Phenyl carbamate compounds for use in alleviating or treating pain
Inventors
Assignees
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Publication Number
US-9162975-B2
Publication Date
2015-10-20
Expiration Date
Abstract
A phenyl carbamate compound; a composition for treating and/or alleviating pain containing the phenyl carbamate compound or a pharmaceutically acceptable salt thereof as an active ingredient; a method of treating and/or alleviating pain comprising administering the phenyl carbamate compound or a pharmaceutically acceptable salt thereof to a patient in need of pain treatment; and a use of the phenyl carbamate compound or a pharmaceutically acceptable salt thereof in treating and/or alleviating pain, are provided.
Core Innovation
The invention relates to a method of alleviating or treating pain in a subject in need of such treatment, where the pain is not muscle spasm-associated pain. The method includes administering a pharmaceutically effective amount of a compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof, and the compound represented by Chemical Formula 1 is the sole active agent.
Chemical Formula 1 defines the compound structure using substituent variables including X as a halogen, n as an integer from 1 to 5, R1 as a linear or branched alkyl group of C1-C4, A as a carbamoyl derivative, B as hydrogen, and R2 as selected from hydrogen, a linear or branched alkyl group of C1-C4, a cycloalkyl group of C3-C8, and a benzyl group. The method is additionally limited to selected pain categories and to stereochemical forms or named stereoisomeric/racemic variants, while keeping the administered Chemical Formula 1 compound as the sole active agent.
The compounds are provided in stereochemical forms including racemate, single enantiomer or diastereomer, and mixtures of enantiomers or diastereomers. The disclosure includes specific stereoisomeric and racemic carbamate variants based on 1-(2-chlorophenyl), 1-(2-fluorophenyl), or 1-(2-iodophenyl) substituted hydroxypropyl or hydroxybutyl derivatives with defined (S)/(R) configurations and optional N-substituted carbamates.
Claims Coverage
The independent claim is directed to a method of treating pain by administering a pharmaceutically effective amount of a Chemical Formula 1 compound as the sole active agent, excluding muscle spasm-associated pain. The claim set includes 5 inventive features centered on the treatment method, the Chemical Formula 1 substituent definition, restricted pain categories, allowed stereochemical forms, and specific stereoisomeric carbamate variants.
Pain treatment using Chemical Formula 1 as sole active agent
Administering a pharmaceutically effective amount of a compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof to a subject in need of alleviating or treating pain that is not muscle spasm-associated pain, wherein the compound represented by Chemical Formula 1 is the sole active agent.
Defined Chemical Formula 1 substituent ranges
Within Chemical Formula 1, X is a halogen; n is an integer from 1 to 5; R1 is a linear or branched alkyl group of C1-C4; A is a carbamoyl derivative; B is hydrogen; and R2 is selected from hydrogen, a linear or branched alkyl group of C1-C4, a cycloalkyl group of C3-C8, and a benzyl group.
Restricted pain categories
The pain being treated is selected from nociceptive pain, psychogenic pain, inflammatory pain, or pathological pain.
Allowed stereochemical forms
The compound is present as a racemate, a single enantiomer or diastereomer, or mixtures of enantiomers or diastereomers.
Specific stereoisomeric carbamate variants
The compound is selected from specified stereoisomeric and racemic carbamate variants based on 1-(2-chlorophenyl), 1-(2-fluorophenyl), or 1-(2-iodophenyl) substituted hydroxypropyl or hydroxybutyl derivatives with defined (S)/(R) configurations and optional N-substituted carbamates.
Overall, the claims cover administering a Chemical Formula 1 compound or salt as the sole active agent to treat pain that is not muscle spasm-associated pain, with further narrowing by substituent limits, specified pain categories, stereochemical form, and enumerated stereoisomeric carbamate species.
Stated Advantages
Remarkably excellent anti-pain activity.
Very low toxicity.
The compound represented by Chemical Formula 1 is the sole active agent that alleviates or treats pain which is not muscle spasm-associated pain.
Documented Applications
A method of alleviating or treating pain in a subject, where the pain is not muscle spasm-associated pain.
Treatment of nociceptive pain, psychogenic pain, inflammatory pain, or pathological pain.
Pain treatment evaluated in pain emulation models.
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