C07D311/78

Applications of Known and Novel Cannabinoids
20210236460 · 2021-08-05 ·

The use of a medicament as a single agent, binary agent, or other combination comprising of substantially pure novel cannabinoids 1 and 2, optionally admixed with one or more known and novel cannabinoids and other known naturally occurring and synthetic tetracyclic 2A and tricyclic 1A cannabinoids for the prevention, treatment or cure of inflammatory mediated diseases or inflammatory mediated pathological conditions, anorexia, arthritis, cancer, pain, glaucoma, migraine, persistent muscle spasms, seizures (epileptic seizures), severe nausea, PTSD, autism spectrum disorder, drug abuse, insomnia, or any other chronic or persistent medical symptom.

Novel Cannabinoids and Cannabinoid Acids and Their Derivatives
20210238157 · 2021-08-05 ·

The present invention relates to novel cannabinoids 1 and 2, synthesized from simple starting materials using a cascade sequence of allylic rearrangement, aromatization and, for tetracyclic cannabinoids, further highly stereoselective and regioselective cyclization. These synthesized cannabinoids can more easily be obtained at high purity levels than cannabinoids isolated or synthesized via known methods. The cannabinoids 2 are obtained containing very low levels of isomeric cannabinoids such as the undesirable Δ8-tetrahydrocannabinol. The analogues with variation in aromatic ring substituents, whilst easily synthesized with the new methodology, would be much more difficult to make from any of the components of cannabis oil. Novel compounds of the formulas 3, 4, 5 and 6, as intermediates for the synthesis of the cannabinoids of the formulas 1 and 2 are also disclosed.

Novel Cannabinoids and Cannabinoid Acids and Their Derivatives
20210238157 · 2021-08-05 ·

The present invention relates to novel cannabinoids 1 and 2, synthesized from simple starting materials using a cascade sequence of allylic rearrangement, aromatization and, for tetracyclic cannabinoids, further highly stereoselective and regioselective cyclization. These synthesized cannabinoids can more easily be obtained at high purity levels than cannabinoids isolated or synthesized via known methods. The cannabinoids 2 are obtained containing very low levels of isomeric cannabinoids such as the undesirable Δ8-tetrahydrocannabinol. The analogues with variation in aromatic ring substituents, whilst easily synthesized with the new methodology, would be much more difficult to make from any of the components of cannabis oil. Novel compounds of the formulas 3, 4, 5 and 6, as intermediates for the synthesis of the cannabinoids of the formulas 1 and 2 are also disclosed.

Synthetic cannabinoid compounds for treatment of substance addiction and other disorders

A method of increasing the cannabinoid levels in a genetically modified Cannabis sativa plant includes genetically modifying the plant to induce the overexpression of the gene that controls the expression of tetrahydrocannabinolic acid (THCA) synthase and/or cannabidiolic acid (CBDA) synthase. The overexpression of THCA synthase and CBDA synthase catalyzes an increased synthesis of cannabigerolic acid to tetrahydrocannabinolic acid and cannabidiolic acid, as well as the cannabinoids (3aR)-2,4,4-trimethyl-7-pentyl-3,3a,4,9b-tetrahydrocyclopenta[c]chromen-9-ol and 2-((1R,5R)-3-methyl-5-(prop-1-en-2-yl)cyclopent-2-en-1-yl)-5-pentylbenzene-1,3-diol. Pharmaceutical compositions comprising the modified cannabinoids produced by the transgenic Cannabis sativa plant or prepared synthetically are used to treat various diseases and conditions.

METHOD FOR SEPARATING NATURAL SUBSTANCE MIXTURES BY MEANS OF SCPC
20210230206 · 2021-07-29 ·

The invention relates to a method for separating natural substance mixtures, in particular those consisting of plant extracts, and for isolating and purifying and obtaining same, by means of sequential centrifugal partition chromatography (sCPC).

METHOD FOR SEPARATING NATURAL SUBSTANCE MIXTURES BY MEANS OF SCPC
20210230206 · 2021-07-29 ·

The invention relates to a method for separating natural substance mixtures, in particular those consisting of plant extracts, and for isolating and purifying and obtaining same, by means of sequential centrifugal partition chromatography (sCPC).

Novel Labelled Cannabinergic Ligands and Related Analogs

Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.

Novel Labelled Cannabinergic Ligands and Related Analogs

Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.

Low molecular weight modulators of the cold menthol receptor TRPM8 and use thereof

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

Low molecular weight modulators of the cold menthol receptor TRPM8 and use thereof

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.