Patent application number | Description | Published |
20090035219 | CB1 receptor antagonists and uses thereof - Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects. A method of detecting a neutral CB1 cannabinoid receptor antagonist, including identifying a candidate compound; subjecting the candidate compound to one or more of a cAMP assay, CB1 competitive binding assay, food intake assay, thermoregulation assay, or emesis assay; and selecting the compound if it exhibits neutral antagonist activity. | 02-05-2009 |
20090163557 | Cannabinergic Lipid Ligands - One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect. | 06-25-2009 |
20090306016 | FATTY ACID AMIDE HYDROLASE INHIBITORS - Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1i and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors. Thus, the compound may not directly modulate the cannabinoid receptors but has the effect of indirectly stimulating the cannabinoid receptors by increasing the levels of endocannabinoid ligands. It may also enhance the effects and duration of action of other exogenous cannabinergic ligands that are administered in order to elicit a cannabinergic response. | 12-10-2009 |
20100063050 | NOVEL HETEROPYRROLE ANALOGS ACTING ON CANNABINOID RECEPTORS - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect. | 03-11-2010 |
20100234379 | Dual modulation of endocannabinoid transport and fatty-acid amide hydrolase for treatment of excitotoxicity - The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury. | 09-16-2010 |
20100261674 | THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS - Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy. | 10-14-2010 |
20110039874 | MONOACYLGLYCEROL LIPASE INHIBITORS FOR MODULATION OF CANNABINOID ACTIVITY - Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. | 02-17-2011 |
20110071178 | Methods and Compounds for Modulating Cannabinoid Activity - Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. | 03-24-2011 |
20110166138 | Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors - Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors. | 07-07-2011 |
20120046280 | NOVEL HETEROPYRROLE ANALOGS ACTING ON CANNABINOID RECEPTORS - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed. | 02-23-2012 |
20120095047 | Novel Heteropyrrole Analogs Acting on Cannabinoid Receptors - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect. | 04-19-2012 |
20120172339 | ANGIOGENIC RESORCINOL DERIVATIVES - Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions. | 07-05-2012 |
20130041037 | THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS - Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy. | 02-14-2013 |
20130123229 | CB1 Receptor Antagonists and Uses Thereof - Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects. A method of detecting a neutral CB1 cannabinoid receptor antagonist, including identifying a candidate compound; subjecting the candidate compound to one or more of a cAMP assay, CB1 competitive binding assay, food intake assay, thermoregulation assay, or emesis assay; and selecting the compound if it exhibits neutral antagonist activity. | 05-16-2013 |
20130289082 | Composition and Method for Treating a Neurodegenerative Event - Disclosed is an article of manufacture featuring a support with a therapeutically effective amount of at least one fatty acid amide hydrolase (FAAH) inhibitor therein. The article has several uses and advantages including use to increase levels of at least one neurotrophin in a subject in need of such treatment. Also disclosed is a method of increasing levels of the neurotrophin in an animal by administering to a subject in need thereof at least one FAAH inhibitor. | 10-31-2013 |