专利号:US-6362009-B1 优先权日:1997-11-21 标 题 :Solid phase synthesis of heterocycles 发明人:MUNOZ BENITO; CHEN CHIXU 权利人:MERCK & CO INC 摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
专利号:US-9662318-B2 优先权日:2012-07-16 标题 :Bitopic muscarinic agonists and antagonists and methods of synthesis and use thereof 发明人:BOULOS JOHN 权利人:BARRY UNIV INC 摘要:Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M 1 , M 2 , M 3 , M 4 , M 5 ) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. Additional bitopic muscarinic antagonists discovered and described herein include BK-23, HD-42, HD153, HD-185, KH-5, JM-31 and JM-32. These bitopic ligands and their structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M 1 -M 5 acetylcholine receptors.
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:EP-2938595-A1 优先权日:2012-12-27 标题:Method for the synthesis of a hydrazine that can be used in the treatment of the papilloma virus
专利号:WO-2014102313-A1 优先权日:2012-12-27 标题 :Method for the synthesis of a hydrazine that can be used in the treatment of the papilloma virus
专利号:US-2014018366-A1 优先权日:2012-07-16 标题:Bitopic muscarinic agonists and antagonists and methods of synthesis and use thereof
1: Oki T, Takagi Y, Inagaki S, Taketo MM, Manabe T, Matsui M, Yamada S. Quantitative analysis of binding parameters of [3H]N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice. Brain Res Mol Brain Res. 2005 Jan 5;133(1):6-11. Epub 2003 Jan 24. Russian. Japanese.
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