公开(公告)号：US11065240B2

公开(公告)日：2021-07-20

申请号：US15501582

申请日：2015-08-05

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Peter Lamb

IPC: A61K31/47 ,  A61K38/05 ,  A61K31/194 ,  A61K31/69 ,  A61K31/4965

Abstract: This invention relates to the combination of a C-Met inhibitor and a proteasome inhibitor to treat cancer, particularly multiple myeloma.

公开(公告)号：US20210155692A1

公开(公告)日：2021-05-27

申请号：US17048549

申请日：2019-04-18

Applicant: EXELIXIS, INC.

Inventor： Lucas BAILEY ,  Qufei LI ,  Malgorzata Agnieszka NOCULA-LUGOWSKA ,  Bryan GLASER

IPC: C07K16/28 ,  C07K16/46 ,  A61P35/00 ,  A61K45/06

Abstract: Anti-ROR antibody constructs, pharmaceutical compositions comprising the constructs, and methods of use thereof are presented.

公开(公告)号：US20210154185A1

公开(公告)日：2021-05-27

申请号：US17152394

申请日：2021-01-19

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.

公开(公告)号：US20200255398A1

公开(公告)日：2020-08-13

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：US20200255382A1

公开(公告)日：2020-08-13

申请号：US16787212

申请日：2020-02-11

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Dana T. Aftab

IPC: 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：US10736886B2

公开(公告)日：2020-08-11

申请号：US16251617

申请日：2019-01-18

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

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：US10590102B2

公开(公告)日：2020-03-17

申请号：US15852280

申请日：2017-12-22

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：US20190185447A1

公开(公告)日：2019-06-20

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: 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：US20180037552A1

公开(公告)日：2018-02-08

申请号：US15618593

申请日：2017-06-09

Applicant: Exelixis,Inc.

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

IPC: C07D215/22 ,  C07D215/233

CPC classification number: 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：US20170296529A1

公开(公告)日：2017-10-19

申请号：US15600147

申请日：2017-05-19

Applicant: Exelixis, Inc. ,  Sanofi

Inventor： Arthur DeCillis ,  Joanne Lager

IPC: A61K31/47 ,  C07D215/233

CPC classification number: A61K31/47 ,  A61K31/498 ,  C07D215/233 ,  C07D241/44

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.