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Treatment of lung and other conditions

A technology of alkyl compounds, applied in the field of treatment of lung diseases and other diseases, can solve the problems of invasion of normal tissues, cell proliferation, mutation, etc.

Active Publication Date: 2018-07-24
UNIVERSITY OF PITTSBURGH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Like other environmental carcinogens that can induce lung cancer, the carcinogens in cigarette smoke cause mutations that cause the affected cells to proliferate uncontrollably and also allow them to invade normal tissues

Method used

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  • Treatment of lung and other conditions
  • Treatment of lung and other conditions
  • Treatment of lung and other conditions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0698] General Synthesis of PB Compounds

[0699] A solution of pyrazine-2-carbaldehyde (4.62 mmol) in pure ethanol (1 ml) was added dropwise to NaOH (0.75 mmol) and ketone (acetone) in pure ethanol under slow stirring over 10 minutes at room temperature and H 2 o 2 (14ml; 1:1 ratio) of the mixture in solution. The solution will turn yellow followed by the formation of a yellow precipitate within 10 minutes. The reaction was stirred at room temperature for 6 h, then the yellow solid was removed by filtration and washed with water; the organic phase was then washed with anhydrous MgSO 4 Dried and concentrated under vacuum to give a pale yellow powder representing PB137 in 97% purity.

Embodiment 2

[0701] Synthesis of PB compounds with acetone

[0702] After 10 minutes at room temperature, under slow stirring, pyrazine-2-carbaldehyde [or 3-aminopyrazine-2-carbaldehyde; 6-amino-5-hydroxypyrazine-2-carbaldehyde; 5-hydroxy- 6-methoxypyrazine-2-carbaldehyde; 3-thiocyanatopyrazine-2-carbaldehyde; 5-(chloromethylthio)pyrazine-2-carbaldehyde; 5-acetylpyrazine-2-carbaldehyde; 6-(trifluoromethoxy)pyrazine-2-carbaldehyde; 5-fluoropyrazine-2-carbaldehyde; 5-(methylthio)pyrazine-2-carbaldehyde; 5-(chloromethylthio)pyrazine -2-carbaldehyde; 6-tert-butoxypyrazine-2-carbaldehyde; 5-acetylpyrazine-2-carbaldehyde; 6-trifluoromethoxypyrazine-2-carbaldehyde; 6-amino-5-hydroxypyridine oxazine-2-carbaldehyde; 5-hydroxy-6-methoxypyrazine-2-carbaldehyde; 6-(trifluoromethyl)pyrazine-2-carbaldehyde: (4.62mmol)] in pure ethanol (1ml) The solution was added dropwise to NaOH (0.75 mmol) and acetone in absolute ethanol and H 2 o 2 (14ml; 1:1 ratio) of the mixture in solution. The solution will ...

Embodiment 3

[0704] Synthesis of PB Compounds Using Cyclohexanone

[0705] After 10 minutes at room temperature, under slow stirring, pyrazine-2-carbaldehyde [or 3-aminopyrazine-2-carbaldehyde; 6-amino-5-hydroxypyrazine-2-carbaldehyde; 5-hydroxy- 6-methoxypyrazine-2-carbaldehyde; 3-thiocyanatopyrazine-2-carbaldehyde; 5-(chloromethylthio)pyrazine-2-carbaldehyde; 5-acetylpyrazine-2-carbaldehyde; 6-(trifluoromethoxy)pyrazine-2-carbaldehyde; 5-fluoropyrazine-2-carbaldehyde; 5-(methylthio)pyrazine-2-carbaldehyde; 5-(chloromethylthio)pyrazine -2-carbaldehyde; 6-tert-butoxypyrazine-2-carbaldehyde; 5-acetylpyrazine-2-carbaldehyde; 6-trifluoromethoxypyrazine-2-carbaldehyde; 6-amino-5-hydroxypyridine oxazine-2-carbaldehyde; 5-hydroxy-6-methoxypyrazine-2-carbaldehyde; or 6-(trifluoromethyl)pyrazine-2-carbaldehyde: (4.62mmol)] in pure ethanol (1ml) A solution of NaOH (0.75 mmol) and cyclohexanone in pure ethanol and H was added dropwise 2 o 2 (14ml; 1:1 ratio) of the mixture in solution. The solu...

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PUM

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Abstract

Disclosed herein is a compound, or a pharmaceutically acceptable salt or ester thereof, having the structure X1-L-X2, wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently optionally substituted N ‑ Heterocycle. Also disclosed herein are methods of treating lung disorders and disorders of other organs or systems with the compounds.

Description

[0001] This application claims the benefit of US Provisional Application No. 61 / 822,224, filed May 10, 2013, which is hereby incorporated by reference in its entirety. [0002] Confirmation of government support [0003] This invention was made with government support under Grant No. HL093196 awarded by the National Institutes of Health. The government has certain rights in this invention. Background technique [0004] The lungs are organs that rely on delicate structures, such as the alveolar-capillary interface for important gas exchange functions, but are often exposed to toxins and irritants in inhaled gases. It can also be damaged by toxins and inflammatory products produced by infection and by misplacement elsewhere in the body. As a result, the lung is subject to a wide variety of diseases, many of which have a pathogenesis that is not fully understood. Some of these diseases and conditions have effective treatments available; these treatments may include the adminis...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/06C07D403/08A61K31/506A61K31/497A61P11/00A61P11/06A61P11/12A61P35/00
CPCC07D239/26C07D239/30C07D239/34C07D239/38C07D239/42C07D239/47C07D239/52C07D241/12C07D241/16C07D241/18C07D241/20A61P11/00A61P11/06A61P11/12A61P29/00A61P35/00A61P37/06A61P37/08A61P39/06A61P43/00A61P9/10
Inventor R·雷迪
Owner UNIVERSITY OF PITTSBURGH
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