公开(公告)号：US12128039B2

公开(公告)日：2024-10-29

申请号：US18436836

申请日：2024-02-08

申请人： Exelixis, Inc.

发明人： Jo Ann Wilson ,  Khalid Shah

IPC分类号： A61K31/47 ,  C07D215/233

CPC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.

公开(公告)号：US20240189298A1

公开(公告)日：2024-06-13

申请号：US18436836

申请日：2024-02-08

申请人： Exelixis, Inc.

发明人： Jo Ann Wilson ,  Khalid Shah

IPC分类号： A61K31/47 ,  C07D215/233

CPC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.

公开(公告)号：US11969419B2

公开(公告)日：2024-04-30

申请号：US18112214

申请日：2023-02-21

申请人： Exelixis, Inc.

发明人： David Smith ,  Maha Hussain

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

CPC分类号： A61K31/47 ,  A61K31/00 ,  A61K31/517 ,  C07C55/02 ,  C07D215/22

摘要： 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

申请人： Exelixis, Inc.

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

IPC分类号： G01N33/574

CPC分类号： G01N33/57492 ,  G01N2800/52

摘要： 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

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：US11597699B2

公开(公告)日：2023-03-07

申请号：US16853043

申请日：2020-04-20

申请人： Exelixis, Inc.

发明人： 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分类号： 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

摘要： 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

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：US11564915B2

公开(公告)日：2023-01-31

申请号：US14782537

申请日：2014-04-04

申请人： Exelixis, Inc.

发明人： Aaron Weitzman

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

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

公开(公告)号：US20220370436A1

公开(公告)日：2022-11-24

申请号：US17869427

申请日：2022-07-20

申请人： Exelixis, Inc.

发明人： Jo Ann Wilson ,  Khalid Shah

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

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

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.