专利号:US-6469065-B1 优先权日:1996-02-02 标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use 发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
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:US-RE41998-E 优先权日:1990-02-26 标题 :Compositions and methods of treatment of sympathetically maintained pain 发明人:CAMPBELL JAMES N 权利人:ARCLON THERAPEUTICS INC 摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.
专利号:US-2005187222-A1 优先权日:1996-02-02 标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds 发明人:GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
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.
1: Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wünsch B. Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Dec 18;144:672-681. doi: 10.1016/j.ejmech.2017.12.054. [Epub ahead of print] doi: 10.3892/etm.2017.5311. Epub 2017 Oct 16. 3: Opere CA, Heruye S, Njie-Mbye YF, Ohia SE, Sharif NA. Regulation of Excitatory Amino Acid Transmission in the Retina: Studies on Neuroprotection. J Ocul Pharmacol Ther. 2017 Dec 21. doi: 10.1089/jop.2017.0085. [Epub ahead of print] doi: 10.1016/j.expneurol.2017.12.005. [Epub ahead of print] doi: 10.1016/j.bmc.2017.12.010. Epub 2017 Dec 7. doi: 10.1016/j.neuropharm.2017.10.014. Epub 2017 Oct 16. 9: Perrio C, Nicole O, Buisson A. GluN2B Subunit Labeling with Fluorescent Probes and High-Resolution Live Imaging. Methods Mol Biol. 2017;1677:171-183. doi: 10.1007/978-1-4939-7321-7_9. doi: 10.1371/journal.pone.0185796. eCollection 2017.
合成参考文献
参考文献:10.1016/j.brainres.2010.02.025 摘要:Hackman JC, Holohean AM. The effects of polyamine agonists and antagonists on N-methyl-D-aspartate-induced depolarizations of amphibian motoneurons in situ. Brain Res. 2010 Apr 14;1325():10–8. doi: 10.1016/j.brainres.2010.02.025. 参考文献:10.1111/j.1460-9568.2011.07763.x 摘要:Baxter AW, Choi SJ, Sim JA, North RA. Role of P2X4 receptors in synaptic strengthening in mouse CA1 hippocampal neurons. Eur J of Neuroscience. 2011 Jul;34(2):213–20. doi: 10.1111/j.1460-9568.2011.07763.x. 参考文献:10.1007/s00737-011-0231-5 摘要:Morrison MF, Freeman EW, Lin H, Sammel MD. Higher DHEA-S (dehydroepiandrosterone sulfate) levels are associated with depressive symptoms during the menopausal transition: results from the PENN Ovarian Aging Study. Archives of Women's Mental Health. 2011 Jul 20;14(5):375. doi: 10.1007/s00737-011-0231-5.