Analgesic therapeutic and method, 1-(3-4(((1R,3S,5S)-adamantan-1-yl)(phenyl)methyl)propyl)-4-methylpiperazine and salts thereof
Inventors
Assignees
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Publication Number
US-11896590-B2
Publication Date
2024-02-13
Expiration Date
Abstract
A method for the treatment and/or prevention of pain which comprises administering to a subject in need of such treatment a therapeutically effective amount of 1-(3-4(((1R,3S,5S)-adamantan-1-yl)(phenyl)methyl)propyl)-4-methylpiperazine and pharmaceutically acceptable salts thereof (“AV1066”), with reference to visceral and neuropathic pain.
Core Innovation
The invention relates to AV1066, defined as 1-(3-4(((1R,3S,5S)-adamantan-1-yl)(phenyl)methyl)propyl)-4-methylpiperazine and salts, described as a mixed sigma-1/sigma-2 ligand for treating and preventing nociceptive and neuropathic pain. The described use emphasizes pain relief and prevention in a subject in need thereof, including neuropathic pain and visceral pain. Chiral forms are defined, including (+) and (−) enantiomeric forms.
A central aspect of the described invention is administration of AV1066 in the (+) form substantially absent the (−) form. The patent content describes pharmaceutical compositions and dosage forms comprising AV1066 or a pharmaceutically acceptable salt, together with pharmaceutically acceptable carriers. The described salt examples include sodium, ammonium, phosphate, hydrochloride, and mesylate.
The disclosure provides nonclinical efficacy context using rat models including chronic constriction injury for peripheral mononeuropathy and TNBS-induced chronic colonic hypersensitivity. It reports dose-dependent restoration of nociceptive and colonic distension thresholds and states that there were no untoward effects. Patient examples are also described for fracture pain, burn pain, obstruction pain, postherpetic pain, and trigeminal pain, with pharmaceutical carrier and potential combination discussion including NSAIDs.
Claims Coverage
The partial content includes two independent claims. Both independent claims share the same core inventive concept: a therapeutically effective amount of AV1066 or a pharmaceutically acceptable salt, formulated with a defined carrier or dosage form and administered so that AV1066 is in the (+) form substantially absent the (−) form, for relieving or preventing pain in a subject in need thereof.
(+)-form AV1066 substantially absent (−)-form for pain relief or prevention
A dosage form comprising a therapeutically effective amount of AV1066 or a pharmaceutically acceptable salt, wherein the therapeutically effective amount is to relieve or prevent pain in a subject in need thereof, and wherein the AV1066 is in the (+) form substantially absent the (−) form.
(+)-form AV1066 substantially absent (−)-form pharmaceutical composition with carrier
A pharmaceutical composition comprising a therapeutically effective amount of AV1066 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein the therapeutically effective amount is to relieve or prevent pain in a subject in need thereof, and wherein the AV1066 is in the (+) form substantially absent the (−) form.
Across both independent claims, the claimed subject matter centers on administering AV1066 in the (+) form substantially absent the (−) form, as a dosage form or as part of a pharmaceutical composition with a pharmaceutically acceptable carrier, to relieve or prevent pain in a subject in need thereof.
Stated Advantages
Dose-dependent restoration of nociceptive and colonic distension thresholds in nonclinical models.
No untoward effects are reported in the nonclinical context described.
Documented Applications
Treating or preventing nociceptive pain, neuropathic pain, visceral pain, and hyperalgesia.
Using the treatment for specific pain conditions described as bone fracture pain, burn pain, obstruction pain, postherpetic pain, and trigeminal neuralgia pain.
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