N-acyl derivatives of dipeptides, their preparation and...

C - Chemistry – Metallurgy – 07 – K

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530/5.06

C07K 5/06 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1243017

ABSTRACT OF THE DISCLOSURE: The invention relates to novel N-acyl derivatives of dipeptides of the formula X-CO-L-Leu-NH-CH2-CO-R I, where X is a saturated cycloaliphatic hydrocarbon radical of 3 to 10 carbon atoms, indanyl or 1,2,3,4-tetrahydro- naphthyl, in which radicals the carbon atom which is bonded to the carbonyl group can also carry an amino group, or X is L-homoprolyl or a saturated or unsaturated 4-mem- bered, 5-membered or 6-membered heterocyclic ring system containing not more than 2 heteroatoms, and the hetero- cyclic structure may furthermore be fused to a benzene nucleus, and, where the heterocyclic structure contains nitrogen, it may also contain an oxo or a C1-C3-alkyl group, and R is C1-C5-alkoxy or a radical NR1R2, where R1 and R are identical or different and are each hydrogen or C1-C5-alkyl, but where X a) cannot be pyrrolidin-2-yl or 5-oxopyrrolidin-2-yl, b) cannot be cyclopentyl if R is amino or ethylamino, and c) cannot be 4-thiazolidinyl if R is amino, and its salts with physiologically tolerated acids. These new derivatives are useful for the therapy of disorders.

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