Bracco International Bv

Bracco Research, USA

Bristol-myers Squibb Compnay

Bracco S.p.a.

Bracco Imaging S.p.a.

Ramachandran S Ranganathan

Michael F Tweedle

Radhakrishna K Pillai

Kondareddiar Ramalingam

Edmund R Marinelli

Thangavel Arunachalam

Paul W Wedeking

Adrian D Nunn

Karen E Linder

Rolf E Swenson

Natarajan Raju

Thangavel Arunchalam

Ruth Wager

Kenneth J Natalie, Jr

Sang I Kang

Helen Fan

Ruth E Wager

Pier Lucio Anelli

Alessandro Maiocchi

Mario Virtuani

Hong (Helen) Fan

Andrea Beltrami

Luisella Calabi

Maurizio Franzini

Peter C Ratsep

Nataranjan Raju

Rajesh Shukla

Xun Zhang

Edmund E Marinelli

Radhakrishua Pillai

Radhakrishna Pillai

The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.

Conjugates of antioxidants with metal chelating ligands for use in diagnostic and therapeutic applications

Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLe) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLecompositions. In particular, the disclosed SLecompounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLecompounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl Le, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

Linkable sialyl Lewis X analogs

Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the &#x3b1;, &#x3b3;, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Metal complexes derivatized with folate for use in diagnostic and therapeutic applications

Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula wherein R, A, Rand Rare as defined herein, are disclosed.

Aminocarboxylate ligands having substituted aromatic amide moieties

Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formulawherein R, A, Rand Rare as defined herein, are disclosed.

Enhanced relaxivity monomeric and multimeric compounds

Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.

Chelating compounds, their complexes with paramagnetic metals

Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the &agr;, &ggr;, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the .alpha., .gamma., or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Metal complexes derivatized with folate for use in diagnostic and

In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.

Methods and compositions for using non-ionic contrast agents to reduce

New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, ##STR2## --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O-- or ##STR3## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl. Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR4## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.

Nonionic radiographic contrast agents

New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, ##STR2## --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O-- or ##STR3## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl. Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR4## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.

Growing community of inventors

Princeton, NJ, United States of America

Ramachandran S Ranganathan