公开(公告)号：US11254649B2

公开(公告)日：2022-02-22

申请号：US16746161

申请日：2020-01-17

申请人： Exelixis, Inc.

发明人： Adrian St. Clair Brown

IPC分类号： C07D401/04 ,  A61P35/02

摘要： This disclosure relates to the crystalline fumarate salt of (S)[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone. The disclosure also relates to pharmaceutical compositions comprising the crystalline fumarate salt of (S)[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone. The disclosure also relates to methods of treating cancers comprising administering to a patient in need thereof the crystalline fumarate salt of (S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone.

公开(公告)号：US20220033357A1

公开(公告)日：2022-02-03

申请号：US17505275

申请日：2021-10-19

申请人： Exelixis, Inc.

发明人： Adrian St. Clair Brown ,  Peter Lamb ,  William P. Gallagher

IPC分类号： C07D215/22 ,  C07D215/233

摘要： Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclo-propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.

公开(公告)号：US20220000857A1

公开(公告)日：2022-01-06

申请号：US17468103

申请日：2021-09-07

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Gisela Schwab ,  Colin Hessel ,  Christian Scheffold ,  Steven Lacy ,  Dale Miles ,  Alan Arroyo ,  Mark Dean

IPC分类号： A61K31/47 ,  A61K31/16 ,  A61P35/00 ,  A61K9/20 ,  A61K9/28

摘要： The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.

公开(公告)号：US11141413B2

公开(公告)日：2021-10-12

申请号：US16093426

申请日：2017-04-17

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Gisela Schwab ,  Colin Hessel ,  Christian Scheffold ,  Steven Lacy ,  Dale Miles ,  Alan Arroyo ,  Mark Dean

IPC分类号： A61K31/47 ,  A61K31/16 ,  A61P35/00 ,  A61K9/20 ,  A61K9/28

摘要： The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.

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.

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.

公开(公告)号：US11065240B2

公开(公告)日：2021-07-20

申请号：US15501582

申请日：2015-08-05

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Peter Lamb

IPC分类号： A61K31/47 ,  A61K38/05 ,  A61K31/194 ,  A61K31/69 ,  A61K31/4965

摘要： This invention relates to the combination of a C-Met inhibitor and a proteasome inhibitor to treat cancer, particularly multiple myeloma.

公开(公告)号：US20210155692A1

公开(公告)日：2021-05-27

申请号：US17048549

申请日：2019-04-18

申请人： EXELIXIS, INC.

发明人： Lucas BAILEY ,  Qufei LI ,  Malgorzata Agnieszka NOCULA-LUGOWSKA ,  Bryan GLASER

IPC分类号： C07K16/28 ,  C07K16/46 ,  A61P35/00 ,  A61K45/06

摘要： Anti-ROR antibody constructs, pharmaceutical compositions comprising the constructs, and methods of use thereof are presented.

公开(公告)号：US20210154185A1

公开(公告)日：2021-05-27

申请号：US17152394

申请日：2021-01-19

申请人： Exelixis, Inc.

发明人： Jo Ann Wilson ,  Khalid Shah

IPC分类号： A61K31/47 ,  C07D215/233

摘要： The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.