Disclosed are compounds having the formula:
##STR1##
where
- R1=H, C1-C6 alkyl, cycloalkyl,
##STR2##
- R2=H, C1-C6 alkyl, cycloalkyl
- W=CnH2n-m—NH (n=1-6, m=0, 2, or 4),
##STR3##
- X=
##STR4##
- R3=
##STR5##
- Y=
##STR6##
- Z=CONR8(CH2)n, CONR8(CH2)nCO,
P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n,
SO2(CH2)nCO, SO2NR8(CH2)n,
SO2NR8(CH2)nCO, n=1-4
- R4=H, (CH2)nOH, (CH2)nOCOR10,
(CH2)nNR10R11, (CH2)nCONR10R11, n=0-4
- R5=H, (CH2)nNR12R13, n=0-4
- R6=H, (CH2)nNR14R15, n=0-4
- R7=H, C1-C6 alkyl, cycloalkyl; R8=H,
C1-C6 alkyl, cycloalkyl; R9=H, C1-C6
alkyl, cycloalkyl;
- R10=H, C1-C6 alkyl, cycloalkyl; R11=H,
C1-C6 alkyl, cycloalkyl; R12=H, C1-C6
alkyl, cycloalkyl;
- R13=H, C1-C6 alkyl, cycloalkyl; R14=H,
C1-C6 alkyl, cycloalkyl; R15=H, C1-C6
alkyl, cycloalkyl.
Dashed lines: optional; conformational constraint by (CH2)n,
n=1-3, R=H or O() as well as pharmaceuticals compositions and methods
for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate
related abstinence syndrome, nicotine addition and obesity based thereon.
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