Amino acid derivatives, medicaments containing said compounds an

Details Amino acid derivatives, medicaments containing said compounds an Amino acid derivatives, medicaments containing said compounds an

1998-05-29

2000-03-21

Kunz, Gary L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

564123, A61K 3800, A01N 3718

Patent

active

06040289&

DESCRIPTION:

BRIEF SUMMARY
The invention relates to new amino acid derivatives of general formula ##STR2## which have NPY-antagonistic properties, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
Amino acid derivatives with NPY-antagonistic properties have already been described in WO 94/17035.
In general formula I above heteroaromatic ring linked via a carbon atom and containing a nitrogen, oxygen or sulphur atom or a nitrogen atom and an oxygen, sulphur or further nitrogen atom, whilst a nitrogen atom of an imino group may be substituted by an alkyl, alkoxycarbonylalkyl, carboxyalkyl, dialkylaminoalkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or alkoxycarbonyl group, or a 6-membered heteroaromatic ring linked via a carbon atom, containing 1, 2 or 3 nitrogen atoms, whilst a 1,4-butadienylene group may be attached both to the 5-membered and to the 6-membered heteroaromatic rings via two adjacent carbon atoms and the bicyclic heteroaromatic rings thus formed may also be bound via a carbon atom of the 1,4-butadienylene group and heteroaromatic rings in their carbon skeleton, may additionally be mono-, di- or at most trisubstituted by fluorine, chlorine or bromine atoms, by alkyl groups, cycloalkyl groups with 3 to 8 carbon atoms, alkoxy, phenyl, phenylalkoxy, trifluoromethyl, alkoxycarbonylalkyl, carboxyalkyl, dialkylaminoalkyl, hydroxy, amino, acetylamino, propionylamino, benzoyl, benzoylamino, benzoylmethylamino, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, cyano, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulphynyl or trifluoromethylsulphonyl groups, whilst the substituents may be identical or different and the abovementioned benzoyl, benzoylamino and benzoylmethylamino groups in turn may additionally be substituted in the phenyl moiety by a fluorine, chlorine or bromine atom, an alkyl, trifluoromethyl, amino or acetylamino group, disubstituted by fluorine, chlorine or bromine atoms, methyl, methoxy, hydroxycarbonylmethoxy, alkoxycarbonylmethoxy, hydroxy or trifluoromethyl groups, whilst the substituents in each case may be identical or different, containing 2 to 5 carbon atoms, which may be substituted in the alkyl moiety by an alkoxycarbonyl or phenylalkoxycarbonyl group, by a phenyl group or by a 5- or 6-membered heteroaromatic ring linked via a carbon atom, or a benzoyl group, wherein the phenyl moiety may also be replaced by a 5- or 6-membered heteroaromatic ring linked via a carbon atom, whilst the 5-membered heteroaromatic rings mentioned hereinbefore may contain a nitrogen, an oxygen or a sulphur atom or a nitrogen atom and an additional oxygen, sulphur or further nitrogen atom and may also be substituted by an alkyl group at a nitrogen atom, the 6-membered heteroaromatic rings may contain 1, 2 or 3 nitrogen atoms, and the phenyl groups mentioned hereinbefore may additionally be mono-, di- or at most tri-substituted, as may the heteroaromatic rings in their carbon skeleton, by fluorine, chlorine or bromine atoms, by alkyl groups, cycloalkyl groups with 3 to 8 carbon atoms, alkoxy, trifluoromethyl, alkoxycarbonylalkyl, carboxyalkyl, hydroxy, amino, acetylamino, propionylamino, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, cyano, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulphynyl or trifluoromethylsulphonyl groups, whilst the substituents may be identical or different, nitrogen atom by alkyl, phenylalkyl, (1-naphthyl)alkyl, (2-naphthyl)alkyl, alkoxycarbonylalkyl, phenylalkoxycarbonylalkyl, phenoxycarbonylalkyl, carboxyalkyl, diphenylalkyl, phenyl, cycloalkyl or cycloalkylalkyl groups with 3 to 8 carbon atoms in the ring in each case, whilst the substituents may be identical or different and the abovementioned phenyl groups may in turn, independently of one another, be mono- or disubstituted by fluorine, chlorin

REFERENCES:
patent: 5616620 (1997-04-01), Rudolf et al.
patent: 5807875 (1998-09-01), Klaus et al.
Interactions of derivatives of guanidinophenylglycine and guanidinophenylalanine with trypsin and related enzymes. Tsunematsu, H. et al. J. Biochem. 88, 1773-1783 (1980).
Interactions of derivatives of guanidinophenylalanine and guanidinophenylglycine with streptomyces griseus trypsin. Hatanaka, Y. et al, Biochimica et Biophysica Acta 822 (1985) 274-279.
Beta-Napthylamides of Guanidinophenyl amino acids as substrates of aminopeptidases. Tsunematsu, H. et al. Chem. Pharm. Bull. 36(3) 1205-1209 (1988).

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