公开(公告)号：US20200330451A1

公开(公告)日：2020-10-22

申请号：US16919562

申请日：2020-07-02

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Thomas Mueller ,  Aaron Weitzman ,  Jaymes Holland

IPC: A61K31/47 ,  A61K31/4706 ,  A61K41/00 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4188 ,  A61N5/10

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：US20190218182A1

公开(公告)日：2019-07-18

申请号：US16362863

申请日：2019-03-25

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy ,  Linh Nguyen

IPC: C07D215/22 ,  G01N33/487 ,  C07C233/60 ,  C07C305/24 ,  C07D215/60

CPC classification number: C07D215/22 ,  C07C233/60 ,  C07C305/24 ,  C07C2601/02 ,  C07D215/60 ,  G01N33/487 ,  G01N2570/00

Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

公开(公告)号：US20190151302A1

公开(公告)日：2019-05-23

申请号：US16251617

申请日：2019-01-18

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Thomas Mueller ,  Aaron Weitzman ,  Jaymes Holland

IPC: A61K31/47 ,  A61N5/10 ,  A61K31/4188 ,  A61K31/4706 ,  A61K45/06 ,  A61K41/00 ,  A61K31/495

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：US10166225B2

公开(公告)日：2019-01-01

申请号：US14346570

申请日：2012-09-20

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Douglas Clary

IPC: A61K31/47 ,  G01N33/68 ,  A61K9/20

Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.

公开(公告)号：US09861624B2

公开(公告)日：2018-01-09

申请号：US14398188

申请日：2013-05-02

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab

IPC: A61K31/47

CPC classification number: A61K31/47

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

公开(公告)号：US20170224672A1

公开(公告)日：2017-08-10

申请号：US15501582

申请日：2015-08-05

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Peter Lamb

IPC: A61K31/47 ,  A61K38/05

CPC classification number: A61K31/47 ,  A61K31/194 ,  A61K31/4965 ,  A61K31/69 ,  A61K38/05 ,  A61K2300/00

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：US20150238477A1

公开(公告)日：2015-08-27

申请号：US14426580

申请日：2013-09-09

Applicant: EXELIXIS, INC.

Inventor： Dana T. Aftab

IPC: A61K31/47 ,  C12Q1/68 ,  A61K45/06

CPC classification number: A61K31/47 ,  A61K9/2054 ,  A61K31/337 ,  A61K31/517 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  C07D215/22 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/57423 ,  G01N2800/52 ,  A61K2300/00

Abstract: This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及患者，特别是患有肺腺癌的患者，特别是患有KIF5B-RET融合阳性非小细胞肺癌的患者，其具有MET，VEGF和RET的抑制剂， 是式I的化合物或其药学上可接受的盐。

公开(公告)号：US11724986B2

公开(公告)日：2023-08-15

申请号：US17084312

申请日：2020-10-29

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

CPC classification number: C07D215/233 ,  C07D215/22 ,  C07B2200/13

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：US20230181559A1

公开(公告)日：2023-06-15

申请号：US17873918

申请日：2022-07-26

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Thomas Mueller ,  Aaron Weitzman ,  Jaymes Holland

IPC: A61K31/47 ,  A61K31/4706 ,  A61K41/00 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4188 ,  A61N5/10

CPC classification number: 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：US11504363B2

公开(公告)日：2022-11-22

申请号：US16787212

申请日：2020-02-11

Applicant: Exelixis, Inc.

Inventor： Gisela Schwab ,  Dana T. Aftab

IPC: A61K31/47 ,  A61P35/04 ,  A61P35/00 ,  A61P19/00 ,  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.