Janssen Pharmaceutica Nv

Ortho-mcneil Pharmaceutical Corp.

Carsten Schubert

Dennis J Hlasta

Bruce L Grasberger

Edward Charles Lawson

Kimberly White

Shyamali Ghosh

Michael H Parker

Cynthia M Milligan

Frank A Lewandowski

Richard Scott Alexander

Renee L DesJarlais

Celine Schalk-Hihi

Diane M Maguire

Allen B Reitz

Yifang Huang

Brett A Tounge

Michael Peter Winters

Eric D Strobel

John Curtis Spurlino

Alfonzo D Jordan

Ingrid Christa Deckman

Diane Maguire

Frank A Lewandoswki

Kimberly B White

The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Alkynyl derivatives useful as DPP-1 inhibitors

The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Bicyclic derivatives useful as inhibitors of DPP-1

The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Substituted benzothiazole and benzoxazole derivatives useful as inhibitors of DPP-1

A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized form of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.

Crystal structure of monoacylglycerol lipase (MGLL)

A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized forms of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.

Alternative crystal form of monoacylglycerol lipase (MGLL)

The present invention includes crystallized HDM2 peptides as well as descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of HDM2 to be determined at atomic resolution so that ligand binding sites on HDM2 can be identified and the interactions of ligands with HDM2 amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MDM2 and HDM2 oncoproteins.

HDM2-inhibitor complexes and uses thereof

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Phoenixville, PA, United States of America

Carsten Schubert