专利号:US-2005085492-A1 优先权日:2003-10-20 标 题:Stereoselective process for the synthesis of chiral garft compounds and intermediates 发明人:RAHMAN LEERA 权利人:AGOURON PHARMACEUTICALS MINC 摘要:The present invention describes a stereoselective preparation of derivatives and precursors of molecules having formula 1: n nMethod of preparing the compounds, intermediates and derivatives are described. The methods described herein allow the preparation of diastereomeric forms of compound having formula 1. The compounds of the invention are GARFT inhibitors.
专利号:US-10793557-B2 优先权日:2018-04-03 标题 :Sting agonist compounds 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHILDERS MATTHEW LLOYD; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIM JONGWON; LU MIN; OTTE RYAN D; TROTTER BENJAMIN WESLEY 权利人:MERCK SHARP & DOHME 摘要:Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
专利号:US-7476767-B2 优先权日:2004-01-30 标题:Alpha-hydroxy sulfonate aldehydes, germicidal compositions containing the alpha-hydroxy sulfonate aldehydes, or mixtures of alpha-hydroxy sulfonate aldehydes and phthalaldehydes, and methods of using the compounds or compositions for disinfection or sterilization 发明人:ZHU PETER C; ROBERTS CHARLES G; TRAN YVONNE 权利人:ETHICON INC 摘要:Disclosed herein are α-Hydroxy sulfonate aldehydes and synthesis methods therefor. Germicidal compositions including the α-hydroxy sulfonate aldehydes, are also disclosed. In one aspect, a germicidal composition may include a diluent, and a germicidally effective amount of a water-soluble germicidal compound including an aldehyde group and an α-hydroxy sulfonate group. The water-soluble compound may have a solubility of at least 5 (w/v) % in water. In a further aspect, the compound may include 1-hydroxy-3-oxo-2-phenyl-propane-1-sulfonic acid salt, (2-formyl-phenyl)-hydroxy-methane sulfonic acid salt, 1-hydroxy-2-(4-methanesulfonyl-2-nitro-phenyl)-3-oxo-propane-1-sulfonic acid salt, 2-bromo-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-chloro-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-(1-formyl-2-hydroxy-2-sulfo-ethyl)-isonicotinic acid salt, 2-benzooxazol-2-yl-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, or 1-hydroxy-2-(4-methoxy-phenyl)-3-oxo-propane-1-sulfonic acid salt. Germicidal compositions including a mixture of an α-hydroxy sulfonate aldehyde and one or more phthalaldehydes, such as phthalaldehyde, isophthalaldehyde, terephthalaldehyde, or a combination thereof, are also disclosed. Methods of using the compounds or compositions for killing bacteria, disinfection, or sterilization, are also disclosed.
专利号:JP-H08501307-A 优先权日:1992-09-23 标题:Synthesis of useful intermediates of substituted imidazole compounds
专利号:US-11702430-B2 优先权日:2018-04-03 标 题:Aza-benzothiophene compounds as STING agonists 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 权利人:MERCK SHARP & DOHME LLC; ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 摘要:Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , R 9 , A, X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
专利号:EP-0662961-A4 优先权日:1992-09-23 标题:METHOD FOR SYNTHESIS OF USEFUL INTERIM PRODUCTS OF SUBSTITUTED IMIDAZOLIC COMPOUNDS.
[参考文献]: Anne-Mari Ruohola, Et Al. Reactions Of 9-Substituted Guanines With Bromomalondialdehyde In Aqueous Solution Predominantly Yield Glyoxal-Derived Adducts. Org Biomol Chem. 2004 Jul 7;2(13):1943-50. [参考文献]: E C Taylor, Et Al. A Simplified And Efficient Synthesis Of 5,10-Dideaza-5,6,7,8-Tetrahydrofolic Acid (Ddathf). Invest New Drugs. 1996;14(3):281-5.
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 451. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 288.