US 6,114,390 AGranted

Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them

AssigneeKarl Thomae GmbH

InventorsWolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim, Michael Entzeroth, Wolfgang Wienen

Life of this patent

Estimating the term…

patentgrep

Loading patent…

Abstract

NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate; (B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate; (C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate; (D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phe nyl]methyl]-argininamide-trifluoroacetate; (E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride; (F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate; (G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-ar gininamide-bis-(trifluoroacetate); and, (H) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl)phenyl]me thyl]-argininamide-trifluoroacetate.

Claims10

Dependent claims

A compound selected from the group consisting of:

(A) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide;
(B) (R,S)-N.sup.5 -(aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide;
(C) (R)-N-[[4-(aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide;
(D) (R)-N.sup.2 -(diphenylacetyl)-N-[[4-(methylaminocarbonylaminomethyl)phenyl]methyl]-arg ininamide;
(E) (R)-N.sup.2 -(diphenylacetyl)-N-[[4-(ethylaminocarbonylaminomethyl)phenyl]methyl]-argi ninamide;
(F) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-(4-methoxyphenyl)acetyl]-argininamide;
(G) (R)-N.sup.2 -(diphenylacetyl)-N-[[4-(ethoxycarbonylmethylaminocarbonylaminomethyl)phen yl]methyl]-argininamide;
(H) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-(4-fluorophenyl)acetyl]-argininamide;
(I) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-(4-chlorophenyl)acetyl]-argininamide;
(J) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-(4-hydroxyphenyl)acetyl]-argininamide;
(K) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-[4-(methoxycarbonylmethoxy)phenyl]acetyl]-argininamide;
and,
(L) (R)-N-[[4-(aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis-[4-(hydroxycarbonylmethoxy)phenyl]acetyl]-argininamide;
or a pharmaceutically acceptable salt thereof.

11 more elements

Dependencies are inferred from the claim text.

Facts

Application: 08/950,113Filed 14 Oct 1997 · continuation
Granted: 5 Sep 2000
Term ends: Not estimatedThe source records don’t support an estimate.

Classification30 codes

C07D 235/06
Benzimidazoles; Hydrogenated benzimidazoles: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in…
C07C 257/18
With replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines: having carbon atoms of amidino groups bound to…
C07C 275/24
Of an unsaturated carbon skeleton: containing six-membered aromatic rings
C07C 275/56
Y being a hydrogen or a carbon atom: x being a nitrogen atom