Pharmaceutically active dimers linked through phenolic hydroxyl groups
AssigneeOrphomed, Inc.
InventorNikhilesh Nihala Singh
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Abstract
Pharmaceutically active homo-dimers of opioid and other pharmaceutically active agents characterized by a single phenolic hydroxyl group wherein the respective monomers are ether-linked through such groups by an ethylene residue. The dimers share the receptor pharmacology of the corresponding monomer, in particular cases are non-absorbed, and the ether link of the dimers is particularly resistant to metabolism when administered to a subject, all conferring divers advantages relative to the corresponding monomers. Exemplary of the dimers are those of buprenorphine, naloxone, naltrexone, des-venlafaxine, albuterol and acetaminophen.
Claims10
A homo-dimer compound of a pharmaceutically active agent selected from the group consisting of naloxone, naltrexone, des-venlafaxine and albuterol wherein two such agents are covalently ether-linked through phenolic hydroxyl groups of the agents by an ethylene residue, or a pharmaceutically acceptable salt or solvate thereof.
A naloxone dimer compound having the Formula:
- or a pharmaceutically acceptable salt or solvate thereof.
A naltrexone dimer compound having the Formula:
- or a pharmaceutically acceptable salt or solvate thereof.
A des-venlafaxine dimer compound having the Formula:
- or a pharmaceutically acceptable salt or solvate thereof.
An albuterol dimer compound having the Formula:
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.