37 results about "Endogenous cannabinoid" patented technology

This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.

The present invention relates to a compound of the general formula (I) which is a non-hydrolysable analogue of endogenous cannabinoids, which are found to be more potent therapeutic agents as they are more stable, for example, to hydrolytic cleavage in the gastrointestinal tract. The cannabinoid analogues of the invention have a therapeutic value. Therefore, pharmaceutical compositions comprising as active ingredient a therapeutically effective amount of at least one compound of the invention may be prepared. Such compositions may be used as anti-inflammatory, anti-asthmatic, analgetic, hypotensive, antiemetic or anti-spasmodic compositions, and as compositions for treating and/or preventing glaucoma or migraine, or as compositions for relieving symptoms of multiple sclerosis and mood stimulating compositions.

A compound provided by the present invention includes an endocannabinoid, endocannabinoid derivative, or endocannabinoid analog moiety covalently bonded to a biologically active peptide. One example of an inventive compound described is a conjugate of an endocannabinoid, endocannabinoid derivative, or endocannabinoid analog moiety covalently coupled to an opioid peptide, such as an endorphin, enkephalin, dynorphin or endomorphin. Also detailed are processes for making the described conjugates and pharmaceutical compositions including such compounds.

The invention discloses a cannabinoid compound as well as a preparation method, a composition and application thereof. The invention discloses a compound shown as a formula I or a pharmaceutically acceptable salt thereof. The compound disclosed by the invention has medium-to-strong affinity to a cannabinoid receptor 1 or a cannabinoid receptor 2, and can be used as a potential therapeutic drug fortreating diseases and symptoms related to an endogenous cannabinoid system; , including but not limited to anorexia, vomiting, pain, epilepsy, spasm, Parkinson's disease, Alzheimer's disease, anxiety, depression, schizophrenia, or drug addiction.

A system and method for treating acute migraine events utilizing multiple sensory/receptive channels (olfactory, audio, visual and other sensory receptors) to both treat and optimize delivery to the afflicted sites in the brain. One of the primary migraine treatment methods includes a composition delivered through the olfactory system. Absorption through the nasal membranes is rapid and avoids delays and dilution inherent in methods using the mouth and gastro-intestinal (GI) processing. Effective, but less preferred methods that avoid GI delays and dilution include delivery as eyedrops or as an intravenous infusion. The effective composition comprises a caffeinic substance to bind and antagonize adenosine receptors in the brain. This immediately blocks continued action of adenosine to dilate the afflicted vessels and inflict pain. The composition also incorporates cannabinolic substances which work simultaneously or in parallel using the body's natural endocannabinoid pathways to rebalance and control blood flow to minimize swelling and pain. Additional features may incorporate additional active components. One available feature may incorporate a recipient/patient control modulus where the patient adjusts treatment using a feedback device such as a stimulation button to increase or adjust delivery. Another additional feature comprises one or more essential oils. Although some essential oil compositions may themselves include one or more compounds that contribute to the desired cannabinolic effects, adding essential oils even those lacking an inherent cannabinolic effect can contribute to effective treatment. Fragrant inclusions in an essential oil additive may provide a calming stimulation to the olfactory system that supports reduced tension and relaxation and thereby removes a tension induced exacerbation of migraine progression.

The invention discloses a carbamyl uracil derivative and application thereof. The structural formula of the derivative is as shown in the description. The derivative is a novel compound with the endogenous cannabinoid hydrolase inhibiting function, and a new method is provided for inflammation and pain treatment.

Provided is a highly potent and selective endocannabioid cellular reuptake inhibitor represented by formula (I):

or a pharmaceutically acceptable solvate or co-crystal thereof as well as to a formulation comprising this inhibitor, and to methods of treatment in which this inhibitor is used.

The invention provides a compound as shown by Formula I having an enzyme activity which can inhibit endocannabinoid hydrolases NAAA and/or FAAH, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and a preparation method and a use of the compound. ##STR00001##

The present invention provides a system enabling the oral delivery of therapeutics derived from polyunsaturated fatty acids (PUFAs), their metabolites and derivatives, including, eicosanoids, prostaglandins, prostacyclins, leukotrienes, resolvins, endocannabinoids, thromboxanes, epoxyeicosa-trienoic acids (EETs), hydroxyeicostetraenoic acids (HETEs), and CMX-020. The delivery system includes a vehicle comprising a purified docosahexaenoic acid (DHA) in triglyceride or ester form; a purified eicosapentaenoic acid (EPA) in triglyceride or ester form; a combination of DHA, EPA in either triglyceride or ester forms; or a modified DHA, EPA, or omega-3 fatty acid analog; and optionally, an antioxidant, a surfactant, a solubilizer, a stabilizer, a lubricant, or a pH/tonicity adjustment agent.

