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Method of Treating Cancer

a cancer and melanoma technology, applied in the field of cancer treatment, can solve the problems of high mortality of ocular melanomas, historically considered ineffective chemotherapy for treating metastasized ocular melanoma, etc., and achieve the effects of reducing tumor invasiveness and metastasis, rapid initiation of endothelial cell apoptosis, and potent activity

Inactive Publication Date: 2012-10-04
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0020]Compound 1 is an orally bioavailable multitargeted tyrosine kinase inhibitor with potent activity against MET and VEGFR2. Compound 1 suppresses MET and VEGFR2 signaling, rapidly induces apoptosis of endothelial cells and tumor cells, and causes tumor regression in xenograft tumor models. Compound 1 also significantly reduces tumor invasiveness and metastasis and substantially improves overall survival in a murine pancreatic neuroendocrine tumor model. In a phase 1 clinical study, Compound 1 was generally well-tolerated, with fatigue, diarrhea, anorexia, rash, and palmar-plantar erythrodysesthesia being the most commonly observed adverse events.

Problems solved by technology

Once metastatic, ocular melanomas are highly fatal, and patients rarely live for more than a year after diagnosis.
Although surgery and / or radiation therapy may be effective for treating ocular melanoma that is localized to the area around the eye, chemotherapy historically has been considered ineffective for treating metastasized ocular melanoma.

Method used

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  • Method of Treating Cancer
  • Method of Treating Cancer
  • Method of Treating Cancer

Examples

Experimental program
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embodiments

[0039]In one embodiment the method employs a compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

[0040]R1 is halo;

[0041]R2 is halo;

[0042]R3 is (C1-C6)alkyl;

[0043]R4 is (C1-C6)alkyl; and

[0044]Q is CH or N.

[0045]In another embodiment, the compound of Formula I is a compound of Formula I(a)

or a pharmaceutically acceptable salt thereof, wherein:

[0046]R1 is halo;

[0047]R2 is halo; and

[0048]Q is CH or N.

[0049]In another embodiment of the method, the compound of Formula I is Compound 1:

or a pharmaceutically acceptable salt thereof. As indicated previously, Compound 1 is also known as N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. WO 2005 / 030140 describes the synthesis of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (Example 12, 37, 38, and 48) and also discloses the therapeutic activity of this molecule to inhibit, regulate and / or modulate the signal transd...

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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.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. provisional patent application Ser. No. 61 / 471,367, filed Apr. 4, 2011, which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]This invention is directed to the treatment of cancer, particularly uveal melanoma, with a dual inhibitor of MET and VEGF, such as a Compound of Formula I as disclosed herein.BACKGROUND OF THE INVENTION[0003]Uveal, or ocular, melanoma, which includes choroidal and iris melanomas, is the most common intraocular tumor found in adults. Tumors arise from the pigment cells, or melanocytes, that reside within the uvea that give color to the eye. Statistics indicate that up to 2000 individuals in the United States are diagnosed with ocular melanoma every year.[0004]Once metastatic, ocular melanomas are highly fatal, and patients rarely live for more than a year after diagnosis. Although surgery and / or radiation therapy may be effective for treatin...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/47A61P35/00
CPCA61K31/47A61P35/00A61P35/04
Inventor AFTAB, DANA T.SCHIMMOLLER, FRAUKE
Owner EXELIXIS INC
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