公开(公告)号：US11708367B2

公开(公告)日：2023-07-25

申请号：US16964228

申请日：2019-01-25

申请人： Exelixis, Inc.

发明人： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Yong Wang ,  Wei Xu

IPC分类号： C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

CPC分类号： C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

摘要： Disclosed herein are compounds of Formula (I′). Compounds of Formula (I′) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer 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.

公开(公告)号：US20220315579A1

公开(公告)日：2022-10-06

申请号：US17033475

申请日：2020-09-25

申请人： Exelixis, Inc.

发明人： Lynne Bannen ,  Minna Bui ,  Faming Jiang ,  Jack Maung ,  Andrew Raub ,  Justin Salvant ,  Benjamin Spangler ,  Kin Tso ,  Yong Wang ,  Wei Xu

IPC分类号： C07D471/04

摘要： The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.

公开(公告)号：US10159666B2

公开(公告)日：2018-12-25

申请号：US15126767

申请日：2015-03-17

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy

IPC分类号： A61K31/47 ,  A61K9/20 ,  A61K9/00

摘要： The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.

公开(公告)号：US20170087143A1

公开(公告)日：2017-03-30

申请号：US15126767

申请日：2015-03-17

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy

IPC分类号： A61K31/47 ,  A61K9/00

CPC分类号： A61K31/47 ,  A61K9/0053 ,  A61K9/2054

摘要： The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.

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.

公开(公告)号：US11718622B2

公开(公告)日：2023-08-08

申请号：US17201380

申请日：2021-03-15

申请人： Exelixis, Inc.

发明人： Sunghoon Ma ,  Yong Wang ,  Wei Xu

IPC分类号： C07D487/04 ,  C07D487/14 ,  C07D513/14 ,  A61K31/4985 ,  A61K31/519 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D513/14

摘要： Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.

公开(公告)号：US20230043835A1

公开(公告)日：2023-02-09

申请号：US17616120

申请日：2020-06-03

申请人： Exelixis, Inc.

发明人： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Kin Tso ,  Yong Wang ,  Wei Xu

IPC分类号： C07D215/233 ,  C07D401/04 ,  C07D407/04 ,  C07D401/14 ,  C07D417/04 ,  C07D413/04 ,  C07D471/04

摘要： Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Ax1 and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.

公开(公告)号：US20220194902A1

公开(公告)日：2022-06-23

申请号：US17466328

申请日：2021-09-03

申请人： Exelixis, Inc.

发明人： Wei Xu ,  David J. Donnelly ,  Patrick L. Chow ,  Benjamin J. Henley

IPC分类号： C07D215/233 ,  C07D215/22

摘要： The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-di-methoxy-quinolin-4-vloxy)-phenyl]amide (4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.

公开(公告)号：US20210292332A1

公开(公告)日：2021-09-23

申请号：US17201380

申请日：2021-03-15

申请人： Exelixis, Inc.

发明人： Sunghoon Ma ,  Yong Wang ,  Wei Xu

IPC分类号： C07D487/04 ,  C07D487/14 ,  C07D513/14

摘要： Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.

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.