Peptide derivatives, their preparation process and their pharmac

Details Peptide derivatives, their preparation process and their pharmac Peptide derivatives, their preparation process and their pharmac

1983-12-15

1985-07-23

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125R, A61K 3700, C07C10352

Patent

active

045308373

ABSTRACT:
The invention relates to novel peptide derivatives, their preparation process and their pharmaceutical use.
These derivatives are in accordance with the following formula: ##STR1## in which A stands for hydrogen, a radical derived from an amino acid, a group of formula DE in which D represents the N-t-butyloxycarbonyl (BOC), tertamyl-oxycarbonyl (tAOC), N-benzyloxycarbonyl, N-benzoyl, N-acetyl, N-pivaloyl, N-carbamoyl, or N-succinyl radical, and E stands for a single bond or a radical derived from an amino acid which is either not substituted or substituted by HSO.sub.3 or a peptide formed from 2 to 5 amino acids, either unsubstituted or substituted by HSO.sub.3 ; B represents the L-methyonyl, D-methionyl, L-norleucyl, D-nodeucyl, L-leucyl, D-leucyl, L-norvalyl or D-norvalvyl radical; Y represents H, CH.sub.2 OH, COOR.sup.1 with R.sup.1 representing hydrogen or an allyl radical in C.sub.1 and C.sub.4 or CO--NHR.sup.2 with R.sup.2 representing hydrogen, an alkyl radical in C.sub.1 and C.sub.4 or NH.sub.2 ; m is an integer between 0 and 6 and X represents an amino derivative having at least 5 carbon atoms and a pentagonal unsaturated heterocycle.
They are usable as antagonists of gastrin and histamine.

REFERENCES:
patent: 4012367 (1977-03-01), Mazur
patent: 4164571 (1979-08-01), Bonfils et al.
E. Gross, et al., The Peptides, vol. I (1979), pp. 80 & 89.

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