(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles
Inventors
Riether, Doris • Binder, Florian Paul Christian • Doods, Henri • MUELLER, Stephan Georg • Nicholson, Janet Rachel • Sauer, Achim
Assignees
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Publication Number
US-11725004-B2
Publication Date
2023-08-15
Expiration Date
Abstract
This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
Core Innovation
The document describes novel (cyano-dimethyl-methyl)-isoxazole and -[1,3,4]thiadiazole CB2 cannabinoid receptor agonist compounds, including pharmaceutically acceptable salts. The compounds are characterized by chemical structures provided in the document and are presented for use in treating CB2 receptor-mediated disorders and conditions.
The background addressed is the need for therapeutic agents for CB2 receptor-mediated disorders and conditions, with treatment methods directed to diabetic neuropathy and neuropathic pain due to diabetic peripheral neuropathy or diabetic neuropathy. The document further addresses nerve injury-induced neuropathic pain through administration of the recited compounds to a human being.
Assay data support the compounds' CB2 activity while showing low CB1 activation and low MDCK efflux versus the closest prior art. Biological data are described using cAMP assays and an MDCK-MDR1 efflux permeability-related measure, with examples presented in a table of biological data.
Claims Coverage
The provided independent claims are directed to four treatment methods, and the core inventive element is selecting from a recited group of compounds and/or pharmaceutically acceptable salts and administering an effective amount to a human being.
Diabetic neuropathy treatment using selected CB2 agonist compounds
A method of treating diabetic neuropathy by administering to a human being an effective amount of a compound selected from the group consisting of the recited compounds and a pharmaceutically acceptable salt thereof.
Neuropathic pain due to diabetic peripheral neuropathy treatment using selected CB2 agonist compounds
A method of treating neuropathic pain due to diabetic peripheral neuropathy by administering to a human being an effective amount of a compound selected from the group consisting of the recited compounds and a pharmaceutically acceptable salt thereof.
Neuropathic pain due to diabetic neuropathy treatment using selected CB2 agonist compounds
A method of treating neuropathic pain due to diabetic neuropathy by administering to a human being an effective amount of a compound selected from the group consisting of the recited compounds and a pharmaceutically acceptable salt thereof.
Nerve injury-induced neuropathic pain treatment using selected CB2 agonist compounds
A method of treating nerve injury-induced neuropathic pain by administering to a human being an effective amount of a compound selected from the group consisting of the recited compounds and a pharmaceutically acceptable salt thereof.
The independent claims cover methods of treating diabetic neuropathy, neuropathic pain due to diabetic peripheral neuropathy, neuropathic pain due to diabetic neuropathy, and nerve injury-induced neuropathic pain by administering an effective amount of a selected CB2 cannabinoid receptor agonist compound and pharmaceutically acceptable salts.
Stated Advantages
Potency with low CB1 activation versus closest prior art, supported by cAMP assay results.
Low MDCK efflux versus closest prior art, supported by an MDCK-MDR1 efflux measure.
Documented Applications
Treating diabetic neuropathy in a human being by administering an effective amount of a compound selected from a group of CB2 cannabinoid receptor agonist compounds and pharmaceutically acceptable salts.
Treating neuropathic pain due to diabetic peripheral neuropathy in a human being by administering an effective amount of a compound selected from a group of CB2 cannabinoid receptor agonist compounds and pharmaceutically acceptable salts.
Treating neuropathic pain due to diabetic neuropathy in a human being by administering an effective amount of a compound selected from a group of CB2 cannabinoid receptor agonist compounds and pharmaceutically acceptable salts.
Treating nerve injury-induced neuropathic pain in a human being by administering an effective amount of a compound selected from a group of CB2 cannabinoid receptor agonist compounds and pharmaceutically acceptable salts.
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