Patent application number | Description | Published |
20110086889 | TETRAZOLE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to tetrazole compounds of formula (I) wherein X, Y, Z, R | 04-14-2011 |
20110105491 | THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R | 05-05-2011 |
20110105514 | 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS - The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I) wherein R | 05-05-2011 |
20110105515 | TARGETING THE ONCOPROTEIN NUCLEOPHOSMIN - (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin. | 05-05-2011 |
20110166170 | SYNTHESIS OF AVRAINVILLAMIDE, STEPHACIDIN B, AND ANALOGUES THEREOF - The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection. | 07-07-2011 |
20110212968 | PHENETHYLAMIDE DERIVATIVES AND THEIR HETEROCYCLIC ANALOGUES - The invention relates to novel phenethylamide derivatives and their wherein A, B, R | 09-01-2011 |
20120088759 | THIAZOLIDIN-4-ONE AND [1,3]-THIAZINAN-4-ONE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R | 04-12-2012 |
20120101111 | NOVEL OXAZOLIDINONE DERIVIATIVES - The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R | 04-26-2012 |
20120316178 | PIPERAZINES AS ANTIMALARIAL AGENTS - The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. | 12-13-2012 |
20130109685 | 1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS | 05-02-2013 |
20140045870 | 7-(Heteroaryl-Amino)-6,7,8,9-Tetrahydropyrido[1,2-A]Indol Acetic Acid Derivatives and Their Use as Prostaglandin D2 Receptor Modulators - The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I), | 02-13-2014 |