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Substituted pyridopyrimidine compounds and their use as FLT3 inhibitors

A compound, C1-C3 technology, applied in the field of substituted pyridopyrimidine compounds and their use as FLT3 inhibitors, which can solve problems such as expression

Active Publication Date: 2015-03-18
OSCOTEC INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, MER is not expressed in normal lymphocytes

Method used

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  • Substituted pyridopyrimidine compounds and their use as FLT3 inhibitors
  • Substituted pyridopyrimidine compounds and their use as FLT3 inhibitors
  • Substituted pyridopyrimidine compounds and their use as FLT3 inhibitors

Examples

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Embodiment

[0111] The following examples illustrate the preparation of the compounds of formula (I) of the present invention and further illustrate the present invention by these examples. The examples are for illustrative purposes only and are not intended and should not be construed as limiting the invention in any way. Those skilled in the art will recognize that changes and modifications can be made without altering the scope of the invention.

[0112] Liquid chromatography-mass spectrometry (LC-MS) method:

[0113] 1. The sample was run at a flow rate of 1.5 mL / min on an Agilent Technologies 6120 MSD system with a Zorbax Eclipse XDB-C18 (3.5 μ) inverted column (4.6×50 mm) running at room temperature.

[0114] 2. The mobile phase uses solvent A (water / 0.1% formic acid) and solvent B (acetonitrile / 0.1% formic acid): 95% / 5% to 0% / 100% (A / B) for 5 minutes.

[0115] 3. Record mass spectra (m / z) using electrospray ionization (ESI).

[0116] 4. Ionization data is rounded to the nearest ...

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Abstract

Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).

Description

[0001] related application [0002] This application claims the benefit of and priority to US Provisional Patent Application No. 61 / 614,274, filed March 22, 2012, which is hereby incorporated by reference in its entirety. Background of the invention [0003] FLT3 (FMS-like tyrosine kinase 3, also known as Flk2) is a member of the type III receptor tyrosine kinase (RTK) family and plays an important role in the proliferation and differentiation of hematopoietic stem cells. Activating mutations and overexpression of this receptor are found in acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), mastocytosis, and gastrointestinal stromal tumors (GIST). In addition to activating mutations, autocrine or paracrine ligand stimulation by overexpressing wild-type FLT3 can lead to malignant phenotypes. [0004] Ligands for FLT3 are expressed by bone marrow stromal cells and other cells and potentiated synergistically with other growth factors to stimulate the proliferation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/519A61P35/00
CPCC07D239/00C07D471/04A61K31/31A61K31/519C07D487/04A61K45/06A61P25/00A61P25/28A61P35/00A61P35/02A61P37/02A61P37/06
Inventor 金宏宇李希奎宋浩俊李宰奎高钟盛金政浩金世园李任勇
Owner OSCOTEC INC
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