Patent application number | Description | Published |
20090105319 | NAPHTHALENE-BASED INHIBITORS OF ANTI-APOPTOTIC PROTEINS - Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: | 04-23-2009 |
20090124621 | PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: | 05-14-2009 |
20090124675 | INHIBITORS OF ANTI-APOPTOTIC PROTEINS - Various compounds comprising a thiazolidine ring are described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. One of the compounds described has the structure the structure A, | 05-14-2009 |
20090131474 | SCREENING METHODS FOR PROTEIN KINASE B INHIBITORS EMPLOYING VIRTUAL DOCKING APPROACHES AND COMPOUNDS AND COMPOSITIONS DISCOVERED THEREBY - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions. | 05-21-2009 |
20090258914 | Inhibitor of Anti-Apoptotic Proteins - A compound having the structure A is described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. | 10-15-2009 |
20090312352 | COMPOSITIONS AND METHODS FOR TREATMENT OF DISEASE CAUSED BY YERSINIA SPP INFECTION - The invention generally relates to compositions and methods for treatment of disease caused by | 12-17-2009 |
20100168162 | SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions. | 07-01-2010 |
20110112112 | APOGOSSYPOLONE DERIVATIVES AS ANTICANCER AGENTS - The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: | 05-12-2011 |
20110212961 | Pyrazole Derivatives as Kinase Inhibitors - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: | 09-01-2011 |
20120015992 | Napthalene-Based Inhibitors of Anti-Apoptotic Proteins - Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: | 01-19-2012 |
20120269901 | Methods and Compounds Useful to Induce Apoptosis in Cancer Cells - The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative. | 10-25-2012 |
20150051138 | INHIBITORS OF FURIN AND OTHER PRO-PROTEIN CONVERTASES - Disclosed herein are Furin/PC inhibitors for inhibiting Furin and other Propprotein Convertases. Method of making the Furin/PC inhibitors, chemical and biological characterization of the Furin/PC inhibitors, and the use of the Furin/PC inhibitors to treat infectious diseases, cancers, and inflammatory/autoimmune disorders, are also disclosed. | 02-19-2015 |
20150073054 | INHIBITORS OF FURIN AND OTHER PRO-PROTEIN CONVERTASES - Disclosed herein are Furin/PC inhibitors for inhibiting Furin and other Propprotein Convertases. Method of making the Furin/PC inhibitors, chemical and biological characterization of the Furin/PC inhibitors, and the use of the Furin/PC inhibitors to treat infectious diseases, cancers, and inflammatory/autoimmune disorders, are also disclosed. | 03-12-2015 |