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Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases

A prostate cancer, osteogenic technology, applied in the field of osteogenic bone metastases and castration-resistant prostate cancer, can solve the problem of limited improvement of survival

Inactive Publication Date: 2013-11-13
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, improvements in survival remain limited and nearly all patients die from the disease, with a median survival of approximately 2 years

Method used

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  • Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
  • Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
  • Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases

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Experimental program
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Embodiment approach

[0067] In one embodiment, the compound of formula I is a compound of formula I(a):

[0068]

[0069] Formula Ia,

[0070] or a pharmaceutically acceptable salt thereof, wherein:

[0071] R 1 is a halo group;

[0072] R 2 is halo; and

[0073] R 3 is substituted by heterocycloalkyl (C 1 -C 6 )alkyl.

[0074] In another embodiment, the compound of formula I is compound 1.

[0075]

[0076] Compound 1

[0077] 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 further comprises a pharmaceutically acceptable carrier, excipient or diluent . In a specific embodiment, the compound of formula I is compound 1.

[0078] Compounds of Formula I, Formula Ia and Compound I as described herein include the recited compounds as well as individual isomers and mixtures of isomers. In each instance, compounds of formula I include p...

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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

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 61 / 386,975, filed September 27, 2010, which is incorporated herein by reference. field of invention [0003] The present invention relates to the treatment of cancer, particularly castration-resistant prostate cancer and osteogenic bone metastases, with dual inhibitors of MET and VEGF. Background of the invention [0004] Castration-resistant prostate cancer (CRPC) is a leading cause of cancer-related death in men. Despite advances in systemic therapy for CRPC, improvements in survival have remained limited, and nearly all patients succumb to the disease, with a median survival of approximately 2 years. The major cause of morbidity and mortality in CRPC is metastases to the bone, which occurs in approximately 90% of cases. [0005] Bone metastasis is a complex process involving interactions between cancer cells and components of the bone microenvironm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/00A61K31/5377A61K31/47A61P35/00A61P35/04
CPCA61K31/47A61K31/00A61K31/5377A61P35/00A61P35/04A61P43/00
Inventor D.史密斯M.侯赛因
Owner EXELIXIS INC
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