US 5,578,725 A · Delta opioid receptor antagonists

Abstract

Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.

Claims21

Dependent claims

A compound of the formula:

##STR5## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, (C.sub.6 -C.sub.12)aryl, trans(C.sub.4 -C.sub.5)alkenyl, allyl;
C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aralkyl or furan-2-ylalkyl, wherein alkyl is (C.sub.1 -C.sub.5)alkyl;
R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl;
R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, wherein alkyl is (C.sub.1 -C.sub.5)alkyl, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkylCO;
X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl;
R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is an integer of 1 to 5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2);
or a pharmaceutically acceptable salt thereof.

4 more elements

Dependencies are inferred from the claim text.

Delta opioid receptor antagonists

Life of this patent

Delta opioid receptor antagonists

Life of this patent

Abstract

Claims21