Disclosed are compounds having the formula:
##STR1##
where
R.sub.1 =H, C.sub.1 -C.sub.6 alkyl, cycloalkyl,
R.sub.2 =H, C.sub.1 -C.sub.6 alkyl, cycloalkyl
##STR2##
W=C.sub.n H.sub.2n-m --NH (n=1-6, m=0, 2, or 4),
##STR3##
Z=CONR.sub.8 (CH.sub.2).sub.n, CONR.sub.8 (CH.sub.2).sub.n CO,
P(CH.sub.3)OCHR.sub.8 OCOR.sub.9, SO.sub.2, SO.sub.2 (CH.sub.2).sub.n,
SO.sub.2 (CH.sub.2).sub.n CO, SO.sub.2 NR.sub.8 (CH.sub.2).sub.n, SO.sub.2
NR.sub.8 (CH.sub.2).sub.n CO, n=1-4
R.sub.4 =H, (CH.sub.2).sub.n OH, (CH.sub.2).sub.n OCOR.sub.10,
(CH.sub.2).sub.n NR.sub.10 R.sub.11, (CH.sub.2).sub.n CONR.sub.10
R.sub.11, n=0-4
R.sub.5 =H, (CH.sub.2).sub.n NR.sub.12 R.sub.13, n=0-4
R.sub.6 =H, (CH.sub.2).sub.n NR.sub.14 R.sub.15, n=0-4
R.sub.7 =H, C.sub.1 -C.sub.6 alkyl, cycloalkyl; R.sub.8 =H, C.sub.1
-C.sub.6 alkyl, cycloalkyl; R.sub.9 =H, C.sub.1 -C.sub.6 alkyl,
cycloalkyl;
R.sub.10 =H, C.sub.1 -C.sub.6 alkyl, cycloalkyl; R.sub.11 =H, C.sub.1
-C.sub.6 alkyl, cycloalkyl; R.sub.12 =H, C.sub.1 -C.sub.6 alkyl,
cycloalkyl;
R.sub.13 =H, C.sub.1 -C.sub.6 alkyl, cycloalkyl; R.sub.14 =H, C.sub.1
-C.sub.6 alkyl, cycloalkyl; R.sub.15 =H, C.sub.1 -C.sub.6 alkyl,
cycloalkyl
Dashed lines: optional; conformational constraint by (CH.sub.2).sub.n,
n=1-3, R'=H or O(.dbd.)
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.
Se divulgan los compuestos que tienen el fórmula: ## del ## STR1 donde R.sub.1 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl, R.sub.2 = H, C.sub.1 - C.sub.6 alkyl, ## del ## STR2 del cycloalkyl W=C.sub.n H.sub.2n-m --NH (n=1-6, m=0, 2, o 4), ## Z=CONR.sub.8 (CH.sub.2).sub.n, CONR.sub.8 (CH.sub.2).sub.n CO, P(CH.sub.3)OCHR.sub.8 OCOR.sub.9, SO.sub.2, SO.sub.2 (CH.sub.2).sub.n, SO.sub.2 (CH.sub.2).sub.n CO, SO.sub.2 NR.sub.8 (CH.sub.2).sub.n, SO.sub.2 NR.sub.8 (CH.sub.2).sub.n CO, n=1-4 del ## STR3 R.sub.4 = H, (CH.sub.2).sub.n OH, (CH.sub.2).sub.n OCOR.sub.10, (CH.sub.2).sub.n NR.sub.10 R.sub.11, (CH.sub.2).sub.n CONR.sub.10 R.sub.11, n=0-4 R.sub.5 = H, (CH.sub.2).sub.n NR.sub.12 R.sub.13, n=0-4 R.sub.6 = H, (CH.sub.2).sub.n NR.sub.14 R.sub.15, n=0-4 R.sub.7 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.8 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.9 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.10 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.11 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.12 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.13 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.14 = H, C.sub.1 - C.sub.6 alkyl, cycloalkyl; R.sub.15 = H, C.sub.1 - C.sub.6 alkyl, líneas discontinuas del cycloalkyl: opcional; constreñimiento del conformational por (CH.sub.2).sub.n, n=1-3, R'=H u O(.dbd.) así como las composiciones y los métodos de los productos farmacéuticos para el tratamiento del apego del nacrótico, la dependencia del nacrótico, la tolerancia del nacrótico, el síndrome relacionado nacrótico de la abstinencia, la adición de la nicotina y la obesidad basaron sobre eso.
