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

A technology for castration resistance and prostate cancer, which is applied in the direction of anti-inflammatory agents, organic active ingredients, non-central analgesics, etc., and can solve the problem of limited improvement of survival period

Inactive Publication Date: 2013-11-13
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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
Comparison scheme
Effect test

Embodiment approach

[0164] In one embodiment, the compound of formula I is a compound of formula Ia:

[0165]

[0166] Formula Ia

[0167] or a pharmaceutically acceptable salt thereof, wherein:

[0168] R 1 is a halo group;

[0169] R 2 is a halo group;

[0170] R 3 Yes (C 1 -C 6 ) alkyl or (C optionally substituted by heterocycloalkyl 1 -C 6 ) alkyl; and

[0171] Q is CH or N.

[0172] In another embodiment, the compound of formula I is a compound of formula Ib:

[0173]

[0174] Formula Ib

[0175] or a pharmaceutically acceptable salt thereof, wherein:

[0176] R 1 is a halo group;

[0177] R 2 is halo; and

[0178] R 3 Yes (C 1 -C 6 ) alkyl or (C optionally substituted by heterocycloalkyl 1 -C 6 )alkyl.

[0179] In another embodiment, the compound of formula I is compound 1.

[0180]

[0181] Compound 1

[0182] In another embodiment, the compound of formula I is compound 2.

[0183]

[0184] Compound 2

[0185] In one embodiment, the compound of formula ...

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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 U.S. Provisional Application No. 61 / 386,971, filed September 27, 2010, U.S. Provisional Application No. 61 / 386,993, filed September 27, 2010, and U.S. Provisional Application No. 61 / 386,983, filed September 27, 2010 priority interest, said application 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 succumbed 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 o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/00A61K31/47A61K31/5377A61K45/06A61P35/00A61P35/04
CPCC07D215/22A61K31/47A61K31/5377A61K45/06A61P13/08A61P19/00A61P29/00A61P35/00A61P35/04A61P43/00A61K2300/00
Inventor D.史密斯M.侯赛因
Owner EXELIXIS INC
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