Janssen Pharmaceutica Nv

Ortho-mcneil Pharmaceutical Corp.

3-dimensional Pharmaceuticals, Inc.

Mediquest Therapeutics, Inc.

Aminex Therapeutics, Inc.

Nand Baindur

Mark R Player

Raymond Joseph Patch

Davoud Asgari

Benjamin Brandt

Naresh Chadha

Taxiarchis M Georgiadis

Kevin Douglas Kreutter

Guozhang Xu

Michael Gaul

Dana L Johnson

Robert W Tuman

Mark R Burns

Alexander Y Kim

Gerard F Graminski

Christian Andrew Baumann

Reitha S Weeks

The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.

Hydrophobic polyamine analogs and methods for their use

The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R, R, R, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Alkylquinoline and alkylquinazoline kinase modulators

The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: wherein R, R, R, and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.

Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis

The invention is directed to compounds of Formula II: wherein A, R, R, R, R, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

c-fms kinase inhibitors

Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitorR-X-L-polyamine

Composition containing polyamine transport inhibitor and use thereof

The invention is directed to compounds of Formulae I, II and III: wherein A, R, R, R, R, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

C-fms kinase inhibitors

The invention is directed to compounds of Formulae I: wherein A, R, R, R, R, X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

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Kendall Park, NJ, United States of America

Nand Baindur