- SUBSTITUTED XANTHINE DERIVATIVES
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The present invention relates to compounds of formula (I) a process for their manufacture, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels. R1, R2, R3, R4 and R5 have meanings given in the description.
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Page/Page column 39-40
(2020/07/07)
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- CAFFEINE INHIBITORS OF MTHFD2 AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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- Effects of Alkyl Substitutions of Xanthine Skeleton on Bronchodilation
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Structure-activity relationships in a series of 1,3,7-trialkyl-xanthine were studied with guinea pigs.Relaxant actions in the tracheal muscle were increased with alkyl chain length at the 1- and 3-positions of the xanthine skeleton, but decreased by alkylation at the 7-position.Positive chronotropic actions in the right atrium were potentiated with 3-alkyl chain length but tended to decrease with 1-alkylation and diminish by 7-substitution.Consequently, while the 1- and 3-substitutions were equally important for the tracheal smooth muscle relaxation, the substitution at the 1-position was more important than the 3-substitution for bronchoselectivity.The 7-alkylation may be significant to cancel heart stimulation.There were good correlations between the smooth muscle relexant action and the cyclic AMP-PDE inhibitory activity in 3-substituents and the affinity for adenosine (A1)receptors in 1-,3-, and 7-substituents.This suggests that not only the cyclic AMP-PDE inhibitory activity but also the adenosine antagonistic activity is important in the bronchodilatory effects of alkylxanthines.Among these xanthine derivatives, 1-butyl-3-propylxanthine and its 7-methylated derivative showed high bronchoselectivity in the in vitro and in vivo experiments compared to theophylline and enprofylline and may be new candidates for bronchodilator.
- Sakai, Ryosuke,Konno, Kayo,Yamamoto, Yasunori,Sanae, Fujiko,Takagi, Kenzo,et al.
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p. 4039 - 4044
(2007/10/02)
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- Method for the treatment of chronic obstructive airway or cardiac diseases
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A method for the treatment of chronic obstructive airway disease or cardiac disease by administration 3-ethylxantine or a pharmaceutically acceptable salt thereof; a pharmaceutical preparation containing 3-ethylxanthine.
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