Commissariat a L'energie Atomique

Other

Les Laboratoires Servier

Athanasios Yiotakis

Vincent Dive

Flavio Toma

Pierre Corvol

Elizabeth Scalbert

Philippe Cuniasse

Marie-Th&eacute;r&egrave;se Chauvet

Eric Ezan

Annie Michaud

Anastasios Makaritis

Jo&euml;l Menard

Jiri Jiracek

Nicolas Jullien

Jo&euml;l Cotton

Compounds of formula (I): wherein: Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.

Phosphinic amino acid compounds

N-terminal site selective inhibitors of human angiotensin conversion enzyme (ACE)

Peptide derivatives usable as zinc endopeptidase 24-15 inhibitors. These peptide derivatives have the following amino acid sequence:

Peptide derivatives usable as zinc endopeptidase 24-15 inhibitors

The invention relates to the use of peptide derivatives for the preparation of medicaments inhibiting endopeptidases 24.15 and 24.16. These peptide derivatives are in accordance with the formula: ##STR1## in which R.sup.1 is an optionally substituted aralkyl group, R.sup.2 is Pro, Hyp, thiazolidine or dehydroproline, R.sup.3 is H or an alkyl radical, R.sup.4 is an alkyl group or the side chain of an amino acid, R.sup.5 and R.sup.6 can be H, NH.sub.4 + or metals and R.sup.7 is H or CH.sub.3. N-(phenylethylphosphonyl)-Gly-Pro-aminohexanoic acid and N-(phenylethyl phosphonyl)-Ala-Pro-aminohexanoic acid are examples of effective derivatives.

Use of peptide derivatives for the preparation of medicaments inhibiting

The invention relates to novel peptide derivatives usable as inhibitors of bacterial collagenases. These derivatives comply with the formula: ##STR1## in which R.sup.1 is a hydrogen atom, a blocking group or a radical derived from an amino acid or a peptide optionally protected by a blocking group, R.sup.2 is the side chain of an .alpha.-amino acid, R.sup.3 is H, a metal, an alkyl or benzyl group, R.sup.4 is the derivative of proline, hydroxyproline, thiazolidine or dehydroproline, R.sup.5 is H or an alkyl, R.sup.6 is the side of an amino acid and R.sup.7 is OR.sup.8 with R.sup.8 being H, a metal, alkyl or benzyl, or in which R.sup.1 and R.sup.7 together form a divalent radical derived from an amino acid or a peptide. The derivatives in which R.sup.3 is a metal or hydrogen are usable as inhibitors of bacterial collagenases.

Derivatives of peptides usable as inhibitors of bacterial collagenases

The invention relates to novel derivatives of peptides usable as inhibitors of bacterial collagenases. These derivatives comply with the formula: ##STR1## in which R.sup.1 is an optionally substituted aryl or aralkyl group or the group ##STR2## with R.sup.6 being the side chain of an .alpha.-amino acid and R.sup.7 R.sup.8 a protective group or a radical derived from an amino acid or a protected peptide, R.sup.2 is derived from proline, hydroxyproline, thiazolidine or dehydroproline, R.sup.3 is H or an alkyl, and R.sup.4 is the side chain of an amino acid and R.sup.5 and R'.sup.5 are H, a metal, an alkyl or benzyl. The derivatives in which R'.sup.5 is a metal or hydrogen can be used as inhibitors of bacterial collagenases.

Phosphonic peptide inhibitors of bacterial collagenases

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Athens, Greece

Athanasios Yiotakis