501423-63-8Relevant 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”.
"One-poto" synthesis of 4-substituted 1,5-diaryl-1H-pyrazole-3- carboxylic acids via a MeONa/LiCl-mediated sterically hindered claisen condensation-Knorr reaction-hydrolysis sequence
Jiang, Jian-An,Du, Cai-Yan,Gu, Chun-Hui,Ji, Ya-Fei
supporting information, p. 2965 - 2968 (2013/02/22)
A "one-poto" synthesis of 4-substituted 1,5-diaryl-1H-pyrazole-3- carboxylic acids was first reported in moderate to good yields. This concise procedure, featuring efficiency and green chemistry, was composed of MeONa/LiCl-mediated sterically hindered Claisen condensation, Knorr reaction and hydrolysis. Georg Thieme Verlag KG · Stuttgart · New York.
A method for parallel solid-phase synthesis of Lodinated analogues of the CB1 receptor inverse agonist rimonabant
Spivey, Alan C.,Tseng, Chih-Chung,Jones, Teyrnon C.,Kohler, Andrew D.,Ellames, George J.
supporting information; experimental part, p. 4760 - 4763 (2009/12/27)
A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor Inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin Is stable to the diversification conditions but allows ipsoiododegermylative cleavage using Nal/NCS even for the products containing the oxidatively labile hydrazide moiety.