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Assignees
Member
Glycos Biomedical LtdWe are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
We are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
Publication Number
US-12624004-B2
Publication Date
2026-05-12
Expiration Date
Abstract
The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.
Core Innovation
The patent discloses a defined set of compounds, or pharmaceutically acceptable salts thereof, selected from substituted cyclohexyl benzoate and related cyclohexan-1-ol structures bearing a dimethylamino methyl group and a 3-methoxyphenyl substituent. The selected compounds include benzenesulfonamide, methanesulfonamide, phenylsulfonyl, thiophene-2-sulfonamide, benzylsulfonyl, and related sulfonamide variants, including hydrochloride salt forms.
The document describes these compounds as opioid receptor-related compounds and reports binding data for representative members, including Ki or binding rate values for mu, delta, and kappa opioid receptors. Comparative data against tramadol is repeatedly stated, and the disclosed compounds are described as showing higher affinity for three opioid receptors than tramadol.
The provided material also places the compounds in an analgesia context, including in vivo hot plate analgesia testing with %MPE and ED50 values and comparison to tramadol. The text further reports chemical characterization such as 1H NMR, 13C NMR, LC-MS or LC-MS-ESI, and optical rotation for selected examples and salt forms.
Claims Coverage
The consolidated claim coverage centers on one independent structural claim covering a selected set of compounds or pharmaceutically acceptable salts, with dependent claims adding a pharmaceutical composition and method-of-treatment coverage. In total, the claim set presents three inventive layers: the selected compound set, the composition with carrier, and treatment methods for opioid receptor-related indications.
Selected cyclohexyl benzoate and sulfonamide compound set
A compound or pharmaceutically acceptable salt thereof selected from named substituted cyclohexyl benzoate, cyclohexan-1-ol, benzenesulfonamide, methanesulfonamide, phenylsulfonyl, thiophene-2-sulfonamide, benzylsulfonyl, and related variants, including hydrochloride forms.
Pharmaceutical composition with optional solvate or hydrate
A pharmaceutical composition comprising the selected compound or pharmaceutically acceptable salt, optionally as a solvate or hydrate, together with a pharmaceutically acceptable carrier.
Method of treating an opioid receptor-related condition
A method of treating an opioid receptor-related condition by administering to a subject in need the pharmaceutical composition defined in the claims.
Opioid receptor-related indication selected from defined conditions
The method wherein the opioid receptor-related indication is chosen from pain, irritable bowel syndrome, pruritus, addiction, or depression.
Pain subtypes selected from defined pain categories
The method wherein the opioid receptor-related indication is pain, chosen from pain during surgery, chronic pain, neuropathic pain, or cancer pain.
Overall, the claims cover a defined compound selection and salts, extend to a pharmaceutical composition with a pharmaceutically acceptable carrier, and further extend to administration methods for opioid receptor-related conditions, with indication narrowing to pain and other specified conditions.
Stated Advantages
Higher affinity for three opioid receptors than tramadol.
Stronger in vivo analgesic effects than tramadol.
Documented Applications
In vivo hot plate analgesia testing with %MPE and ED50 reported for representative compounds and tramadol.
Competitive binding assays on CHO cells expressing mu, delta, or kappa opioid receptors, with Ki or binding values reported.
Treating opioid receptor-related conditions by administering the claimed pharmaceutical composition, including pain, irritable bowel syndrome, pruritus, addiction, or depression.
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