Ligand Pharmaceuticals, Inc.

Pharmacopeia Inc.

Venenum Biodesign, LLC

Bristol-myers Squibb Compnay

Wyeth

Accelrys Software, Inc.

David J Diller

Brian F McGuinness

Andrew Graham Cole

Axel Metzger

Lin Zhi

Koc-Kan Ho

Cornelis Arjan Van Oeveren

Bijan Pedram

Jeffrey John Letourneau

Jason Conrad Pickens

Yixing Shen

David Rosen

Ian Henderson

Gulzar Ahmed

Katerina Leftheris

Chunjian Liu

Stephen T Wrobleski

Nasrin Ansari

Vidyadhar Madhav Paradkar

Grant E Gallagher

Gary L Schieven

Irina Neagu

Adolph C Bohnstedt

Michael J Ohlmeyer

Celia Kingsbury

David E Kaelin

Jason Trama

Jun Wen

Michael S McQueney

Rukiye Nazan Eraslan

Michael H Ohlmeyer

Steven David Paget

Chia-Yu Huang

Audrey Hospital

Yajing Rong

Zahid Hussain

Kenneth M Merz, Jr

Venugopalareddy Bommireddy Venkata

Andrew Laird Roughton

James Wen

Marc-Raleigh Brescia

David E Kaelin, Jr

William Ronald Solvibile, Jr

Joan J Zhang

Koc Kan Ho

Brian F Mcguiness

Audrey Julie Hospital

Jason C Pickens

Methods for treating bladder cancer and solid tumors are disclosed. The methods include administering to a patient a compound of formula 1 Pharmaceutical compositions of compound 1 are also disclosed.

Sting agonists for treating bladder cancer and solid tumors

Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.

Heterocycle amines and uses thereof

The present invention provides compounds of Formula I': wherein, W, X, Y, Z, Z, Z, R, R, R, Rand Rare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

Sting agonists

N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-&#x3b1; expression utilizing compounds of the present invention are also disclosed.

N-heterocyclic inhibitors of TNF-alpha expression

A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC&#x3b8;. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I:   A representative example is: 

Purinones and 1H-imidazopyridinones as PKC-theta inhibitors

Compounds of the formula wherein Rrepresents optionally substituted C-Calkyl, aryl or heteroaryl, and Rrepresents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.

8-heteroarylpurine MNK2 inhibitors for treating metabolic disorders

The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II shown below, in which Q is selected from the group consisting of CX and nitrogen; and A is chosen from the group consisting of H, (C-C) alkyl, heteroaryl, and aryl: 

6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression

N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I):  Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-&#x3b1; expression utilizing compounds of the present invention are also disclosed.

N-heterocyclic inhibitors of TNF-&#x3b1; expression

A high-throughput molecular docking facility is presented for screening combinatorial libraries to identify binding ligands and ultimately pharmaceutical compounds. The facility employs a pre-docking conformational search to generate multiple solution conformations of a ligand. The molecular docking facility includes: generating a binding site image of the protein, the binding site image having multiple hot spots; matching hot spots of the binding site image to atoms in at least one solution conformation of the multiple solution conformations of the ligand to obtain at least one ligand position relative to the protein in a ligand-protein complex formation; and optimizing the at least one ligand position while allowing translation, orientation and rotatable bonds of the ligand to vary, and while holding the protein fixed.

Molecular docking technique for screening of combinatorial libraries

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Hightstown, NJ, United States of America

David J Diller