Cylene Pharmaceuticals, Inc.

Merck Sharp + Dohme Corp.

Senhwa Biosciences, Inc.

Peter C Chua

Johnny Yasuo Nagasawa

Fabrice Pierre

Jeffrey Paul Whitten

Michael Schwaebe

Mark T Bilodeau

Nicholas D P Cosford

Jacob M Hoffman

Mustapha Haddach

Collin Regan

The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.

Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators

The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.

Protein kinase modulators

The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Inhibitors of Akt activity

The invention relates in part to fused tricyclic compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The fused tricyclic compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such fused tricyclic compounds.

Compounds having formula 1: are produced by contacting a compound having formula (6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L, W, X, B', R and n are as defined herein.

Methods of preparing quinolone analogs

The present invention provides quinolone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing quinolone analogs, and methods of using the same.

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San Diego, CA, United States of America

Peter C Chua