Visen Medical, Inc.

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Millennium Pharmaceuticals Limited

Perkinelmer Health Sciences, Inc.

Millenium Pharmaceuticals, Inc.

Guojie Ho

Paul J Coleman

Milind Rajopadhye

Bohumil Bednar

Le T Duong

Kevin Groves

Nara Narayanan

Antoinette D Paone

Catherine De Tollenaere

Brice Bonnet

Christine Devijver

Darren J Carrozzella

Catherine Detollenaere

This disclosure provides a family of compounds that absorb and fluoresce in the short wave infrared region (SWIR, optionally 1000 nm to 1300 nm), including hydrophilic compounds that exhibit absorption and emission spectral profiles in aqueous solutions substantially similar to those observed in organic solvents such as methanol or DMSO. The compounds can be chemically linked to biomolecules including proteins, nucleic acids, and therapeutic small molecules. The compounds are useful for imaging in a variety of medical, biological and diagnostic applications, including SWIR in vivo imaging of regions of interest within a mammal.

NIR to SWIR fluorescent compounds for imaging and detection

The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Integrin targeting agents and in-vivo and in-vitro imaging methods using the same

The invention provides a family of agents that target bacterial infection, which can be used as imaging agents or therapeutic agents. The agents can be used to image sites of bacterial infection as well as other physiological processes in a subject.

Bacterial imaging agents and methods of using same

The invention provides a family of agents that target the prostate specific antigen, which can be used as imaging agents or therapeutic agents. The agents can be used to image prostate cancer as well as other physiological processes in a subject.

Prostate specific antigen agents and methods of using same for prostate cancer imaging

The present invention provides, inter alia, convergent processes for preparing eptifibatide that involve coupling a 2-6 eptifibatide fragment to an activated cysteinamide residue to form a 2-7 eptifibatide fragment, attaching a mercaptopropionic acid residue to the 2-7 eptifibatide fragment through disulfide bond formation, coupling the peptide intramolecularly, and removing the protecting group, to form eptifibatide. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide, and novel compounds that are structurally similar to eptifibatide.

Processes for preparing eptifibatide

This invention provides a method for making maytansinoids having a chiral amino acid side chain, such as DM1 and DM4 that are used to treat cancer. According to this method, the side chain may be added with little epimerization of the amino acid chiral center.

Method of acylating maytansinol with chiral amino acids

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Sudbury, MA, United States of America

Guojie Ho