Bracco Imaging S.p.a.

Bracco International Bv

Enzo Biochem, Inc.

Bracco Suisse Sa

Bracco Research, USA

Icn Pharmaceuticals, Inc.

Natarajan Raju

Kondareddiar Ramalingam

Karen E Linder

Michael F Tweedle

Edmund R Marinelli

Palaniappa Nanjappan

Adrian D Nunn

Rolf E Swenson

Luciano Lattuada

Enrico Cappelletti

Praveen Pande

Zaiguo Li

Radhakrishna K Pillai

Mathew A Von Wronski

Ramachandran S Ranganathan

Thangavel Arunachalam

Paul W Wedeking

Michel Schneider

Feng Yan

Ruth E Wager

Kandasamy Ramasamy

Ruth Wager

Arthur F Lewis

Roland K Robins, Deceased

Vjera Pejanovic

Ramesh Bharadwaj

Mary Ellen Maddalena

The present disclosure provides reactive quencher dyes that can be used in the detection and/or quantification of desirable target molecules, such as proteins, nucleic acids and various cellular organelles. These dyes are essentially non-fluorescent but are efficient quenchers of various fluorescent dyes. Also, provided are methods of using the dyes, bio-probes incorporating dyes and methods of using the bio-probes. The quencher dyes described herein are modified to provide beneficial properties.

Monoazo dyes with cyclic amine as fluorescence quenchers

The invention provides methods for synthesizing the compound (2R,3S,4E)-N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol, also known as SK1-I, and intermediate compounds used in its synthesis.

Methods and intermediates for synthesizing SK1-I

Monoazo dyes with cyclic amine as fluorescence quencers

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

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. 

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.

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.

The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-1 receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.

Compounds for targeting endothelial cells, compositions containing the same and methods for their use

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 define 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.

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Kendall Park, NJ, United States of America

Natarajan Raju