The invention relates to a Cannabis-based pharmaceutical composition for the treatment of hypertensive disorders by submucosal delivery comprising a pharmaceutically acceptable base and an effective amount of at least one cannabinoid or endocannabinoid containing extract of a cloned hybrid of the plant Cannabis sativa, subspecies sativa and Cannabis sativa, subspecies indica of the CTSX-ISS lineage; and methods of treatment of primary and secondary hypertension, the secondary hypertension resulting from pheochromocytoma, primary hyperaldosteronism, adrenal hyperplasia, pulmonary hypertension, portal hypertension, folate deficiency hypertension, arterial hypertension or familial hypertension by administration between one and eight times per day.

The present invention relates to ophthalmic compositions and methods for the treatment of dry eye and other inflammatory ocular conditions. In particular, the present invention relates to a composition comprising an esterified anti-inflammatory lipid mediator, which is an ester of an anti-inflammatory lipid mediator that is a reaction product of the anti-inflammatory lipid mediator and a polyol wherein the majority of the anti-inflammatory lipid mediator is present in an ester form. In this way, the compositions are substantially free of an acid form of the anti-inflammatory lipid mediators. Anti-inflammatory lipid mediators can be selected from the group consisting of polyunsaturated fatty acids (e.g., omega-three and omega-six fatty acids), resolvins or a metabolically stable analog, protectins or a metabolically stable analog, lipoxins or a metabolically stable analog, prostaglandins or a metabolically stable analog, retinoic acids, endocannabinoids, metabolites thereof, and mixtures thereof. This composition can be topically delivered to the ocular surface via a preparation, solution, gel, ointment, and/or strip and/or a contact lens.

A compound is provided that has the formula (II):

where R¹ in each occurrence is independently H, or C₁-C₄ alkyl; R² is a nullity or CH—CH₃, R³ is a nullity or C(O)—R⁶—NH; R⁶ is C₂-C₆ alkyl, (CH₂CH₂—O)_n, or (CH(OH)CH₂)_n; n is an integer of between 1 and 4; R⁴ is a nullity or NH—R⁶—C(O); and R⁵ is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, endocannabinoids 1 & 2, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptide transferrin, glucosyl ester, lactic acid, leucine, tryptophan, glutamic acid.

The invention relates to the technical field of novel medicinal application, and particularly relates to novel medicinal application of a CB2 receptor stimulant. An endocannabinoid signal system can be used for maintaining the energy balance and glucose homeostasis in a body; when fat and skeletal muscle cells are subjected to glucose deprivation, the messenger-ribonucleic acid (RNA) expression profile of the signal system changes, and ECS has the effects of mediating insulin resistance and regulating diabetes mellitus, obesity and other metabolic diseases. Animal tests of SER 601 in the CB2 receptor stimulant prove that the CB2 receptor stimulant has a remarkable effect for improving pancreas islet function, improving insulin sensitivity and improving accumulation of whole body fat, especially abdominal fat. The CB2 receptor stimulant can be used for reducing the content of fat in a body while improving the insulin sensitivity, preventing/treating diabetes mellitus patients, especially patients with type 2 diabetes mellitus, and preventing /treating obesity, lipodystrophy, weight and fat reduction and other diseases.

Regulation of striatal indirect pathway endocannabinoid-mediated long-term depression (eCB-LTD) is used to improve motor deficits of striatal-based brain disorders. In such treatment, a dopamine D2 receptor agonist is administered in conjunction with an inhibitor of endocannabinoid degradation. In some embodiments, the inhibitor of endocannabinoid degradation is a fatty acid amine hydrolase inhibitor, or a monoacylglycerol lipase antagonist. The combination provides for a synergistic effect, with improved therapeutic effects. Also provided are kits and systems for practicing the subject methods, as well as methods of use of agents identified in the screening method of the invention.

The present invention relates to high affinity compounds, able to bind CB₁ and CB₂ endocannabinoid receptors. The compounds of the invention find particular application as agents for pain therapy and/or anti-inflammatory and/or anti-stress and/or anti-oxidising and/or hypotensive and/or immune suppressive therapy and/or anti-spastic activity in multiple sclerosis and/or anti-cancer.