Amino acid derivatives and their use as antidepressives and hypotensive agents
OwnerBernard Roques, Jean-Charles Schwartz +1inventors
InventorsBernard Roques, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Abstract
Derivatives having the general formula: ##STR1## in which the various radicals, A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.
Claims8
An amino acid derivative of the formula ##STR65## wherein R.sub.1 is phenyl optionally mono- or polysubstituted with halogen;
- R.sub.2 is hydrogen or methyl;
- Z is --(CH.sub.2)-- or .dbd.(CH)--;
- p is 0 when Z is .dbd.(CH)-- and 1 when Z is --(CH.sub.2);
- R.sub.3 is hydroxy;
- C.sub.1-4 alkoxy optionally mono-substituted with halogen;
- phenyl C.sub.1-4 alkoxy whose phenyl group is optionally substituted with halogen;
- C.sub.1-6 alkyl amino;
- phenyl C.sub.1-4 alkyl amino whose phenyl group is optionally mono-substituted with halogen;
- X is disubstituted aminomethyl of the formula ##STR66## in which R" is hydrogen, benzyl, benzoyl or C.sub.1-4 alkoxy carbonyl and R"' is hydrogen, methyl, benzyl, fluorobenzyl or trifluoroethyl.
An amino acid derivative of the formula ##STR68## wherein R.sub.1 is phenyl optionally mono-substituted with halogen;
- R.sub.2 is hydrogen or methyl;
- Z is --(CH.sub.2)-- or .dbd.(CH)--;
- p is 0 when Z is .dbd.(CH)-- and 1 when Z is --(CH.sub.2);
- R.sub.3 is hydroxy;
- C.sub.1-4 alkoxy optionally mono-substituted with halogen;
- C.sub.1-4 alkoxy substituted with dialkylamino in which the alkyl groups contain 1-4 carbon atoms;
- phenyl C.sub.1-4 alkoxy whose phenyl group is optionally substituted with halogen;
- C.sub.1-6 alkyl amino;
- phenyl C.sub.1-4 alkyl amino whose phenyl group is optionally mono-substituted with halogen;
- X is monosubstituted carbamoylmethyl of the formula --CH.sub.2 --CO--NH--OR" in which R" is benzyl, benzoyl or C.sub.1-4 alkoxy carbonyl.
An amino acid derivative of the formula ##STR70## wherein R.sub.1 is hydrogen;
- C.sub.1-4 alkyl;
- phenyl optionally mono-substituted with halogen;
- or indolyl;
- R.sub.2 is hydrogen;
- methyl;
- or alkyl optionally substituted with indolyl;
- Z is --(CH.sub.2)-- or .dbd.(CH)--;
- p is 0 when Z is .dbd.(CH)-- and 1 when Z is --(CH.sub.2)--;
- R.sub.3 is hydroxy;
- C.sub.1-4 alkoxy optionally mono-substituted with halogen;
- phenyl C.sub.1-4 alkoxy whose phenyl group is optionally substituted with halogen;
- C.sub.1-6 alkyl amino;
- or phenyl C.sub.1-4 alkyl amino whose phenyl group is optionally mono-substituted with halogen;
- X is disubstituted aminomethyl of the formula ##STR71## or a mono- or disubstituted carbamoylmethyl of the formula ##STR72## in which R" is hydrogen, benzyl, benzoyl or C.sub.1-4 alkoxy carbonyl, R"' is hydrogen, methyl, benzyl fluorobenzyl or trifluoroethyl, and R.sub.4 is benzyl, benzoyl or C.sub.1-4 alkoxy carbonyl.
An amino acid derivative of the formula ##STR75##
Dependencies are inferred from the claim text.