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Pyrazinone derivatives and their use in the treatment of lung diseases

A technology of compounds and medicinal salts, applied in the field of pyrazinone derivatives, can solve problems such as unsatisfactory efficacy

Active Publication Date: 2013-06-05
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although glucocorticoid therapy can yield important benefits, the efficacy of these drugs is often far from satisfactory, especially in the treatment of COPD

Method used

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  • Pyrazinone derivatives and their use in the treatment of lung diseases
  • Pyrazinone derivatives and their use in the treatment of lung diseases
  • Pyrazinone derivatives and their use in the treatment of lung diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0707] N-cyclopropyl-3-[3-(2-fluoro-benzylamino)-2-oxo-2H-pyrazin-1-yl]-4-methyl-benzamide

[0708]

[0709] a) 3-[(cyanomethyl)amino]-4-methyl-benzoic acid methyl ester

[0710] To a stirred solution of methyl 3-amino-4-methyl-benzoate (10.0 g) in anhydrous tetrahydrofuran was added N,N-diisopropylethylamine (12.6 mL) followed by bromoacetonitrile (5.1 mL ). The reaction mixture was heated at reflux under nitrogen atmosphere while stirring for 12 h. Water was added, and the mixture was extracted with ethyl acetate. The pooled organics were washed with brine, dried (MgSO 4 ), filtration, and removal of the solvent under reduced pressure to afford the subtitle compound as a solid (12.4 g).

[0711] MS: APCI (+ve) 178 (M+H + ).

[0712] 1 H NMR (DMSO-d 6 , 300MHz) 7.31 (1H, dd), 7.23-7.17 (2H, m), 5.91 (1H, t), 4.33 (2H, d), 3.83 (3H, s), 2.17 (3H, s).

[0713] b) 3-(3,5-Dibromo-2-oxo-2H-pyrazin-1-yl)-4-methyl-benzoic acid methyl ester

[0714] To 3-[(cyanomethyl)...

Embodiment 2

[0723] N-cyclopropyl-4-methyl-3-[3-(4-methyl-piperazin-1-yl)-2-oxo-pyrazin-1(2H)-yl]-benzamide

Embodiment 3

[0725] N-cyclopropyl-3-[3-[[3-(dimethylamino)propyl]amino]-2-oxo-pyrazin-1(2H)-yl]-4-methyl-benzyl Amide

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PUM

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Abstract

The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Description

technical field [0001] The present invention relates to pyrazinone derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. Background technique [0002] The essential function of the lung requires a delicate structure to be exposed extensively to the environment including pollutants, microorganisms, allergens and carcinogens. Host factors arising from the interplay of lifestyle choices and genetic makeup influence the response to this exposure. Injury or infection to the lungs can produce a wide range of respiratory diseases (or respiratory diseases). Many of these diseases are of enormous public health importance. Respiratory diseases include acute lung injury, acute respiratory distress syndrome (ARDS), occupational lung disease, lung cancer, tuberculosis, fibrosis, pneumoconiosis, pneumonia, emphysema, chronic obstructive pulmonary disease (COPD), and asthma . [0003] The most common respiratory disease is a...

Claims

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Application Information

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IPC IPC(8): C07D241/20C07D401/12C07D403/04C07D403/12C07D413/12A61K31/454A61P11/06
CPCC07D401/12C07D241/20C07D403/04C07D403/12C07D413/12C07D241/08C07D405/12C07D413/04C07D471/10C07D491/113A61P1/04A61P1/08A61P1/16A61P11/00A61P11/02A61P11/06A61P11/08A61P13/08A61P13/10A61P15/00A61P17/00A61P17/04A61P17/06A61P19/00A61P19/02A61P19/10A61P21/00A61P25/00A61P25/06A61P25/28A61P27/02A61P29/00A61P31/12A61P35/00A61P37/06A61P43/00A61P5/00A61P9/00A61P9/10A61K31/454
Inventor 斯蒂芬·布拉夫理查德·埃文斯蒂莫西·J·卢克皮奥特·劳伯
Owner ASTRAZENECA AB
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