784181-20-0

Upstream product

• 681178-99-4 ethyl 1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-1 H-pyrazole-3-carboxylate 

Downstream Products

• 784181-21-1 1-(2-Chloro-phenyl)-5-(4-chloro-phenyl)-4-(isopropylamino-methyl)-1H-pyrazole-3-carboxylic acid ethyl ester 
• 913368-47-5 1-(2-chloro-phenyl)-5-(4-chloro-phenyl)-4-[(2-ethoxycarbonyl-ethylamino)-methyl]-1H-pyrazole-3-carboxylic acid ethyl ester 
• 1034266-31-3 5-(4-chloro-phenyl)-1-(2-chloro-phenyl)-4-cyanomethyl-1H-pyrazole-3-carboxylic acid 
• 917081-51-7 C₂₀H₁₅Cl₂N₃O₂ 
• 1174629-11-8 ethyl 1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-hydroxymethyl-1H-pyrazole-3-carboxylate 

Relevant academic research and scientific papers

Exploring SAR features in diverse library of 4-cyanomethyl-pyrazole-3-carboxamides suitable for further elaborations as CB1 antagonists

A chemically diverse library of secondary and tertiary 4-cyanomethyl-1,5-diphenyl-1H-pyrazole-3-carboxamides was synthesized to enable mapping of the SAR, in the eastern amide region, with regard to CB1 antagonist activity, This study was initiated as a prelude to the design and synthesis of possible CB1 antagonists that do not readily pass the blood-brain-barrier. In general a range of modifications were found to be tolerated in this part of the molecule, although polar and especially charged groups did to a degree reduce the CB1 antagonistic activity. Several compounds with single-digit or even sub-nanomolar potency, suitable for further elaboration of the nitrile moiety, were identified.

Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand

Numerous research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, proved to be efficacious in human for the treatment of obesity. In the present study, a series of 1,2,4-triazole-containing diarylpyrazolyl carboxamides based on the 1,5-diarylpyrazole template of rimonabant, was synthesized and tested for CB1 receptor binding affinity. The structure-activity relationship studies demonstrated that incorporation of 1,2,4-triazole ring onto the pyrazole scaffold via a methylene linker led to a significant improvement for CB1 receptor binding affinity. Importantly, these analogues also exhibited excellent selectivity for CB1 receptor over CB2 receptor.

CANNABINOID RECEPTOR MODULATORS

Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein:X is a bond, or a divalent radical selected from -C(R10)(R11)-*, -C(R10)(R11)

FUSED PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS

The present invention relates to novel cannabinoid receptor modulators of formula (I), in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabi

CB1 RECEPTOR MODULATORS

Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention

Acylaminobicyclic heteroaromatic compounds and uses thereof

Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.

Cannabinoid receptor ligands and uses thereof

Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.