Praecis Pharmaceuticals, Inc.

Janssen Pharmaceutica Nv

Johnson & Johnson Pharmaceuticals Research & Development, L.l.c.

Lily Lee

Gary Olson

Christopher Self

Charles Michael Cook

Jens Birktoft

Barry A Morgan

Christopher C Arico-Muendel

Peter J Connolly

Guozhang Xu

Stuart Emanuel

Gilles C Bignan

Steven A Middleton

Steven K Wetter

Marta Cristina Abad

Kathleen A Battista

Terry V Hughes

Tianbao Lu

Kevin Douglas Kreutter

Hui Huang

Venkatraman Mohan

Sharmila Patel

Prabha Saba Karnachi

Prabha S Kamachi

Mark Fitzgerald

Xu Guozhang

The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.

Substituted pyrimidinyl oxime kinase inhibitors

Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R-R, R, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Substituted phenyl acetamides and their use as protease inhibitors

The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

Therapeutic agents and methods of use thereof for the treatment of melanoma

The present invention provides methods of treating a lymphoma (e.g., a T-cell lymphoma or a B-cell lymphoma) in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention, for example, compounds of formulae I and XV: 

Methionine aminopeptidase-2 inhibitors and methods of use thereof

Therapeutic agents and methods of use thereof for the modulation of angiogenesis

The present invention provides methods of treating an autoimmune disorder (e.g., lupus erythematosus, multiple sclerosis, myasthenia gravis, vasculitis and diabetes mellitus) in a subject by administering to the subject a therapeutically effective amount of one or more compounds of the invention.

The present invention provides methods of treating, parasitic infections, thymoma, and lymphoid malignancies in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.

The present invention provides methods of treating a parasitic infection, a lymphoid malignancy or an autoimmune disorder in a subject by administering to the subject a therapeutically effective amount of an angiogenesis inhibitor compound comprising a MetAP-2 inhibitory core coupled to a peptide.

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Edison, NJ, United States of America

Lily Lee