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公开(公告)号：US20200002353A1
公开(公告)日：2020-01-02
申请号：US16565041
申请日：2019-09-09
Applicant: Genentech, Inc.
Inventor： Sharada Labadie , Jun Li , Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Jason Zbieg , Birong Zhang , Nicholas Charles Ray , Simon Goodacre , Jiangpeng Liao
IPC: C07D495/04 , C07D491/048 , A61K31/4355 , A61K45/06 , A61K31/4365 , C07D487/04 , A61K31/55 , A61K31/4985 , C07D471/04 , A61K31/437 , C07D471/14 , A61K31/4375 , A61K31/695 , C07F7/18
Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and 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, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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![TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF](/abs-image/US/2019/05/23/US20190152970A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190152970A1
公开(公告)日：2019-05-23
申请号：US16250879
申请日：2019-01-17
Applicant: Genentech, Inc.
Inventor： Sharada LABADIE , Jun Li , Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Jason Zbieg , Birong Zhang , Nicholas Charles Ray , Simon Goodacre , Zhiguo Liu , Tao Wang
IPC: C07D471/04 , A61K31/437 , A61K45/06
Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号：US20180002344A1
公开(公告)日：2018-01-04
申请号：US15623904
申请日：2017-06-15
Applicant: Genentech, Inc.
Inventor： Sharada Labadie , Jun Li , Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Jason Zbieg , Birong Zhang , Nicholas Charles Ray , Simon Goodacre , Jiangpeng Liao
IPC: C07D495/04 , C07D491/048 , C07D487/04 , C07D471/14 , C07D471/04 , A61K31/695 , A61K31/4355 , A61K31/55 , A61K31/4985 , A61K31/4375 , A61K31/437 , A61K31/4365 , C07F7/18 , A61K45/06
CPC classification number: C07D495/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4985 , A61K31/55 , A61K31/695 , A61K45/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/048 , C07F7/1804
Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and 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, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号：US09546164B2
公开(公告)日：2017-01-17
申请号：US14603273
申请日：2015-01-22
Applicant: GENENTECH, INC. , XENON PHARMACEUTICALS INC.
Inventor： Jean-Christophe Andrez , Paul Robert Bichler , Chien-An Chen , Sultan Chowdhury , Shannon Marie Decker , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Jun Li , Zhiguo Liu , Daniel F. Ortwine , Brian Safina , Daniel Sutherlin , Tao Sheng , Shaoyi Sun , Andrew D. White , Michael Scott Wilson , Alla Yurevna Zenova , Jiuxiang Zhu
IPC: C07D211/32 , C07D211/54 , C07D233/68 , C07D453/02 , A61K31/337 , A61K31/397 , A61K31/4015 , A61K31/415 , A61K31/4412 , A61K31/495 , C07D237/08 , C07D241/04 , C07D205/04 , C07D207/12 , C07D211/42 , C07D305/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D403/04 , C07D487/08 , C07D265/30 , C07D211/60
CPC classification number: A61K31/445 , A61K31/337 , A61K31/397 , A61K31/4015 , A61K31/415 , A61K31/4412 , A61K31/4523 , A61K31/4545 , A61K31/495 , C07D205/04 , C07D207/12 , C07D211/22 , C07D211/32 , C07D211/42 , C07D211/54 , C07D211/60 , C07D233/68 , C07D237/08 , C07D241/04 , C07D265/30 , C07D305/08 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D453/02 , C07D487/08 , C07F7/0812
Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Abstract translation: 本发明提供具有通式I的化合物及其药学上可接受的盐，其中变量RA，RAA，下标n，环A，X2，L，下标m，X1，R1，R2，R3，R4，R5和RN 具有本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。
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Patent Agency Ranking
15.发明申请公开(公告)号：US20140349996A1
公开(公告)日：2014-11-27
申请号：US14456670
申请日：2014-08-11
Applicant: Array BioPharma Inc. , Genentech, Inc.
