公开(公告)号：US11504363B2

公开(公告)日：2022-11-22

申请号：US16787212

申请日：2020-02-11

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Dana T. Aftab

IPC: A61K31/47 ,  A61P35/04 ,  A61P35/00 ,  A61P19/00 ,  C07D215/233 ,  A61K31/536

Abstract: This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.

公开(公告)号：US20220194902A1

公开(公告)日：2022-06-23

申请号：US17466328

申请日：2021-09-03

Applicant: Exelixis, Inc.

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

IPC: C07D215/233 ,  C07D215/22

Abstract: 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：US20220056010A1

公开(公告)日：2022-02-24

申请号：US17521396

申请日：2021-11-08

Applicant: Exelixis, Inc.

Inventor： Adrian St. Clair Brown

IPC: C07D401/04 ,  A61P35/02

Abstract: 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]methamine. 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：US11254649B2

公开(公告)日：2022-02-22

申请号：US16746161

申请日：2020-01-17

Applicant: Exelixis, Inc.

Inventor： Adrian St. Clair Brown

IPC: C07D401/04 ,  A61P35/02

Abstract: 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

Applicant: Exelixis, Inc.

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

IPC: C07D215/22 ,  C07D215/233

Abstract: 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

Applicant: Exelixis, Inc.

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

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

Abstract: 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

Applicant: Exelixis, Inc.

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

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

Abstract: 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

Applicant: Exelixis, Inc.

Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

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

Abstract: 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

Applicant: Exelixis, Inc.

Inventor： 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: 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

Abstract: 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

Applicant: Exelixis, Inc.

Inventor： 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: 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

Abstract: 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.