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Method of Treating Cancer

a cancer and treatment method technology, applied in the field of cancer treatment, can solve the problems of abnormal deposition of unstructured bone, morbidity and mortality in crpc, modest improvement in survival, etc., and achieve the effect of prolonging the overall survival of patients

Inactive Publication Date: 2014-02-27
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a new treatment for bone pain caused by metastatic bone lesions associated with CRPC (a type of prostate cancer). The treatment involves using a pharmaceutical composition containing a compound called Compound of Formula I or its malate salt. The patent also mentions that this treatment can help extend the overall survival of patients with CRPC.

Problems solved by technology

Despite progress in systemic therapy for CRPC, improvements in survival are modest, and virtually all patients succumb to this disease within about 2 years.
The primary cause of morbidity and mortality in CRPC is metastasis to the bone, which occurs in about 90% of cases.
Although most CRPC patients with bone metastases display features of both types of lesions, prostate cancer bone metastases are often osteoblastic, with abnormal deposition of unstructured bone accompanied by increased skeletal fractures, spinal cord compression, and severe bone pain.

Method used

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  • Method of Treating Cancer
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Examples

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embodiments

[0048]In one embodiment the compound of Formula I is the compound of Formula Ia:

or a pharmaceutically acceptable salt thereof, wherein:

[0049]R1 is halo;

[0050]R2 is halo; and

[0051]Q is CH or N.

[0052]In another embodiment, the compound of Formula I is Compound 1:

or a pharmaceutically acceptable salt thereof. As indicated previously, 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. WO 2005 / 030140 discloses Compound 1 and describes how it is made (Example 12, 37, 38, and 48) and also discloses the therapeutic activity of this compound to inhibit, regulate and / or modulate the signal transduction of kinases, (Assays, Table 4, entry 289). Example 48 is on paragraph [0353] in WO 2005 / 030140.

[0053]In other embodiments, the compound of Formula I, Ia, or Compound 1, or a pharmaceutically acceptable salt thereof, is administered as a pharmaceutical composition, wherein the pharmaceutical composition additio...

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Abstract

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

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of priority to U.S. Provisional Application No. 61 / 386,959, filed Sep. 27, 2010, and U.S. Provisional Application No. 61 / 481,671, filed May 2, 2011, which is incorporated herein by reference.FIELD OF THE INVENTION[0002]This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.BACKGROUND OF THE INVENTION[0003]Castration-Resistant Prostate Cancer (CRPC) is a leading cause of cancer-related death in men. Despite progress in systemic therapy for CRPC, improvements in survival are modest, and virtually all patients succumb to this disease within about 2 years. The primary cause of morbidity and mortality in CRPC is metastasis to the bone, which occurs in about 90% of cases.[0004]Metastasis to the bone is a complex process that involves interactions between cancer cells and components of the ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07D215/22C07C55/02
CPCC07C55/02C07D215/22A61K31/00A61K31/517A61K31/47A61P13/08A61P19/00A61P35/00A61P35/04A61P43/00
Inventor SMITH, DAVID C.HUSSAIN, MAHA
Owner EXELIXIS INC
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