796875-23-5Relevant articles and documents
Compounds for Treating Cannabinoid Toxicity and Acute Cannabinoid Overdose
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, (2022/02/11)
The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as Δ9-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.3]heptanes with unique pharmacokinetic and pharmacodynamic properties for treating “Acute Cannabinoid Overdose”.
Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists
Kim, Jong Yup,Seo, Hee Jeong,Lee, Sung-Han,Jung, Myung Eun,Ahn, Kwangwoo,Kim, Jeongmin,Lee, Jinhwa
scheme or table, p. 142 - 145 (2009/05/30)
Since the CB1 receptor antagonist SR141716 (rimonabant) was reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target in the treatment of obesity. Several series of derivatives based on diarylimidazolyl oxadiazole an
Bioisosteric replacements of the pyrazole moiety of rimonabant: Synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists
Lange, Jos H. M.,Van Stuivenberg, Herman H.,Coolen, Hein K. A. C.,Adolfs, Tiny J. P.,McCreary, Andrew C.,Keizer, Hiskias G.,Wals, Henri C.,Veerman, Willem,Borst, Alice J. M.,De Looff, Wouter,Verveer, Peter C.,Kruse, Chris G.
, p. 1823 - 1838 (2007/10/03)
Series of thiazoles, triazoles, and imidazoles were designed as bioisosteres, based on the 1,5-diarylpyrazole motif that is present in the potent CB1 receptor antagonist rimonabant (SR141716A, 1). A number of target compounds was synthesized an