PI3K inhibitor for treatment of respiratory disease

A technology for the respiratory system and diseases, applied in the field of PI3K inhibitors for the treatment of respiratory diseases, which can solve problems such as inappropriate PI3Kδ activity

Inactive Publication Date: 2016-05-25
GLAXOSMITHKLINE INTPROP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mutations in PI3Kδ can thus result in inappropriate PI3Kδ activity, which can be increased or lower compared to the wild-type protein

Method used

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  • PI3K inhibitor for treatment of respiratory disease
  • PI3K inhibitor for treatment of respiratory disease
  • PI3K inhibitor for treatment of respiratory disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0341] 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazole-2- base)-1H-indazole hydrochloride for the treatment of Streptococcus pneumoniae

[0342] Germ-free C57BL / 6 male and female mice aged 10-12 weeks were intranasally administered 0.2% Tween-80 / saline vehicle or 0.2 mg / kg micronized 6-(1H-indole in the same vehicle Indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-ind azole hydrochloride. Compound administration was performed twice daily for 11 days under anesthesia (induction with 3% isoflurane and maintenance with 2% isoflurane). Started on the second day and administered 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1, One hour after 3-oxazol-2-yl)-1H-indazole hydrochloride or vehicle, mice were anesthetized with isoflurane as described above and treated with 1 × 10 7 CFU of intranasal infection with Streptococcus pneumoniae strain TIGR4. S. pneumoniae was obtained and prepared as previously ...

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Abstract

The present invention is directed to compounds and pharmaceutically acceptable salts thereof which are inhibitors of the activity or function of the phosphoinositide 3'OH kinase family (hereinafter PI3K) for use in the treatment or prevention of respiratory infections, the treatment of airway damage, and / or the prevention of airway injury in patients.

Description

field of invention [0001] The present invention relates to compounds and pharmaceutically acceptable salts thereof as inhibitors of the activity or function of the phosphoinositide 3'OH kinase family (hereinafter referred to as PI3K), in particular PI3Kδ, for use in patients, especially those with Treatment or prophylaxis of respiratory infections, treatment of airway damage (airway damage) and / or prevention of airway damage (airway injury) in patients with PI3Kδ mutations. Background of the invention [0002] The class I PI3 kinase family includes four independent isoforms (α, β, γ, and δ) that are distinguished by the sequence and structure of the p110 catalytic subunit. A number of different genetic variants of PI3Kδ have been observed (Jou et al., International Journal of Immunogenetics, 2006, 33, 361-369, Angulo et al., Science DOI: 10.1126 / science.1243292, and Lucas et al., Nature Immunology DOI: 10.1038 / ni.2271) . Some genetic variants can result in silent nucleotid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/497A61K31/553A61P11/00
CPCA61K31/497A61K31/553A61P11/00A61P11/02A61P11/04A61P29/00A61P31/04C07D231/56C07D413/14A61K31/496A61K31/5377
Inventor A.阿穆J.N.汉布林E.赫塞尔D.米夏尔洛维基S.斯里斯坎塔拉雅
Owner GLAXOSMITHKLINE INTPROP
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