Patent application number | Description | Published |
20090221016 | MODIFIED TUMOR NECROSIS FACTOR-ALPHA CONVERTING ENZYME AND METHODS OF USE THEREOF - The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE. | 09-03-2009 |
20090258868 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 10-15-2009 |
20090306047 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 12-10-2009 |
20090312341 | CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT - Disclosed are novel compounds of the formula | 12-17-2009 |
20100136620 | SOLUBLE, STABLE FORM OF HDM2, CRYSTALLINE FORMS THEREOF AND METHODS OF USE THEREOF - The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes. | 06-03-2010 |
20100152138 | CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 06-17-2010 |
20100184111 | MODIFIED TUMOR NECROSIS FACTOR-ALPHA CONVERTING ENZYME AND METHODS OF USE THEREOF - The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE. | 07-22-2010 |
20110218194 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 09-08-2011 |
20130004518 | CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 01-03-2013 |
20130018066 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 01-17-2013 |
20140057910 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 02-27-2014 |
20140128361 | CYCLIC AMIDE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 05-08-2014 |
Patent application number | Description | Published |
20080200445 | Heterocyclic aspartyl protease inhibitors -
Disclosed are compounds of the formula I
| 08-21-2008 |
20100178294 | MACROCYCLIC BETA-SECRETASE INHIBITORS - Disclosed are novel compounds of the formula | 07-15-2010 |
20100203616 | REFOLDED RECOMBINANT ALPHA SECRETASE CRYSTALS AND METHODS FOR PREPARING AND USING THE SAME - The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization. | 08-12-2010 |
20100267150 | HDM2 POLYPEPTIDES - The present invention relates to HDM2 polypeptides and mutants thereof which are complexed with various compounds, e.g., HDM2 inhibitors. | 10-21-2010 |
20120231017 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 09-13-2012 |
20120231018 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 09-13-2012 |
20120276118 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 11-01-2012 |