Patent application number | Description | Published |
20090068695 | Sir2 products and activities - A novel compound, 2′/3′-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2′ and 3′ regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2′-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD | 03-12-2009 |
20090233948 | Inhibitors of nucleoside phosphorylases and nucleosidases - The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 09-17-2009 |
20090239885 | Inhibitors of nucleoside phoshorylases and nucleosidases - The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 09-24-2009 |
20090325986 | Deazapurine Analogs of 1'-Aza-L-Nucleosides - The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds. | 12-31-2009 |
20100062995 | Transition state structure of human 5'methylthioadenosine phosphorylase - Provided are methods of designing a putative inhibitor of a human 5′-methylthioadenosine phosphorylase (MTAP). Also provided are methods of inhibiting a human MTAP. | 03-11-2010 |
20100168141 | AZETIDINE ANALOGUES NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS - Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH | 07-01-2010 |
20100222370 | Methods of Treating Cancer - The invention relates to the treatment of cancer using an inhibitor of 5′-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer. | 09-02-2010 |
20110046167 | ACYCLIC AMINE INHIBITORS OF 5-METHYTIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE - The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds. | 02-24-2011 |
20110053146 | COMPOUNDS AND METHODS FOR DETECTING RICIN AND USES THEREOF - This application provides fluorescent probes, substrates, kits and methods for detecting the presence or absence of an enzyme, such as ricin, that catalyzes the release of adenine from a GAGA RNA tetraloop. | 03-03-2011 |
20110086812 | Transition state sturcture of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases - Provided are methods of designing a putative inhibitor of a 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase. The methods comprise designing a chemically stable compound that resembles the charge and geometry of the 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase transition state. Also provided are methods of inhibiting 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidases using the inhibitors found by the above methods. | 04-14-2011 |
20110092521 | Methods of Treating Diseases Using Inhibitors of Nucleoside Phosphorylases and Nucleosidases - The invention relates to treating a disease or condition in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase (MTAP) and/or 5′-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5′-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer. | 04-21-2011 |
20110130412 | Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases - The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 06-02-2011 |
20110136106 | METHODS FOR DETECTING RICIN AND RELATED COMPOUNDS AND USES THEREOF - The present invention is directed to methods for detecting the presence of ricin and compounds that catalyze the release of adenine from nucleic acids or other biological materials and for screening for inhibitors of such compounds. | 06-09-2011 |
20110178102 | SIR2 REGULATION - Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed. | 07-21-2011 |
20110201674 | Saporin-L1 inhibitors and uses thereof - Inhibitors of saporin-L1 are disclosed, as are related compositions and uses thereof, in particular in cancer therapy that employs saporin-L1-linked immunotoxins. | 08-18-2011 |
20110301104 | Transition state structure of orotate phosphoribosyl transferases and uses thereof - Methods are provided for designing a transition state inhibitor of orotate phosphoribosyltransferase (OPRT) and for inhibiting OPRT. | 12-08-2011 |
20120157479 | 3-HYDROXYPYRROLIDINE INHIBITORS OF 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE - The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds. | 06-21-2012 |
20130004947 | LUCIFERASE-LINKED ANALYSIS OF DNA-METHYLTRANSFERASE, PROTEIN METHYLTRANSFERASE AND S-ADENOSYLHOMOCYSTEINE AND USES THEREOF - The present invention relates to methods for detecting the activity of DNA (cytosine 5)-methyltransferase, protein methyltransferase or any enzyme that forms S-adenosyl-1-homocysteine (AdoHcy) as a product, and for screening for inhibitors of DNA (cytosine 5)-methyltransferase, protein methyltransferase and any enzyme that forms S-adenosyl-1-homocysteine (AdoHcy) as a product using luciferase-linked assays that convert the S-adenosyl-1-homocysteine (AdoHcy) product to a quantifiable luminescent signal. | 01-03-2013 |
20130231351 | SIR2 REGULATION - Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed. | 09-05-2013 |
20130274220 | METHODS, ASSAYS AND COMPOUNDS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING METHYLTHIOINOSINE PHOSPHORYLASE - The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors. | 10-17-2013 |