Commissariat a L'energie Atomique

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Commissariat &#xc0; L'&#xc9;nergie Atomique Et Aux &#xc9;nergies Alternatives

Les Laboratoires Servier

Vincent Dive

Athanasios Yiotakis

Flavio Toma

Fabrice Beau

Philippe Cuniasse

Bertrand Czarny

Pierre Corvol

Bertrand Tavitian

Paul Basset

Elizabeth Scalbert

Marie-Christine Rio

André Menez

Joël Cotton

Anastasios Makaritis

Jiri Jiracek

Laurent Devel

Jo&euml;l Menard

Annie Michaud

Eric Ezan

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

Jo&euml;l Cotton

Stamania Vassiliou

Sarah Bregant

Athanasios Yotakis

Dimitri Georgiadis

Nicolas Jullien

Marie-Claire Nevers

The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.

Pseudodipeptides as MMP inhibitors

The invention relates to an amplification-free method of screening groups of radioactive molecules, comprising at least the following steps: (1) the group of molecules is administered to at least one animal; (2) at least one of the animals is slaughtered and the tissue distribution of the radioactivity of the molecules administered is analyzed in vivo; (3) sections of tissue or organs in which a radioactivity signal is detected are selected; (4) radioactive fractions from the sections of tissue or organs are isolated using suitable techniques such as chromatography and/or extraction techniques; and (5) the molecule(s) from the radioactive fractions obtained in step 4 are characterized using suitable analysis techniques such as chromatography and/or mass spectrometry.

Method of screening groups of radioactive molecules and applications thereof

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

The invention relates to the use of phosphinic pseudopeptide derivatives for production of a medicament for selectively inhibiting the active C-terminal site of angiotensin I converting enzyme. These derivatives are of formula (II): where, Rmay be a protecting group for amino functions usually used in peptide chemistry or an amino acid or a peptide protected by the above type of protecting groups, Rand Rcorrespond to a natural or unnatural amino acid side chain and Rand Rrepresent a hydrogen atom or a counterion.

Phosphinic pseudopeptide derivatives for the selective inhibition of the C-terminal active site of angiotensin I converting enzyme (ACE)

Phosphinic pseudo-peptides that may be used as matrix zinc metalloprotease inhibitors

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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Palaiseau, France

Vincent Dive