公开(公告)号：US12227481B2

公开(公告)日：2025-02-18

申请号：US18344267

申请日：2023-06-29

Applicant: Exelixis, Inc.

Inventor： Khalid Shah

IPC: C07D215/22

Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).

公开(公告)号：US12195475B2

公开(公告)日：2025-01-14

申请号：US18334113

申请日：2023-06-13

Applicant: Exelixis, Inc.

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

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

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：US12128039B2

公开(公告)日：2024-10-29

申请号：US18436836

申请日：2024-02-08

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  C07D215/233

CPC classification number: 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.

公开(公告)号：US20240189298A1

公开(公告)日：2024-06-13

申请号：US18436836

申请日：2024-02-08

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Khalid Shah

IPC: A61K31/47 ,  C07D215/233

CPC classification number: 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.

公开(公告)号：US11969419B2

公开(公告)日：2024-04-30

申请号：US18112214

申请日：2023-02-21

Applicant: Exelixis, Inc.

Inventor： David Smith ,  Maha Hussain

IPC: A61K31/47 ,  A61K31/00 ,  A61K31/517 ,  C07C55/02 ,  C07D215/22

CPC classification number: A61K31/47 ,  A61K31/00 ,  A61K31/517 ,  C07C55/02 ,  C07D215/22

Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

公开(公告)号：US20230314440A1

公开(公告)日：2023-10-05

申请号：US18022209

申请日：2021-08-20

Applicant: Exelixis, Inc.

Inventor： Christopher Del Nagro ,  Jason Wall ,  Evelyn Wang ,  Chih-Jian Lih

IPC: G01N33/574

CPC classification number: G01N33/57492 ,  G01N2800/52

Abstract: This invention is directed to the treatment of cancer, particularly solid tumors, using cabozantinib in combination with an immune checkpoint inhibitor or an anti-cancer vaccine and in predicting responses to such cancer treatments.

公开(公告)号：US11708367B2

公开(公告)日：2023-07-25

申请号：US16964228

申请日：2019-01-25

Applicant: Exelixis, Inc.

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

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

CPC classification number: C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

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：US11597699B2

公开(公告)日：2023-03-07

申请号：US16853043

申请日：2020-04-20

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D205/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/04 ,  C07D409/12

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20230045783A9

公开(公告)日：2023-02-09

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：US11564915B2

公开(公告)日：2023-01-31

申请号：US14782537

申请日：2014-04-04

Applicant: Exelixis, Inc.

Inventor： Aaron Weitzman

IPC: A61K31/47 ,  A61K9/20 ,  A61K9/00 ,  A61K9/28 ,  A61K31/194

Abstract: This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.