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公开(公告)号：US20150202196A1
公开(公告)日：2015-07-23
申请号：US14518733
申请日：2014-10-20
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Timothy Patrick Forsyth , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Yong Wang , Wei Xu , Diane Simeone
IPC分类号： A61K31/47 , A61N5/10 , A61K31/7068
CPC分类号： A61K31/47 , A61K31/517 , A61K31/7068 , A61K45/06 , A61N5/10 , A61K2300/00
摘要： Disclosed are methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional treatments, wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl; R4 is (C1-C6)alkyl; and Q is CH or N.
摘要翻译： 公开了通过给予式I化合物或其药学上可接受的盐与吉西他滨（GEM）或其药学上可接受的盐以及任选的一种或多种另外的治疗组合治疗癌症的方法，其中：R1是卤素; R2是卤素; R3是（C1-C6）烷基; R4是（C1-C6）烷基; Q为CH或N.
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公开(公告)号：US20150376133A1
公开(公告)日：2015-12-31
申请号：US14847801
申请日：2015-09-08
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/46 , A61K31/506 , A61K31/47 , C07D401/12 , A61K31/4709 , A61K31/505 , C07D239/94 , C07D413/12 , C07D417/12 , A61K31/5377 , A61K31/4725 , A61K31/501 , A61K31/496 , C07D401/14 , C07D413/14 , C07D405/14 , C12Q1/48 , C07D403/12
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译： 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节激酶受体，特别是c-Met，KDR，c-Kit，flt-3和flt-4，与细胞活性变化相关的信号转导途径的喹啉和喹啉 含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号：US20200331860A1
公开(公告)日：2020-10-22
申请号：US16921542
申请日：2020-07-06
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D215/22 , C07D295/15 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D239/88 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , C07D215/46 , C07D239/94 , C07D403/12 , C07D413/12 , C07D417/12 , C12Q1/48 , C07D215/36 , C07D215/38
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20160185725A1
公开(公告)日：2016-06-30
申请号：US15066872
申请日：2016-03-10
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , C07D239/88 , C12Q1/48 , C07D215/36 , C07D215/38 , C07D401/12 , C07D401/14
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20130252940A1
公开(公告)日：2013-09-26
申请号：US13888592
申请日：2013-05-07
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-ming Chan , Jeff Chen , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , C07D413/14 , C07D401/14 , C07D405/14 , C07D295/15 , C07D401/12
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译： 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号：US20170355678A1
公开(公告)日：2017-12-14
申请号：US15688310
申请日：2017-08-28
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , C07D239/94 , A61K31/4725 , C07D239/88 , C07D405/14 , A61K31/5377 , A61K31/505 , A61K31/517 , C07D295/15 , C07D413/12 , A61K31/506 , C07D401/12 , A61K31/501 , C07D413/14 , C07D215/46 , A61K31/47 , C12Q1/48 , A61K31/4709 , C07D403/12 , C07D215/22 , C07D215/36 , C07D417/12 , C07D215/38 , C07D401/14 , A61K31/496
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20140155378A9
公开(公告)日：2014-06-05
申请号：US13888592
申请日：2013-05-07
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-ming Chan , Jeff Chen , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , C07D413/14 , C07D401/14 , C07D405/14 , C07D295/15 , C07D401/12
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译： 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号：US11124482B2
公开(公告)日：2021-09-21
申请号：US15688310
申请日：2017-08-28
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/22 , C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D295/15 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D239/88 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , C07D215/46 , C07D239/94 , C07D403/12 , C07D413/12 , C07D417/12 , C12Q1/48 , C07D215/36 , C07D215/38
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20210253530A9
公开(公告)日：2021-08-19
申请号：US15688310
申请日：2017-08-28
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/233 , A61K31/496 , C07D239/94 , A61K31/4725 , C07D239/88 , C07D405/14 , A61K31/5377 , A61K31/505 , A61K31/517 , C07D295/15 , C07D413/12 , A61K31/506 , C07D401/12 , A61K31/501 , C07D413/14 , C07D215/46 , A61K31/47 , C12Q1/48 , A61K31/4709 , C07D403/12 , C07D215/22 , C07D215/36 , C07D417/12 , C07D215/38 , C07D401/14
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US20140155396A1
公开(公告)日：2014-06-05
申请号：US13928977
申请日：2013-06-27
申请人： Exelixis, Inc.
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： C07D215/22 , C07D401/12 , C07D239/88
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译： 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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