Morphinan compounds
First Claim
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1. A method of evaluating the metabolic stability of a deuterated morphinan compound, comprising:
- a. contacting a first amount of the deuterated morphinan compound with a metabolizing enzyme source for a period of time sufficient to allow the formation of a mixture comprising one or more metabolic products of the deuterated morphinan compound and a remaining amount of the deuterated morphinan compound;
b. at the period of time, determining the remaining amount of the deuterated morphinan compound and the amount of at least one of the one or more metabolic products in the mixture; and
c. comparing the remaining amount of the deuterated morphinan compound determined in step b. with the first amount of the deuterated morphinan compound and/or comparing the first amount of the deuterated morphinan compound with the amount of the at least one of the one or more metabolic products determined in step b. to determine the metabolic stability of the deuterated morphinan compound, wherein the metabolic stability is expressed as the % of the amount of the deuterated morphinan compound determined in step b. relative to the first amount and/or as the % of the at least one of the one or more metabolic products determined in step b. relative to the first amount of the deuterated morphinan compound, wherein the deuterated morphinan compound is a compound of Formula I
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Abstract
This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity.
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16 Claims
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1. A method of evaluating the metabolic stability of a deuterated morphinan compound, comprising:
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a. contacting a first amount of the deuterated morphinan compound with a metabolizing enzyme source for a period of time sufficient to allow the formation of a mixture comprising one or more metabolic products of the deuterated morphinan compound and a remaining amount of the deuterated morphinan compound; b. at the period of time, determining the remaining amount of the deuterated morphinan compound and the amount of at least one of the one or more metabolic products in the mixture; and c. comparing the remaining amount of the deuterated morphinan compound determined in step b. with the first amount of the deuterated morphinan compound and/or comparing the first amount of the deuterated morphinan compound with the amount of the at least one of the one or more metabolic products determined in step b. to determine the metabolic stability of the deuterated morphinan compound, wherein the metabolic stability is expressed as the % of the amount of the deuterated morphinan compound determined in step b. relative to the first amount and/or as the % of the at least one of the one or more metabolic products determined in step b. relative to the first amount of the deuterated morphinan compound, wherein the deuterated morphinan compound is a compound of Formula I - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
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10. A method of evaluating the metabolic stability of a deuterated morphinan compound in a subject, comprising:
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a. administering a first amount of the deuterated morphinan compound to a subject; b. obtaining a serum, blood, tissue, urine, or feces sample from the subject at a period of time following the administration of the compound to the subject, wherein the period of time is sufficient to allow the formation of one or more metabolic products of the deuterated morphinan compound in the sample; c. at the period of time, determining the remaining amount of the deuterated morphinan compound and the amount of at least one of the one or more metabolic products in the sample; and d. comparing the remaining amount of the deuterated morphinan compound determined in step b. in the sample with the first amount of the deuterated morphinan compound and/or comparing the first amount of the deuterated morphinan compound with the amount of the at least one of the one or more metabolic products determined in step b. in the sample to determine the metabolic stability of the deuterated morphinan compound, wherein the metabolic stability is expressed as the % of the remaining amount of the deuterated morphinan compound determined in step b. relative to the first amount and/or as the % of the at least one of the one or more metabolic products determined in step b. relative to the first amount of the deuterated morphinan compound, wherein the deuterated morphinan compound is a compound of Formula I - View Dependent Claims (11, 12, 13, 14, 15, 16)
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Specification