Neurotensin antagonist peptides process for their preparation and pharmaceutical compositions containing them

摘要

PCT No. PCT/FR95/00643 Sec. 371 Date Nov. 19, 1996 Sec. 102(e) Date Nov. 19, 1996 PCT Filed May 17, 1995 PCT Pub. No. WO95/32218 PCT Pub. Date Nov. 30, 1995The invention is directed to a compound of formula (I) in which R represents a hydroxyl, alkyloxy, phenylalkyloxy or -NH-CH2-COOH radical, R1 represents a hydrogen atom, an adamantylacetyl, adamantylcarbonyl, norbornylacetyl, norbornylphenoxycarbonyl, benzoyl, nicotinoyl, 4-phenylbenzoyl, 4-tert-butylbenzoyl or 2-pyrrolidinecarbonyl radical or a protective group for an amine functional group, R2 represents an Arg or Lys residue, R3 represents an Arg or Lys residue, R4 represents a Pro residue, m, n and p, which are the identical or different, represent a number equal to 0 or 1, R5 and R6 are identical and represent a hydroxyl or methoxy radical and R7 represents a hydrogen, chlorine, bromine or iodine atom or a nitro radical, or the compound wherein one or a number of peptide bonds between two amino acid residues are replaced by -CH2-NH bonds or the peptide bond between the R2 and R3 amino acid residues is replaced by a CH=CH bond, provided that when R1 is a hydrogen atom, then the sum of m+n+p is at least equal to 1. The invention is also directed to a pharmaceutical composition comprising the compound of formula I and the preparation of the compound.