专利号:WO-2016005407-A1 优先权日:2014-07-07 标 题:One-pot synthesis of squaramides 发明人:MÃ?RQUEZ LÓPEZ MARÃ?A EUGENIA; ALEGRE REQUENA JUAN VICENTE; PÉREZ HERRERA RAQUEL 权利人:UNIV ZARAGOZA; CONSEJO SUPERIOR INVESTIGACION 摘要:The present invention refers to the first one-pot synthesis of squaramides. The one-pot synthesis of squaramides described herein is an easy and straightforward procedure to obtain squaramide derivatives which saves energy, avoids time consuming purification steps, reduces costs and provides better yields as compared with those squaramides obtained through the traditional 'stop-and-go' approach. Moreover, the authors of the present invention herein demonstrate the efficiency of this one-pot process with the synthesis of three biologically active structures, improving in most of the cases the results of the previous stepwise syntheses.
专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
专利号:WO-2011000122-A1 优先权日:2009-07-01 标题 :Formulation based on the synthesis of microspheres made from cross-linked natural gelatine, used as a carrier for strains of probiotic lactobacillus spp. for treating skin wounds and/or lesions 发明人:CASTRO INOSTROZA ERICA; BORQUEZ YANEZ RODRIGO; GONZALES RIQUELME MARGARITA; KLATTENHOFF STOHR DIETTER 权利人:UNIV CONCEPCION; CASTRO INOSTROZA ERICA; BORQUEZ YANEZ RODRIGO; GONZALES RIQUELME MARGARITA; KLATTENHOFF STOHR DIETTER 摘要:The invention relates to technology comprising a probiotic formulation for topical use which includes (1) microspheres with a matrix composition made from cross-linked natural gelatine and (2) a viable probiotic strain of Lactobacillus spp . The invention is characterised mainly in the joint action of the two components, which is essential in order to obtain the intended effect. The invention also relates to a method for generating said microspheres and the use thereof in lesions such as wounds, ulcers, burns and/or surgery, including infected tissues and chronic infections. Said microspheres also have cosmetic and dermatological uses.
专利号:WO-2017095212-A1 优先权日:2015-11-30 标 题 :Biotechnological method for the detoxification and associated production of biofuels/biolubricants from oleaginous pastes 发明人:RODRÃ?GUEZ GONZÃ?LEZ JORGE ALBERTO; MATEOS DÃ?AZ JUAN CARLOS; CAMACHO RUIZ ROSA MARÃ?A; COSÃ?O CUADROS RICARDO; PADILLA CAMBEROS EDUARDO; MÃ?RQUEZ AGUIRRE ANA LAURA; CANALES AGUIRRE ALEJANDRO ARTURO; RODRÃ?GUEZ GONZÃ?LEZ ERNESTO; ESPINOSA ANDREWS HUGO; JIMÉNEZ OCAMPO RAFAEL 权利人:CENTRO DE INVESTIGACIÓN Y ASISTENCIA EN TECNOLOGÃ?A Y DISEÑO DEL ESTADO DE JALISCO A C; INST NAC DE INVESTIG FORESTALES AGRÃ?COLAS Y PECUARIAS 摘要:The present invention relates to a biotechnological method that allows the detoxification and associated production of biofuels/biolubricants from oleaginous pastes, particularly from jatropha paste and castor-oil plant paste. The method comprises grinding, optionally followed by sterilising the paste, and subsequently inoculating same with an innocuous filamentous fungus that detoxifies the paste up to 99% and produces a biocatalyst with lipase activity. The paste with lipase activity is dried and used in the synthesis of biofuels/biolubricants, using the lipids remaining from the pastes in the presence of alcohols, in the absence or presence of an apolar solvent with a log of P between 2 and 5.
专利号:WO-2015015035-A1 优先权日:2013-07-31 标 题 :Method for the synthesis of covalent organic frameworks 发明人:ZAMORA ABANADES FÉLIX JUAN; MAS-BALLESTÉ RUBÉN; RODRÃ?GUEZ SAN MIGUEL DAVID; SEGURA CASTEDO JOSÉ LUIS; DE LA PEÑA RUIGÓMEZ ALEJANDRO 权利人:FUNDACIÓN IMDEA NANOCIENCIA; UNIV AUTÓNOMA DE MADRID; UNIV MADRID COMPLUTENSE 摘要:The invention relates to a method for producing covalent organic frameworks (COF) comprising a plurality of sub-units of amines and aldehydes. Said method involves the formation of polyimines by means of condensation reactions. The invention also relates to the COFs that can be produced by means of said method, in the form of a gel and in the form of a solid with a microstructure similar to a sphere. The invention further relates to the uses of the COFs produced in the coating of surfaces, ink-jet printing, spray deposition, material encapsulation and coordination chemistry.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
1: Kerscher M, Reuther T, Krueger N, Buntrock H. Effects of an oral contraceptive containing chlormadinone acetate and ethinylestradiol on hair and skin quality in women wishing to use hormonal contraception. J Eur Acad Dermatol Venereol. 2013 May;27(5):601-8. doi: 10.1111/j.1468-3083.2012.04497.x. Epub 2012 Mar 10. doi: 10.2165/1153874-S0-000000000-00000. Review. doi: 10.1177/0748233710380216. Epub 2010 Aug 16. e1-2. doi: 10.1016/j.genhosppsych.2013.10.014. Epub 2013 Oct 30. doi: 10.1016/j.contraception.2011.12.011. Epub 2012 Mar 28. doi: 10.2165/1153875-S0-000000000-00000. doi: 10.1016/j.contraception.2011.03.024. Epub 2011 May 26. doi: 10.1016/j.contraception.2012.02.004. Epub 2012 Mar 23. doi: 10.1055/s-0031-1296455. Epub 2006 May 15. doi: 10.2165/11586720-000000000-00000. 13: Fiet J, Giton F, Auzerie J, Galons H. Development of a new sensitive and specific time-resolved fluoroimmunoassay (TR-FIA) of chlormadinone acetate in the serum of treated menopausal women. Steroids. 2002 Dec;67(13-14):1045-55. doi: 10.1177/1933719110371515. German. doi: 10.2165/11585900-000000000-00000. doi: 10.1016/j.fertnstert.2009.06.057. Epub 2009 Aug 25. Japanese.
合成参考文献
摘要: 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要: 摘要:Sigma-Aldrich; Material Safety Data Sheet for Chlormadinone acetate. Product Number C5145. Version 4.0 (March 2010). Available from, as of March 3, 2011: 摘要:Mill T et al; Environmental Fate and Exposure Studies Development of a PC-SAR for Hydrolysis: Esters, Alkyl Halides and Epoxides. EPA Contract No. 68-02-4254. Menlo Park, CA: SRI International (1987)