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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：US20140171407A1
公开(公告)日：2014-06-19
申请号：US14182190
申请日：2014-02-17
Applicant: Genentech, Inc.
Inventor： Hazel Joan Dyke , Lewis Gazzard , Karen Williams , Huifen Chen , Samuel Kintz , Joy Drobnick , Joseph P. Lyssikatos , Simon Goodacre , Calum Macleod , Charles Ellwood
IPC: C07D471/14 , A61K31/4375 , C07D453/02 , A61K45/06 , A61K31/4545 , A61K31/439 , A61K31/55 , A61K31/5377 , A61K31/496
CPC classification number: C07D471/14 , A61K31/4375 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D453/02 , C07D519/00
Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。
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公开(公告)号：US20150328195A1
公开(公告)日：2015-11-19
申请号：US14743835
申请日：2015-06-18
Applicant: GENENTECH, INC.
Inventor： Hazel Joan Dyke , Lewis Gazzard , Karen Williams , Huifen Chen , Samuel Kintz , Joy Drobnick , Joseph P. Lyssikatos , Simon Goodacre , Calum Macleod , Charles Ellwood
IPC: A61K31/4375 , C07D471/14 , A61K31/496 , A61K45/06 , C07D453/02 , C07D519/00 , A61K31/55 , A61K31/5377 , A61K31/439
CPC classification number: C07D471/14 , A61K31/4375 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D453/02 , C07D519/00
Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。
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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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Patent Agency Ranking
公开(公告)号：US09440976B2
公开(公告)日：2016-09-13
申请号：US14743835
申请日：2015-06-18
Applicant: Genentech, Inc.
Inventor： Hazel Joan Dyke , Lewis Gazzard , Karen Williams , Huifen Chen , Samuel Kintz , Joy Drobnick , Joseph P. Lyssikatos , Simon Goodacre , Calum Macleod , Charles Ellwood
IPC: C07D471/14 , C07D453/02 , A61K31/5377 , C07D519/00 , A61K31/4375 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/55 , A61K45/06
CPC classification number: C07D471/14 , A61K31/4375 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D453/02 , C07D519/00
Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。
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公开(公告)号：US20180065983A1
公开(公告)日：2018-03-08
申请号：US15258175
申请日：2016-09-07
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 , A61K31/553 , A61K31/5383 , A61K31/498 , A61K31/4439 , A61K31/428 , A61K31/423 , A61K31/4196 , C07D491/044 , A61K45/06 , C07D519/00
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：US10851091B2
公开(公告)日：2020-12-01
申请号：US16140392
申请日：2018-09-24
Applicant: Genentech, Inc.
Inventor： Marie-Gabrielle Braun , Emily Hanan , Steven T. Staben , Robert Andrew Heald , Calum Macleod , Richard Elliott
IPC: C07D413/14 , C07D267/08 , C07D498/04 , A61K31/553
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：US10065970B2
公开(公告)日：2018-09-04
申请号：US15258175
申请日：2016-09-07
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 , A61K31/553 , A61K31/5383 , A61K31/498 , A61K31/4439 , A61K31/428 , A61K31/423 , A61K31/4196 , C07D491/044 , A61K45/06 , C07D519/00
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：US20180162873A9
公开(公告)日：2018-06-14
申请号：US15258175
申请日：2016-09-07
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 , A61K31/553 , A61K31/5383 , A61K31/498 , A61K31/4439 , A61K31/428 , A61K31/423 , A61K31/4196 , C07D491/044 , A61K45/06 , C07D519/00
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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