Novel xanthines having adenosine A1-receptor antagonist properties
OwnerPascal Druzgalainventor
Life of this patent
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Abstract
The subject invention provides 1,3-dipropylxanthines that have an ester function at the 8-position also have potent and specific A1AdoR antagonist properties.
Claims11
An A1AdoR antagonist that has at least one characteristic chosen from the group consisting of:
- a. the compound is metabolized both by CYP450 and by a non-oxidative metabolic enzyme or system of enzymes;
- b. the compound has a short (up to four (4) hours) non-oxidative metabolic half-life;
- c. the compound contains a hydrolysable bond that can be cleaved non-oxidatively by hydrolytic enzymes;
- d. the primary metabolites of the compound result from the non-oxidative metabolism of the compound;
- e. the primary metabolites are soluble in water at physiological pH;
- f. the primary metabolites have negligible inhibitory activity at the IKR (HERG) channel at normal therapeutic concentration of the parent drug in plasma;
- g. the compound, as well as the metabolites thereof, does not cause metabolic DDI when co-administered with other drugs;
- and
- h. the compound, as well as metabolites thereof, does not elevate LFT values when administered alone.
A pharmaceutical composition comprising an A1AdoR antagonist that has at least one characteristic chosen from the group consisting of:
- a. the compound is metabolized both by CYP450 and by a non-oxidative metabolic enzyme or system of enzymes;
- b. the compound has a short (up to four (4) hours) non-oxidative metabolic half-life;
- c. the compound contains a hydrolysable bond that can be cleaved non-oxidatively by hydrolytic enzymes;
- d. the primary metabolites of the compound result from the non-oxidative metabolism of the compound;
- e. the primary metabolites are soluble in water at physiological pH;
- f. the primary metabolites have negligible inhibitory activity at the IKR (HERG) channel at normal therapeutic concentration of the parent drug in plasma;
- g. the compound, as well as the metabolites thereof, does not cause metabolic DDI when co-administered with other drugs;
- and
- h. the compound, as well as metabolites thereof, does not elevate LFT values when administered alone;
- wherein said composition further comprises a pharmaceutical carrier.
A method for inhibiting the A1Ado receptor in an individual in need of such treatment wherein said method comprises administering to said individual a pharmaceutical composition comprising an A1AdoR antagonist that has at least one characteristic chosen from the group consisting of:
- a. the compound is metabolized both by CYP450 and by a non-oxidative metabolic enzyme or system of enzymes;
- b. the compound has a short (up to four (4) hours) non-oxidative metabolic half-life;
- c. the compound contains a hydrolysable bond that can be cleaved non-oxidatively by hydrolytic enzymes;
- d. the primary metabolites of the compound result from the non-oxidative metabolism of the compound;
- e. the primary metabolites are soluble in water at physiological pH;
- f. the primary metabolites have negligible inhibitory activity at the IKR (HERG) channel at normal therapeutic concentration of the parent drug in plasma;
- g. the compound, as well as the metabolites thereof, does not cause metabolic DDI when co-administered with other drugs;
- and
- h. the compound, as well as metabolites thereof, does not elevate LFT values when administered alone.
Dependencies are inferred from the claim text.