专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-2024424490-A1 优先权日:2021-01-25 标 题 :Method of synthesis of carbon-supported platinum group metal or metal alloy nanoparticles 发明人:WNUK PAWEL; LEWERA ADAM; JURCZAKOWSKI RAFAL; POWALA FILIP; KOLODZIEJCZYK JAN 权利人:UNIV WARSZAWSKI 摘要:The presented invention relates to a method of synthesis of carbon-supported platinum group metal or metal alloy nanoparticles, which comprises the following steps:n adsorbing on carbon support complexes of a platinum group metal with a urea complexing agent selected from a group comprising urea, urea derivative, a mixture of urea with at least one urea derivative, and a mixture of at least two urea derivatives; and reducing the complexes adsorbed on the carbon support to metal nanoparticles, forming a product of carbon-supported metal nanoparticles. nn The invention also provides the use of the carbon-supported platinum group metal or metal alloy nanoparticles obtained by the method of the invention as catalyst. n The present invention further relates to a method of adsorption of precursors of platinum group metals on the surface of a carbon support and use of complexes of platinum group metals with urea complexing agent for adsorption of platinum group metal precursors on carbon support.
专利号:US-4627968-A 优先权日:1984-09-10 标 题 :Synthesis of crystalline aluminosilicate with alkylurea or alkylthiourea 发明人:KAI TADASHI 权利人:ASAHI CHEMICAL IND 摘要:In the synthesis of a crystalline aluminosilicate by heating an aqueous mixture containing a silica source, an alumina source and an alkali metal source, at least one compound selected from lower alkylureas and lower alkylthioureas is permitted to co-exist with the mixture.
专利号:US-6869973-B2 优先权日:2000-06-22 标题:Nitrosated and nitrosylated taxanes, compositions and methods of use 发明人:GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; RICHARDSON STEWART K; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, 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 present invention also provides novel compositions comprising at least one taxane 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 compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.
专利号:US-7384976-B2 优先权日:2001-05-02 标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use 发明人:GARVEY DAVID S 权利人:NITROMED INC 摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.
专利号:US-5136097-A 优先权日:1989-04-06 标 题 :Process for the preparation of sulfonylmethanes and derivatives thereof 发明人:ARMAND MICHEL 权利人:CENTRE NAT RECH SCIENT; HYDRO QUEBEC 摘要:The invention relates to a process for the synthesis of sulfonylmethanes and derivatives thereof of the formula M[(RSO 2 ) 2 CH] m (I), in which M represents H, an alkali metal or alkaline earth metal or NR' 4 , R' and R are monovalent organic radicals and m represents the valence of M. n The process comprises reacting an ionic carbide with a sulfonyl halide, hydrolyzing the product obtained, adding a compound M y Y m , in which Y represents an anion capable of reacting with the cation of the ionic carbide to the reaction medium before or after hydrolysis to give a compound which can be separated from compound (I), and y represents the valence of Y.
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合成参考文献
参考文献:10.1007/s10895-011-0918-z 摘要:Kumaran R, Ramamurthy P. Photophysical studies on the interaction of formamide and alkyl substituted amides with photoinduced electron transfer (PET) based acridinedione dyes in water. J Fluoresc. 2011 Nov;21(6):2165–72. doi: 10.1007/s10895-011-0918-z.