公开(公告)号：US20220370436A1

公开(公告)日：2022-11-24

申请号：US17869427

申请日：2022-07-20

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：US20220315579A1

公开(公告)日：2022-10-06

申请号：US17033475

申请日：2020-09-25

Applicant: Exelixis, Inc.

Inventor： Lynne Bannen ,  Minna Bui ,  Faming Jiang ,  Jack Maung ,  Andrew Raub ,  Justin Salvant ,  Benjamin Spangler ,  Kin Tso ,  Yong Wang ,  Wei Xu

IPC: C07D471/04

Abstract: 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.

公开(公告)号：US20220089541A1

公开(公告)日：2022-03-24

申请号：US17425661

申请日：2020-01-24

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Faming Jiang ,  Kin Tso ,  Xu Wei

IPC: C07D215/22 ,  C07D215/48 ,  C07D401/12 ,  C07D471/04 ,  A61P35/00

Abstract: The present invention relates to compounds that modulate cellular activities such as proliferation, differentiation, programmed cell death, migration, and chemoinvasion, by modulating protein kinase enzymatic activity, and compositions thereof, and methods of using such compounds.

公开(公告)号：US20220056138A1

公开(公告)日：2022-02-24

申请号：US17519327

申请日：2021-11-04

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Christian Scheffold ,  Colin Hessel

IPC: C07K16/28 ,  A61P35/04 ,  A61K31/47 ,  A61K39/395 ,  A61K45/06

Abstract: This invention relates to the combination of cabozantinib and atezolizumab to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma.

公开(公告)号：US11098015B2

公开(公告)日：2021-08-24

申请号：US17171752

申请日：2021-02-09

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-fluorophenyl)cyclopropane-1, 1-dicarboxamide.

公开(公告)号：US20210139430A1

公开(公告)日：2021-05-13

申请号：US17149365

申请日：2021-01-14

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：US10851061B2

公开(公告)日：2020-12-01

申请号：US16671834

申请日：2019-11-01

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Nathan Guz ,  Stephen Lau ,  Noel Hamill ,  Tracy Walker ,  Jana Galbraith ,  Simon Yau ,  Khalid Shah

IPC: C07D215/233 ,  C07D215/22

Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), 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 thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

公开(公告)号：US10793541B2

公开(公告)日：2020-10-06

申请号：US16271215

申请日：2019-02-08

Applicant: Exelixis, Inc. ,  Genentech, Inc.

Inventor： Sriram Naganathan ,  Nathan Guz ,  Matthew Pfeiffer ,  C. Gregory Sowell ,  Tracy Bostick ,  Jason Yang ,  Amit Srivastava ,  Neel Kumar Anand

IPC: C07D471/04 ,  C07D401/04 ,  C07D498/04

Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.

公开(公告)号：US10328069B2

公开(公告)日：2019-06-25

申请号：US15600147

申请日：2017-05-19

Applicant: Exelixis, Inc. ,  Sanofi

Inventor： Arthur DeCillis ,  Joanne Lager

IPC: A61K31/498 ,  A61K31/47 ,  C07D241/44 ,  C07D215/233

Abstract: Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein.

公开(公告)号：US20190030021A1

公开(公告)日：2019-01-31

申请号：US16151653

申请日：2018-10-04

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, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.