Ultrashort-acting opioids for transdermal application
AssigneeARYx Therapeutics, Inc.
InventorPascal Druzgala
Life of this patent
Estimating the term…
Abstract
The subject invention concerns novel analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.
Claims22
An opioid compound having at least one characteristic selected 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 opioid compound having at least one characteristic selected 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 treating pain wherein said method comprises administering to a patient in need of such treatment an opioid compound having at least one characteristic selected 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.