Commissariat a L'energie Atomique

Joël Cotton

Vincent Dive

Bertrand Tavitian

Fabrice Beau

Reto Stöcklin

Bertrand Czarny

André Menez

Dimitri Georgiadis

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

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)

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Orsay, France

Joël Cotton