917080-41-2Relevant academic research and scientific papers
PYRAZOLE DERIVATES AS CANNABINOID RECEPTOR MODULATORS
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Page/Page column 20-21, (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.
