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Methods of using ALK inhibitors

A technology of use and medicinal salt, which is applied in the field of ALK inhibitor use, and can solve problems such as acquired drug resistance, relapse, and unsatisfied

Active Publication Date: 2013-12-18
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, relapses (or acquired resistance) have been reported
Therefore, the needs of patients carrying the EML4-ALK fusion gene remain unmet

Method used

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  • Methods of using ALK inhibitors
  • Methods of using ALK inhibitors
  • Methods of using ALK inhibitors

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Antitumor activity in NCI-H2228 NSCLC mouse model

[0044]In vitro cell growth and proliferation. NCI-H2228 cells were obtained from the American Type Culture Collection (ATCC) (Manassa, USA) and modified by virus infection to stably express luciferase. For cell growth and proliferation assays, using a μ-filler device (Bio-Tek), cells were placed in 50 μL RPMI medium (Gibco, Carlsbad, CA) containing 10% fetal bovine serum (FBS) (Gibco, Carlsbad, CA). 2250 cells were plated on the solid bottom of a white 384-well plate (Corning, Acton, MA). Plates were incubated for 1 hour at 37°C in a tissue culture incubator before compound addition using a MiniTrak device (Perkin-Elmer). 50 nL of the 1 :3 diluted compound plate was added to the assay plate such that the final concentrations were 10000, 3333, 1111, 370, 123, 41, 14, 4.6, 1.5, 0.5 and 0.17 nM. After compound addition, plates were incubated in a tissue culture incubator at 37°C for 3 days. On day 3, the plates were a...

Embodiment 2

[0052] Antitumor activity in crizotinib-resistant tumors

[0053] Mouse xenograft tumors obtained from NCI-H2228 were treated with crizotinib at a dose of 50 mg / kg for 9 days, followed by 75 mg / kg for 9 days, then 100 mg / kg Administration for 33 days. Alternatively, xenograft tumors obtained from NCI-H2228 were initially treated with crizotinib at a dose of 100 mg / kg for 14 days, and treatment with crizotinib was stopped for several days until tumor regrowth. When the tumor grew again, the animals were treated with crizotinib 100 mg / kg until the tumor became resistant to crizotinib treatment. Tumors obtained from individual animals were collected when they became resistant to crizotinib. Several drug-resistant tumors were randomly selected for the following research. Each drug-resistant tumor was diced and implanted into 5 animals; when the tumor volume in 5 animals was sufficiently large, the tumors were harvested and then implanted into 25 animals for compound testing. A...

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Abstract

The invention provides methods for using compounds of formula (I) for treating an EML4-ALK+ mediated condition such as EML4-ALK+ non-small cell lung cancer, and optionally resistant to crizotinib; wherein R1, R2, R3, R4, R5 and R6 are as defined above.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Application Serial No. 61 / 438,878, filed February 2, 2011, the entire contents of which are incorporated herein by reference. technical field [0003] The present invention relates to the use of ALK inhibitors as medicaments. Background technique [0004] Lung cancer is the leading cause of cancer death in Western countries (Jemal et al., CA Cancer J. Clin. 56, 106-130 (2006)). Patients with non-small cell lung cancer (NSCLC), which accounts for approximately 80 percent of lung cancer cases, are usually diagnosed at an advanced stage of the disease. Given that conventional chemotherapy regimens only marginally improve treatment outcomes for such individuals, their average survival is less than one year after diagnosis (Schiller et al., N. Engl. J. Med. 346, 92-98 (2002)). Therefore, there is still a need for new treatment options for lung cancer patients. Clinical studies ha...

Claims

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Application Information

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IPC IPC(8): A61K31/00A61K31/506A61P35/00
CPCA61K31/506A61P11/00A61P35/00A61P43/00C07D401/12C07D401/14
Inventor N·李J·L·哈里斯P·麦克纳马拉F·孙
Owner NOVARTIS AG
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