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-2006014773-A1 优先权日:2001-04-19 标题:Mental agility lozenge, edible strip, food or drink 发明人:MCCLEARY EDWARD L 权利人:MCCLEARY EDWARD L 摘要:A mental agility composition is composed of at least one agent which promotes synthesis of ATP and/or creatine phosphate in the body; at least one antioxidant for scavenging free radicals in at least one pathway in the body; at least one agent for normalizing or maintaining membrane function and structure in the body; at least one agent for normalizing or maintaining normal neurotransmitter function in the body; at least one agent for down-regulating cortisol action; and at least one agent for suppressing activation of apoptotic pathways in the body. The composition may further contain one or more of at least one agent for suppressing inflammation in the body; at least one agent for normalizing or maintaining vascular wall function and structure in the body; at least one agent for normalizing or maintaining function of nerve growth factors and/or neurotropic factors in the body; at least one agent for suppressing toxic metal ionic effects; at least one agent for normalizing or maintaining methyl metabolism in the body; at least one agent for normalizing or maintaining metabolism of insulin and glucose in the body; and at least one agent for up-regulating activity of heat shock proteins in the body. The composition is administered in the form of a breath-care strip, mint or lozenge, or a food or beverage product.
专利号:US-2015283095-A1 优先权日:2012-11-16 标 题:Nanoparticles with biodegradable and biocompatible polymer plga, loaded with the drug for human use pentoxifylline 发明人:CONSTANDIL CÓRDOVA LUIS ERNERTO; IBARRA DURÃ?N PAULA SOLEDAD; VILOS ORTIZ CRISTIAN ANDRES; VELÃ?SQUEZ CUMPLIDO LUIS; PELISSIER SERRANO TERESA; LAURIDO FUENZALIDA CLAUDIO AURELIO; HERNÃ?NDEZ KUNSTMANN ALEJANDRO 权利人:UNIV SANTIAGO CHILE 摘要:The invention relates to a novel pharmaceutical formulation comprising polymer nanoparticles of the biodegradable and biocompatible polymer poly(lactic-glycolic) acid (PLGA), loaded with the drug pentoxifylline, the method for the synthesis of the PLGA nanoparticles loaded with pentoxifylline, and to the use thereof in the effective treatment for the relief of chronic pain and for the prevention of chronic pain via the administration of a single dose.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:US-6458822-B2 优先权日:2000-03-13 标题 :2-oxo-imidazolidine-4-carboxylic acid hydroxamide compounds that inhibit matrix metalloproteinases 发明人:ROBINSON RALPH P; LAIRD ELLEN R 权利人:PFIZER 摘要:The present invention relates to a compound of the formula n wherein R 1 , R 2 , R 3 and R 4 are as defined above, and pharmaceutically acceptable salts and solvates thereof, that are useful, for example, as matrix metalloproteinase inhibitors. The present invention is also directed to pharmaceutical compositions comprising such compounds and methods of treatment for diseases such as osteoarthritis, rheumatoid arthritis, cancer, osteoporosis, tissue ulceration, restinosis, periodontal disease, inflammation, epidermolysis bullosa, scleritis, stroke, Alzheimer's disease, and the like, characterized by inappropriate matrix metalloproteinase activity. Processes for the synthesis of compounds of formula (I) are also disclosed.
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