公开(公告)号：US20160082019A1

公开(公告)日：2016-03-24

申请号：US14782493

申请日：2014-04-04

Applicant: EXELIXIS, INC.

Inventor： Christopher J. Sweeney ,  Phili W. Kantoff

IPC: A61K31/58 ,  A61K31/573 ,  A61K31/47

CPC classification number: A61K31/58 ,  A61K9/2054 ,  A61K31/47 ,  A61K31/517 ,  A61K31/573 ,  A61K31/575 ,  A61K2300/00

Abstract: This invention relates to the combination of cabozantinib and abiraterone to treat cancer, particularly castration resistant prostate cancer.

Abstract translation: 本发明涉及卡泊沙坦和阿比特龙联合治疗癌症，特别是抗阉割前列腺癌。

公开(公告)号：US20160051532A1

公开(公告)日：2016-02-25

申请号：US14933801

申请日：2015-11-05

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Frauke Schimmoller

IPC: A61K31/47

CPC classification number: A61K31/47

Abstract: This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.

公开(公告)号：US20150202196A1

公开(公告)日：2015-07-23

申请号：US14518733

申请日：2014-10-20

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrison B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wei Xu ,  Diane Simeone

IPC: A61K31/47 ,  A61N5/10 ,  A61K31/7068

CPC classification number: A61K31/47 ,  A61K31/517 ,  A61K31/7068 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

Abstract: Disclosed are methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional treatments, wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl; R4 is (C1-C6)alkyl; and Q is CH or N.

Abstract translation: 公开了通过给予式I化合物或其药学上可接受的盐与吉西他滨（GEM）或其药学上可接受的盐以及任选的一种或多种另外的治疗组合治疗癌症的方法，其中：R1是卤素; R2是卤素; R3是（C1-C6）烷基; R4是（C1-C6）烷基; Q为CH或N.

公开(公告)号：US20250017916A1

公开(公告)日：2025-01-16

申请号：US18899774

申请日：2024-09-27

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：US20240316030A1

公开(公告)日：2024-09-26

申请号：US18733183

申请日：2024-06-04

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Dana T. Aftab

IPC: A61K31/47 ,  A61K31/536 ,  A61P19/00 ,  A61P35/00 ,  A61P35/04 ,  C07D215/233

CPC classification number: A61K31/47 ,  A61P19/00 ,  A61P35/00 ,  A61P35/04 ,  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：US20240300897A1

公开(公告)日：2024-09-12

申请号：US18657052

申请日：2024-05-07

Applicant: Exelixis, Inc.

Inventor： Frenel DeMorin ,  Khalid Shah ,  Sagar Shakya ,  Peter Wong ,  Courtney S. Johnson ,  Melanie Janelle Bevill ,  Stephan D. Parent

IPC: C07D215/48

CPC classification number: C07D215/48 ,  C07B2200/13

Abstract: The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.

公开(公告)号：US12084496B2

公开(公告)日：2024-09-10

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 ,  A61K39/00 ,  A61K45/06 ,  A61P35/00 ,  C07K16/46

CPC classification number: C07K16/2803 ,  A61K45/06 ,  A61P35/00 ,  C07K16/468 ,  A61K2039/505

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

公开(公告)号：US20240279181A1

公开(公告)日：2024-08-22

申请号：US18612538

申请日：2024-03-21

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)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：US20230382917A1

公开(公告)日：2023-11-30

申请号：US18323510

申请日：2023-05-25

Applicant: Exelixis, Inc.

Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

IPC: C07D487/04 ,  C07D513/14 ,  C07D487/14

CPC classification number: C07D487/04 ,  C07D513/14 ,  C07D487/14

Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.

公开(公告)号：US20230357391A1

公开(公告)日：2023-11-09

申请号：US18018860

申请日：2021-08-03

Applicant: EXELIXIS, INC.

Inventor： Bryan GLASER ,  Bonnie HAMMER ,  Seema KANTAK

IPC: C07K16/28 ,  C12N15/63 ,  A61K45/06

CPC classification number: C07K16/2803 ,  A61K45/06 ,  C12N15/63 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/92 ,  C07K2317/94

Abstract: The present disclosure provides CD47 binding agents (e.g., antibodies, including multispecific antibodies, such as bispecific antibodies) and uses thereof.