Bracco Suisse Sa

Bracco Imaging S.p.a.

Other

Bracco International Bv

Bernard Lamy

Philippe Bussat

Rolf E Swenson

Sibylle Pochon

Bo Song

Samir Cherkaoui

Palaniappa Nanjappan

Radhakrishna K Pillai

Hong (Helen) Fan

Edmund R Marinelli

Thierry Bettinger

Irene Guilbert-Brigger

Kondareddiar Ramalingam

Hong (helen) Fan

Hong Helen Fan

Hong Fan

The present invention discloses a new efficient process for the preparation of the KDR-targeting peptide-phospholipid conjugate of formula (I), which can be useful in therapeutic and diagnostic compositions and particularly in the preparation of ultrasound contrast agents.

Optimized process for dimeric peptide-phospholipid conjugate

Peptide vectors having high KDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.

Targeting vector-phospholipid conjugates

Gas-filled microvesicles associated with a polypeptide comprising a sequence of amino acids, said sequence exhibiting binding affinity for selectins, particularly p-selectin. The gas-filled microvesicles can be used in ultrasound imaging.

Targeting constructs

Targeted gas-filled microvesicles

Fibrin-binding peptides having high binding affinity and excellent physical characteristics compared to previously known fibrin-binding peptides are provided. These fibrin-binding peptides may be conjugated to a detectable label or a therapeutic agent and used to detect and facilitate treatment of pathological conditions associated with the presence of fibrin such as thrombic, angiogenic and neoplastic conditions. These peptides may be used in imaging processes such as MRI, ultrasound and nuclear medicine imaging (e.g. PET, scintigraphic imaging, etc.). The peptides may also be used therapeutically. The present invention also provides processes and methods for making and using such peptides and conjugates thereof.

Fibrin-binding peptides and conjugates thereof

New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein: M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.

Targeting and therapeutic compounds and gas-filled microvesicles comprising said compounds

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Saint-Julien-en-Genevois, France

Bernard Lamy