专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:WO-2022226312-A1 优先权日:2021-04-22 标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers 发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES 权利人:CLEAR CREEK BIO INC 摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides
专利号:US-2008125354-A1 优先权日:2005-11-21 标题 :Selective inhibition of matrix metalloproteinases 发明人:FIELDS GREGG B; HAMMER ROBERT 权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE 摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.