158941-22-1Relevant academic research and scientific papers
The structure of two pyrazole esters related to Rimonabant
Alkorta, Ibon,Goya, Pilar,Pérez-Fernández, Ruth,Alvarado, Mario,Elguero, José,García-Granda, Santiago,Menéndez-Taboada, Laura
, p. 10 - 15 (2009)
Two 1,5-diarylpyrazoles related to the antiobesity agent Rimonabant have been synthesized and their structure determined by X-ray crystallography. Compound 2, 1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxy late, forms strange cry
Synthesis, Spectral Studies and Tritiation of the Cannabinoid Antagonist SR141716A
Seltzman, Herbert H.,Carroll, F. Ivy,Burgess, Jason P.,Wyrick, Christopher D.,Burch, David F.
, p. 1549 - 1550 (1995)
An efficient synthesis of the cannabinoid antagonist SR141716A is presented and the structure is established by nOe experiments; tritiated SR141716A is synthesized by a novel sequence of metallation-iodination-tritiation and the labelled site is shown by tritium NMR and tritium-hydrogen nOe experiments.
Synthesis of novel pyrazole derivatives incorporating one dicarba-closo-dodecaborane unit
Vázquez, Naiara,Gómez-Vallejo, Vanessa,Llop, Jordi
, p. 4743 - 4746 (2012)
Boron clusters, and especially dicarba-closo-dodecaboranes, can be used as hydrophobic pharmacophores in the design of new drugs. In the current letter, analogs of the CB1 receptor inverse agonist Rimonabant incorporating a carborane cage (either ortho- o
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”.
Process for Making Biologically Active Compounds and Intermediates Thereof
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, (2022/02/05)
A process of manufacturing biologically active compounds, their analogs, pharmaceutically acceptable salts, solvates, polymorphs, isotopic variants, and intermediates thereof. Notably, the compounds of the formula IA, 1B, 1C. 1D. 1E, 1F and IG for which novel processes have been disclosed, selectively act on the cannabinoid receptors, and with high affinity. The processes for the preparation of the compounds enable the syntheses of cannabinoid modulators on a large-scale that are eco-friendly and economically viable. Additionally, the processes disclosed enable the synthesis of cannabinoid modulators with high purity and in high yield for their use in making drug substance and drug products.
Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effects
Hendawy,Gomaa, Hesham A.M.,Alzarea, Sami I.,Alshammari, Mutariah S.,Mohamed, Fatma A.M.,Mostafa, Yaser A.,Abdelazeem, Ahmed H.,Abdelrahman, Mostafa H.,Trembleau, Laurent,Youssif, Bahaa G.M.
, (2021/09/01)
COX-2 selective drugs have been withdrawn from the market due to cardiovascular side effects, just a few years after their discovery. As a result, a new series of 1,5-diaryl pyrazole carboxamides 19–31 was synthesized as selective COX-2/sEH inhibitors wit
MMPL3 INHIBITORS, COMPOSITIONS AND USES THEREOF
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Paragraph 0176; 0177, (2020/06/10)
Disclosed are inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof.
Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes
Grant, Phillip S.,Kahlcke, Nils,Govindpani, Karan,Hunter, Morag,MacDonald, Christa,Brimble, Margaret A.,Glass, Michelle,Furkert, Daniel P.
supporting information, (2019/10/02)
The cannabinoid-1 receptor (CB1R) inverse agonist SR141716A has proven useful for study of the endocannabinoid system, including development of divalent CB1R ligands possessing a second functional motif attached via a linker unit. These have predominantly employed the C3 position of the central pyrazole ring for linker attachment. Despite this precedent, a novel series of C3-linked CB1R-D2R divalent ligands exhibited extremely high affinity at the D2R, but only poor affinity for the CB1R. A systematic linker attachment point survey of the SR141716A pharmacophore was therefore undertaken, establishing the C5 position as the optimal site for linker conjugation. This linker attachment survey enabled the identification of a novel divalent ligand as a lead compound to inform ongoing development of high-affinity CB1R molecular probes.
FUSED PYRAZOLE COMPOUNDS AS CB1R ANTAGONISTS AND USES THEREOF
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Page/Page column 75, (2015/11/03)
The present invention relates to compounds of formula I, or isotopic forms, stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, S-oxides or N- oxides thereof, and processes for their preparation. The invention furt
SUBSTITUTED PYRAZOLE COMPOUNDS AS CB1 RECEPTOR ANTAGONISTS AND USES THEREOF
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Page/Page column 69; 70, (2015/11/16)
The present invention relates to compounds of formula 1, or isotopic forms, stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, S-oxides or N-oxides thereof, and processes for their preparation. The invention furth
