Tranzyme Pharma Inc.

Telomerase Activation Sciences, Inc.

Geron Corporation

Ocera Therapeutics, Inc.

Mahesh Ramaseshan

Hamid R Hoveyda

Mark L Peterson

Graeme Lovat Fraser

Luc Ouellet

Yves Dory

Sylvie Beaubien

Calvin B Harley

Ruoxi Lan

Pierre Deslongchamps

Daniel Fortin

Gérald Villeneuve

Éric Marsault

Premchandran H Ramiya

Soo-Peang Khor

Zhu Zhen Pirot

Tong Lin

Steven Fauce

Krisztina Pongracz

Kamel Benakli

Shigui Li

Eric Marsault

Martin Vezina

Martin Vézina

Hamid Hoveyda

Graeme Fraser

This invention relates to antisense oligonucleotides comprising at least one N3'&#x2192;P5&#x2032; phosphorodiamidate linkage (NPN) in the backbone, useful for modulating gene expression involved in the pathogenesis of a disease. Compounds useful as building blocks of said antisense oligonucleotides and methods of preparing building block compounds including NPN linkages are provided.

Phosphorodiamidate backbone linkage for oligonucleotides

The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells.

Compositions and methods for increasing telomerase activity

This invention relates to antisense oligonucleotides comprising at least one N3'&#x2192;P5&#x2032; phosphorodiamidate linkage (NPN) in the backbone, and kits and pharmaceutical compositions thereof, useful for modulating gene expression involved in the pathogenesis of a disease. Also included are compounds useful as building blocks of said antisense oligonucleotides and methods of preparing said antisense oligonucleotides and building block compounds including NPN linkages.

Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

Spatially-defined macrocycles incorporating peptide bond surrogates

Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

Spatially-defined macrocyclic compounds useful for drug discovery

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Macrocyclic modulators of the ghrelin receptor

Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists

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Sunnyvale, CA, United States of America

Mahesh Ramaseshan