Patent application number | Description | Published |
20080248566 | MATRIPTASE, A SERINE PROTEASE AND ITS APPLICATIONS - The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors. | 10-09-2008 |
20080269140 | Conformationally Constrained Smac Mimetics and the Uses Thereof - The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 10-30-2008 |
20090082424 | SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS - The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-X | 03-26-2009 |
20090082445 | GOSSYPOL CO-CRYSTALS AND THE USE THEREOF - This invention relates to compositions comprising co-crystals of (−)-gossypol with a C | 03-26-2009 |
20090092684 | SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS - The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-X | 04-09-2009 |
20090118377 | APOGOSSYPOLONE AND THE USES THEREOF - The invention relates to the compound apogossypolone and salts and prodrugs thereof. Apogossypolone functions as an inhibitor of Bcl-2 family proteins. The invention also relates to the use of apogossypolone for inhibiting hyperproliferative cell growth, for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death. | 05-07-2009 |
20090123480 | BIVALENT SMAC MIMETICS AND THE USES THEREOF - The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 05-14-2009 |
20100069344 | SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS - The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-X | 03-18-2010 |
20100093645 | SMAC Peptidomimetics and the Uses Thereof - The invention relates to peptidomimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these peptidomimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 04-15-2010 |
20100273799 | SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s). | 10-28-2010 |
20100273812 | DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF - The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 10-28-2010 |
20100317661 | SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s). | 12-16-2010 |
20110046189 | HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF - The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 02-24-2011 |
20110112052 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 05-12-2011 |
20110184033 | Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same - Potent and selective ligands for the dopamine 3 (D | 07-28-2011 |
20110251252 | BIOMARKERS FOR MDM2 INHIBITORS FOR USE IN TREATING DISEASE - Provided herein are methods for selecting and treating a subject with leukemia, wherein the subject is selected for treatment and is treated with an MDM2 inhibitor because said subject's cells contain an FLT3-ITD mutation. | 10-13-2011 |
20110312997 | Inhibition of WDR5 Interaction with Its Binding Partners - Peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed. | 12-22-2011 |
20110319362 | STAT3 LIGANDS AND THERAPEUTIC USES THEREOF - Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed. | 12-29-2011 |
20120101092 | SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s). | 04-26-2012 |
20120122947 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 05-17-2012 |
20120189539 | BCL-2/BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed. | 07-26-2012 |
20120232118 | SELECTIVE LIGANDS FOR THE DOPAMINE 3 (D3) RECEPTOR AND METHODS OF USING THE SAME - Potent and selective ligands for the dopamine 3 (D | 09-13-2012 |
20120263675 | BIVALENT DIAZO BICYCLIC SMAC - The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer. | 10-18-2012 |
20120289494 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 11-15-2012 |
20120302629 | BIOMARKERS FOR GOSSYPOL CHEMOTHERAPY AND METHODS OF TREATING DISEASE - The present invention provides a biomarker for selecting a patient for treatment with gossypol, wherein the biomarker comprises an elevated expression level of c-Myc, Mcl-1, or combination thereof, relative to the normal expression level of c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for targeting patients for treatment with gossypol, wherein the patient has a disease, condition, or disorder that overexpresses c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for treating or ameliorating a disease, condition, or disorder in a patient comprising determining the expression level of c-Myc, Mcl-1, or combination thereof in the patient and administering gossypol to the patient. In certain embodiments of the invention, the disease is cancer, and the cancer cells show elevated expression levels of c-Myc compared to non-cancerous cells. The invention also provides methods for overcoming Mcl-1-mediated chemoresistance comprising administering gossypol to a patient in need thereof. | 11-29-2012 |
20120309961 | DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF - The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis. | 12-06-2012 |
20130030173 | PROCESS FOR THE PREPARATION OF SMALL MOLECULE INHIBITORS OF MDM2 AND INTERMEDIATES USED THEREIN - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s). | 01-31-2013 |
20130150309 | CYCLIZED PEPTIDOMIMETIC SMALL MOLECULE INHIBITORS OF THE WDR5 AND MLL1 INTERACTION - Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed. | 06-13-2013 |
20130296303 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 11-07-2013 |
20140057924 | BIVALENT INHIBITORS OF IAP PROTEINS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed. | 02-27-2014 |
20140148494 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 05-29-2014 |
20140199234 | BCL-2/BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed. | 07-17-2014 |
20140256706 | BET BROMODOMAIN INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed. | 09-11-2014 |
20140378680 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 12-25-2014 |