Inventor： Ian S. Mitchell , James F. Blake , Rui Xu , Nicholas C. Kallan , Dengming Xiao , Keith Lee Spencer , Josef R. Bencsik , Eli M. Wallace , Stephen T. Schlacter , Anna L. Banka , Jun Liang , Brian Safina , Jun Li , Christine Chabot
IPC: C07D409/14 , A61K31/517 , A61K45/06 , C07D239/70 , C07D409/12 , C07D401/14 , C07D403/12 , C07D405/12 , A61K31/5377 , C07D403/04 , C07D403/14
CPC classification number: C07D409/14 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12
Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US09694002B2
公开(公告)日：2017-07-04
申请号：US15275131
申请日：2016-09-23
Applicant: GENENTECH, INC. , XENON PHARMACEUTICALS INC.
Inventor： Jean-Christophe Andrez , Paul Robert Bichler , Chien-An Chen , Sultan Chowdhury , Shannon Marie Decker , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Jun Li , Zhiguo Liu , Daniel F. Ortwine , Brian Safina , Daniel Sutherlin , Tao Sheng , Shaoyi Sun , Andrew D. White , Michael Scott Wilson , Alla Yurevna Zenova , Jiuxiang Zhu
IPC: C07D211/32 , C07D211/54 , C07D233/68 , A61K31/445 , A61K31/4545 , A61K31/4523
CPC classification number: A61K31/445 , A61K31/337 , A61K31/397 , A61K31/4015 , A61K31/415 , A61K31/4412 , A61K31/4523 , A61K31/4545 , A61K31/495 , C07D205/04 , C07D207/12 , C07D211/22 , C07D211/32 , C07D211/42 , C07D211/54 , C07D211/60 , C07D233/68 , C07D237/08 , C07D241/04 , C07D265/30 , C07D305/08 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D453/02 , C07D487/08 , C07F7/0812
Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
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![TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF](/abs-image/US/2025/04/10/US20250114338A1/abs.jpg.150x150.jpg)
公开(公告)号：US20250114338A1
公开(公告)日：2025-04-10
申请号：US18985513
申请日：2024-12-18
Applicant: Genentech, Inc.
Inventor： Sharada Labadie , Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Jason Zbieg , Birong Zhang , Simon Charles Goodacre , Nicholas Charles Ray , Jun Li
IPC: C07D471/04 , A61K31/437 , A61K31/4545 , A61K45/06
Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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![Tetrahydro-pyrido[3,4-b]indole estrogen receptor modulators and uses thereof](/abs-image/US/2018/05/29/US09980947B2/abs.jpg.150x150.jpg)
公开(公告)号：US09980947B2
公开(公告)日：2018-05-29
申请号：US14972326
申请日：2015-12-17
Applicant: Genentech, Inc.
Inventor： Sharada Labadie , Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Jason Zbieg , Birong Zhang , Simon Charles Goodacre , Nicholas Charles Ray , Jun Li
IPC: C07D471/04 , A61K31/437 , A61K31/4545 , A61K31/138 , A61K31/497 , A61K31/506 , A61K31/565 , A61K45/06
CPC classification number: A61K31/437 , A61K31/138 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/565 , A61K45/06 , C07D471/04
Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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公开(公告)号：US20130317001A1
公开(公告)日：2013-11-28
申请号：US13899526
申请日：2013-05-21
Applicant: XENON PHARMACEUTICALS INC. , GENENTECH, INC.
Inventor： Jean-Christophe Andrez , Sultan Chowdhury , Shannon Marie Decker , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Jun Li , Daniel F. Ortwine , Brian Safina , Tao Sheng , Shaoyi Sun , Daniel P. Sutherlin , Michael Scott Wilson , Alla Yurevna Zenova
IPC: C07D403/12 , C07D213/64 , C07D205/04 , C07D311/58 , C07D295/26 , C07D233/84 , C07D257/04 , C07C311/51 , C07C307/06 , C07D213/82 , C07D265/30
CPC classification number: C07D491/107 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/44 , A61K31/5375 , C07B2200/05 , C07C307/06 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/18 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50 , C07C2603/66 , C07C2603/68 , C07C2603/74 , C07D205/04 , C07D207/46 , C07D207/48 , C07D209/52 , C07D211/22 , C07D211/96 , C07D213/64 , C07D213/82 , C07D233/84 , C07D257/04 , C07D265/30 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/18 , C07D309/08 , C07D311/58 , C07D311/70 , C07D311/72 , C07D403/12 , C07D405/12 , C07D413/12 , C07D451/02 , C07D471/08
Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
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