Abstract: The present invention relates to a method that allows to detect the active form of a specific matrix metalloproteinase and its use in diagnostic methods.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, alkylcarbonyloxyalkyl or alkylcarbonylthioalkyl, R2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl or optionally substituted arylalkyl, R3 represents phenyl, which is optionally substituted, or indolyl, their isomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.

Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, alkylcarbonyloxyalkyl or alkylcarbonylthioalkyl, R2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl or optionally substituted arylalkyl, R3 represents phenyl, which is optionally substituted, or indolyl, their isomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.

Abstract: The invention relates to an amplification-free method of screening groups of radioactive molecules, the products from the molecule groups obtained and the application thereof in order to identify molecules that are capable of binding selectively to a tissue or a particular organ. The inventive method can be used for the development of novel therapeutic compounds and contrast agents for medical imaging and for the screening of medicaments.

Abstract: 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, R1 may 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, R2 and R3 correspond to a natural or unnatural amino acid side chain and R4 and R5 represent a hydrogen atom or a counterion.

Abstract: 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, R1 may 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, R2 and R3 correspond to a natural or unnatural amino acid side chain and R4 and R5 represent a hydrogen atom or a counterion. Applications: prevention and treatment of cardiovascular diseases in humans.

Abstract: The invention relates to pseudo-peptides according to the formula: wherein R1 is a group inhibiting an amine function, or an amino acid residue or peptide with an inhibited terminal amino function, R2 represents the lateral chain of a natural or non-natural amino acid, R3 represents: 1) the lateral chain of a natural amino acid except for Gly and Ala, not substituted or substituted by an aryl group, 2) an aralkyl group, or 3) an alkyl group comprising at least 3 carbon atoms, and R4 represents a lateral chain of natural or non-natural amino acid. They are useful as matrix zinc metalloprotease inhibitors, particularly in the treatment of cancer.

Abstract: The invention relates to peptide derivatives that can be used as selective inhibitors of the N-terminal site of human angiotensin-converting enzyme. The derivatives comprise the amino acid sequence with the following formula: -Asp-Phe-&PSgr;(PO2CH2)-Ala-Xaa′-  (I) wherein: &PSgr;(PO2CH2) indicates that the peptide bond (CONH) between Phe and Ala has been replaced by the phosphonic bond PO2CH2, and Xaa′ represents an amino acid residue. They can be used in pharmaceutical formulations, particularly to protect haematopoietic strain cells of patients undergoing aggressive chemotherapy or radiotherapy treatment.

Abstract: Peptide derivatives usable as zinc endopeptidase 24-15 inhibitors.These peptide derivatives have the following amino acid sequence:-Phe.psi.(PO.sub.2 CH.sub.2)-.sub.(L,D) Xaa'-Yaa'-Zaa'-in which .psi.(PO.sub.2 CH.sub.2) indicates that the peptide bond (CONH) has been replaced by the phosphine bond (PO.sub.2 CH.sub.2), Xaa' and Zaa', which can be the same or different, in each case represent a natural amino acid or an amino pseudo-acid and Yaa' represents Arg or Lys.As examples of such derivatives, reference can be made to those of formula:Z-.sub.(L,D) Phe.psi.(PO.sub.2 CH.sub.2)-.sub.(L,D) -Gly-Arg-MetOHZ-.sub.(L,D) Phe.psi.(PO.sub.2 CH.sub.2)-.sub.(L,D) -Ala-Arg-MetOHZ-.sub.(L,D) Phe.psi.(PO.sub.2 CH.sub.2)-.sub.(L,D) -Ala-Arg-PheOHwith Z representing the benzyloxycarbonyl group.

Abstract: 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.

Abstract: 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.

Abstract: 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.