Abuse-resistant prodrugs of oxycodone and other pharmaceuticals
First Claim
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1. A compound comprising a drug attached to an organic chain via a nucleophile present on the drug, wherein the organic chain has, at the end distal to the drug, an organic group susceptible to enzymatic cleavage and substantially unsusceptible to non-enzymatic cleavage.
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Abstract
One aspect of the present invention relates to compositions and methods for discouraging improper use of habit-forming and addictive drugs, such as oxycodone. In a preferred embodiment, a habit-forming or addictive drug is chemically modified to block its physiological activity until the drug is transformed to a physiologically active form in the mammalian gastrointestinal tract.
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53 Claims
- 1. A compound comprising a drug attached to an organic chain via a nucleophile present on the drug, wherein the organic chain has, at the end distal to the drug, an organic group susceptible to enzymatic cleavage and substantially unsusceptible to non-enzymatic cleavage.
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13. A method of making a drug more difficult to abuse, comprising bonding an organic radical to the drug at one end of the organic radical via a nucleophile on the drug, wherein said organic radical comprises a functional group that is susceptible to enzymatic cleavage and substantially unsusceptible to non-enzymatic cleavage.
- 15. A compound of formula I:
- 38. A method of making a drug more difficult to abuse, comprising bonding to a nucleophile on the drug a radical of formula II:
Specification