501426-50-2Relevant academic research and scientific papers
PYRAZOLE DERIVATES AS CANNABINOID RECEPTOR MODULATORS
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Page/Page column 23-24, (2010/11/25)
Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter alia in the treatment of obesity: (I) wherein A1 is hydrogen, -COOH, or tetrazolyl, and A2 is hydrogen, -COOH, tetrazolyl, -CN, -CF3, -COR6, -SO2R6, -OR7, -NR7R8, -NHCOR6, and -NR7SO2R8 provided that one of A1 and A2 is either -COOH or tetrazolyl; p is O or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is O or 1 ; R1 is a bond, or - (CH2)aB1(CH2)b- wherein a and b are independently O, 1 , 2 or 3 provided that a+b is not greater than 4, and B1 is -CO-, -0-, -S-, -SO-, -SO2-, -CH2-, -CHOH- or -NR7-; R2 is a bond, -(CH2)aB1 (CH2)b- or -[(CH2)aB1 (CH2)b]n-A4-[(CH2)cB2(CH2)d]m- wherein a, b, and B1 are as defined for R1; B2 is as defined for B1, c and d are independently 0,1 , 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently O or 1 and A4 is a monocarbocyclic or monoheterocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF3, C1-C4 alkyl, cycloalkyl, -OR9, oxo or -NR7R8; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, -CF3, -OR9, -NR7R8, -(CH2)SCOR6, -(CH2)SSO2R6, -(CH2)SNR7COR6, -(CH2)SNR7COOR8, -(CH2)SNR7SO2R6, wherein s is 1 , 2, 3 or 4; R4 and R5 independently -R9, -CN, -F, -Cl, -Br, -OR9, -NR7R8, -NR7COR6, -NR7SO2R6, -COR6, -SR9, -SOR9, -SO2R6, (C1-C4 alkyl)OR9, -(C1-C4 alkyl)NR7R8, -(C1-C4 alkyl)NR7COR6, C1-C4 alkyl)NR7COOR8, -(C1-C4 alkyl)NR7SO2R6, -(C1-C4 alkyl)COR6, -(C1-C4 alkyl)SO2R6, -NR7COOR8, or [N-(C1-C4 alkyl)]- tetrazolyl; R6 is C1-C4 alkyl, cycloalkyl, -CF3 or -NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl and R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl.
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: Development of central cannabinoid receptor ligands with lower lipophilicity
Katoch-Rouse, Reeti,Pavlova, Olga A.,Caulder, Tara,Hoffman, Alexander F.,Mukhin, Alexey G.,Horti, Andrew G.
, p. 642 - 645 (2007/10/03)
Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in the CNS. Current tracers are highly lipophi
