公开(公告)号：US20230301978A1

公开(公告)日：2023-09-28

申请号：US17975765

申请日：2022-10-28

Applicant: Exelixis, Inc.

Inventor： Khalid Shah ,  Gisela Schwab ,  Steven Lacy

IPC: A61K31/47 ,  A61P35/00 ,  A61K9/00

CPC classification number: A61K31/47 ,  A61P35/00 ,  A61K9/0053

Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.

公开(公告)号：US11673897B2

公开(公告)日：2023-06-13

申请号：US16964274

申请日：2019-01-25

Applicant: Exelixis, Inc.

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

IPC: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D491/147 ,  C07D471/04

CPC classification number: C07D491/147 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

Abstract: 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：US20230149384A1

公开(公告)日：2023-05-18

申请号：US17965529

申请日：2022-10-13

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Dana T. Aftab

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

CPC classification number: 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：US11433064B2

公开(公告)日：2022-09-06

申请号：US16919562

申请日：2020-07-02

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Thomas Mueller ,  Aaron Weitzman ,  Jaymes Holland

IPC: A61K51/00 ,  A61M36/14 ,  A61K31/47 ,  A61K31/4706 ,  A61K41/00 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4188 ,  A61N5/10 ,  A61K31/015 ,  A61P43/00 ,  A61K31/517 ,  A61P35/00 ,  C07D215/22

Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.

公开(公告)号：US20220259151A9

公开(公告)日：2022-08-18

申请号：US17371372

申请日：2021-07-09

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)cyclopropane-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-ffuorophenyl)cyclopropane-1,1-dicarboxamide.

公开(公告)号：US20220087999A1

公开(公告)日：2022-03-24

申请号：US17538310

申请日：2021-11-30

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  A61K9/20 ,  A61K45/06 ,  A61K9/28

Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.

公开(公告)号：US20220031688A1

公开(公告)日：2022-02-03

申请号：US17505307

申请日：2021-10-19

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  A61K9/28 ,  A61K9/20 ,  A61K45/06

Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.

公开(公告)号：US11124481B2

公开(公告)日：2021-09-21

申请号：US15500312

申请日：2015-07-31

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-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.

公开(公告)号：US11123338B2

公开(公告)日：2021-09-21

申请号：US16722563

申请日：2019-12-20

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  A61K9/20 ,  A61K9/28 ,  A61K45/06

Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.

公开(公告)号：US20210161885A1

公开(公告)日：2021-06-03

申请号：US17170275

申请日：2021-02-08

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  C07D215/233

Abstract: 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.