Myriad Genetics, Inc.

Molecumetics Ltd.

Mercury Therapeutics, Inc.

Hoechst Marion Roussel

Augusta Pharmaceuticals Inc.

Aventis Pharmaceuticals Inc.

Hwa-Ok Kim

Michael S Kahn

Masakatsu Eguchi

Cyprian Okwara Ogbu

Marcin Stasiak

Patrick Douglas Boatman, Jr

Norton P Peet

Jan Urban

Sharanappa B Rajur

Hiroshi Nakanishi

Gangadhar Nagula

Neal C Birnberg

Christopher Lum

Hong Liu

Qing Ping Weng

Haibo Shang

Pan Yin

Paresh D Salgaonkar

Michael R Angelastro

Shujaath Mehdi

Paresh Salgaonkar

Jun Xian

Chaeho Moon

Madhavi Neelagiri

Dorre A Grueneberg

Venugopal Rao Neelagiri

Mark A Blaskovich

Matthew D Linnik

Ori Kalid

Divakaramenon Sethumadhavan

The present invention relates to a method using some novel compounds and compositions for the inhibition of ROS tyrosine kinase. In particular, the present invention covers a method to treat abnormal cell growth, such as cancer, with ROSinhibitors and compositions having ROS inhibitors. An illustrative compound of the invention is shown below Formula (I). 

Methods, compounds, and compositions for inhibition of ROS

The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.

AMPK modulators

Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

Reverse-turn mimetics and methods relating thereto

There are disclosed &#x3b2;-sheet mimetics and methods relating to the same for imparting or stabilizing the &#x3b2;-sheet structure of a peptide, protein or molecule. In one aspect, &#x3b2;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &#x3b2;-sheet mimetic is a thrombin inhibitor.

&#x3b2;-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R, R, Rand Rare as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Reverse-turn mimetics and compositions and methods related thereto

Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A', B, X, Y, R, R, Rand Rare as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are tryptase antagonists.

&#x3b2;-sheet mimetics and composition and methods relating thereto

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed:wherein A, R, R, Rand Rare as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Reverse-turn mimetics and composition and methods relating thereto

There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, &bgr;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &bgr;-sheet mimetic is a thrombin inhibitor.

&bgr;-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins

Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetics of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Growing community of inventors

Lexington, MA, United States of America

Hwa-Ok Kim