Bracco Suisse Sa

Dyax Corporation

Bracco International Bv

Bracco Imaging S.p.a.

Other

Takeda Pharmaceutical Company Limited

Feng Yan

Radhakrishna Pillai

Christophe Arbogast

Philippe Bussat

Sibylle Pochon

Karen E. Linder

Hong Fan

Edmund R. Marinelli

Bo Song

Palaniappa Nanjappan

Rolf E Swenson

Edmund R Marinelli

Karen E Linder

Kondareddiar Ramalingam

Radhakrishna K Pillai

Adrian D Nunn

Mathew A Von Wronski

Michael F Tweedle

Natarajan Raju

Aaron Sato

Daniel T Dransfield

Ajay Shrivastava

Luciano Lattuada

Enrico Cappelletti

Sharon Michele Walker

Hong (Helen) Fan

Samir Cherkaoui

Bernard Lamy

Robert Charles Ladner

Sudha Khurana

David P Nowotnik

Michel Schneider

Daniel J Sexton

Sybille Pochon

Mary Ellen Maddalena

Aaron K Sato

Robert C Ladner

Hong Helen Fan

Hong (helen) Fan

The present invention provides polypeptides, peptide dimer, and multimeric complexes comprising at least one binding moiety for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity (e.g., having a K&#x3c;1 &#x3bc;M), and dimer and multimeric constructs comprising these polypeptides.

KDR and VEGF/KDR binding peptides and their use in diagnosis and therapy

The present invention provides polypeptides, peptide dimers, and multimeric complexes comprising at least one binding moiety for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity (e.g., having a K&#x3c;1 &#x3bc;M), and dimer and multimeric constructs comprising these polypeptides, particularly contrast agents. Also provided are methods for monitoring and evaluating the therapeutic effectiveness of treatment protocols for diseases associated with angiogenesis or endothelial cell hyperproliferation, such as cancer, using contrast agents of the invention.

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

The invention provides compositions and methods for therapeutic and diagnostic applications.

Multivalent constructs for therapeutic and diagnostic applications

A polypeptide or multimeric polypeptide construct having the ability to bind to cMet or a complex comprising cMet and HGF, and methods for use are disclosed.

Peptides that specifically bind HGF receptor (cMet) and uses thereof

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N&#x2014;O&#x2014;P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N&#x2014;O&#x2014;P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

Gastrin releasing peptide compounds

Improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N-O-P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer, said methods comprising the step of administering to a subject a dose comprising an amount of radioactively labeled L70, N-[4-[[[[[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]acetyl]amino]benzoyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valyl-glycyl-L-histidyl-L-leucyl-L-methioninamide. 

New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N&#x2014;O&#x2014;P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N&#x2014;O&#x2014;P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.

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Princeton, NJ, United States of America

Palaniappa Nanjappan