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Dual inhibitor of met and vegf for treating cancer

A technology for bone cancer and prostate cancer, applied in the field of castration-resistant prostate cancer and bone metastases, can solve problems such as limited survival improvement

Inactive Publication Date: 2014-11-19
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite advances in systemic therapy for CRPC, survival improvements have been limited, and virtually all patients die of the disease within ~2 years

Method used

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  • Dual inhibitor of met and vegf for treating cancer
  • Dual inhibitor of met and vegf for treating cancer
  • Dual inhibitor of met and vegf for treating cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0085] In one embodiment, the compound of formula I is a compound of formula Ia:

[0086]

[0087]Formula Ia

[0088] or a pharmaceutically acceptable salt thereof, wherein:

[0089] R 1 is a halo group;

[0090] R 2 is halo; and

[0091] Q is CH or N.

[0092] In another embodiment, the compound of formula I is compound 1:

[0093]

[0094] Compound 1

[0095] or a pharmaceutically acceptable salt thereof. As previously indicated, compound 1 is referred to herein as N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamide. WO2005 / 030140 discloses compound 1 and describes how it is prepared (Example 12, Example 37, Example 38 and Example 48) and also discloses the therapeutic activity of this compound to inhibit, modulate and / or modulate the signal transduction of kinases (assay , Table 4, entry 289). Example 48 is in paragraph [0353] of WO2005 / 030140.

[0096] In other embodiments, the compound of Formula I, Formu...

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Abstract

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

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority to US Provisional Application No. 61 / 557,358, filed November 8, 2011, the entire contents of which are incorporated herein by reference. field of invention [0003] The present invention relates to the treatment of cancer, in particular castration-resistant prostate cancer and bone metastases, with dual inhibitors of MET and VEGF. Background of the invention [0004] Castration-resistant prostate cancer (CRPC) is the leading cause of cancer-related death in men. Despite advances in systemic therapy for CRPC, survival improvements have been limited, and virtually all patients succumbed to the disease within about 2 years. The major cause of morbidity and mortality in CRPC is bone metastasis, which occurs in approximately 90% of cases. [0005] Bone metastasis is a complex process involving the interaction between cancer cells and components of the bone microenvironment, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K31/517A61P35/00A61K35/04
CPCA61K31/517A61K31/47A61P13/08A61P19/08A61P35/00A61P35/04
Inventor D.T.阿夫塔布F.施莫尔勒
Owner EXELIXIS INC
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