: Genentech, Inc.
Inventor： Marie-Gabrielle Braun , Keira Garland , Emily Hanan , Hans Purkey , Steven T. Staben , Robert Andrew Heald , Jamie Knight , Calum Macleod , Aijun Lu , Guosheng Wu , Siew Kuen Yeap
IPC: C07D498/04 , C07D519/00 , C07D498/06 , A61K31/5365 , A61K31/4188 , A61K31/498 , A61K31/4196 , C07D491/044 , A61K31/428 , A61K31/4439 , A61K31/5383 , A61K31/553 , A61K45/06 , A61K31/423
CPC classification number: C07D498/04 , A61K31/4188 , A61K31/4196 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/498 , A61K31/5365 , A61K31/5383 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/06 , C07D519/00
Abstract: Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US20170210733A1
公开(公告)日：2017-07-27
申请号：US15481764
申请日：2017-04-07
Applicant: Genentech, Inc.
Inventor： Marie-Gabrielle Braun , Emily Hanan , Steven T. Staben , Robert Andrew Heald , Calum MacLeod , Richard Elliott
IPC: C07D413/14 , C07D267/08
CPC classification number: C07D413/14 , A61K31/553 , C07D267/08 , C07D498/04
Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.
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公开(公告)号：US09643980B2
公开(公告)日：2017-05-09
申请号：US15200307
申请日：2016-07-01
Applicant: Genentech, Inc.
Inventor： Marie-Gabrielle Braun , Emily Hanan , Steven T. Staben , Robert Andrew Heald , Calum MacLeod , Richard Elliott
IPC: A61K31/553 , C07D498/04 , C07D498/14 , C07D519/00 , A61K45/06
CPC classification number: C07D498/04 , A61K31/553 , A61K45/06
Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US10435414B2
公开(公告)日：2019-10-08
申请号：US16044862
申请日：2018-07-25
Applicant: Genentech, Inc.
Inventor： Marie-Gabrielle Braun , Keira Garland , Emily Hanan , Hans Purkey , Steven T. Staben , Robert Andrew Heald , Jamie Knight , Calum Macleod , Aijun Lu , Guosheng Wu , Siew Kuen Yeap
IPC: A61K31/4188 , A61K31/424 , A61K31/498 , A61K31/5365 , A61K45/06 , C07D498/04 , C07D498/06 , C07D519/00 , A61K31/4196 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/5383 , A61K31/553 , C07D491/044
Abstract: Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
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公开(公告)号：US20170283424A1
公开(公告)日：2017-10-05
申请号：US15627847
申请日：2017-06-20
Applicant: Genentech, Inc.
Inventor： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark E. Zak , Aihe Zhou , Bing-Yan Zhu , Christopher Hurley
IPC: C07D487/04
CPC classification number: C07D487/04 , A61K31/519 , A61P17/06 , A61P29/00 , A61P35/02
Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
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公开(公告)号：US20140107099A1
公开(公告)日：2014-04-17
申请号：US14134150
申请日：2013-12-19
Applicant: Genentech, Inc.
Inventor： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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10.发明申请
公开(公告)号：US20140088076A1
公开(公告)日：2014-03-27
申请号：US14068774
申请日：2013-10-31
Applicant: Genentech, Inc.
Inventor： Joseph P. Lyssikatos , Lewis J. Gazzard , Emily Hanan , Samuel S. Kintz , Hans Edward Purkey
IPC: C07D471/04 , C07D417/04 , C07D405/14 , C07D401/12 , C07D405/12 , C07D413/12 , C07D217/22 , C07D401/04
CPC classification number: C07D471/04 , A61K31/47 , A61K31/4725 , C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/04
Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
Abstract translation: 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。
