专利号:US-8754259-B2 优先权日:2008-08-15 标 题 :Synthesis of cyclohexane derivatives useful as sensates in consumer products 发明人:YELM KENNETH EDWARD; BUNKE GREGORY MARK; HAUGHT JOHN CHRISTIAN 权利人:PROCTER & GAMBLE; PROCTER & GAMBLE 摘要:The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect. Preparation schemes for neoisomers of other menthyl derivatives which are useful as coolants, including esters, ethers, carboxy esters and other N-substituted carboxamides are also provided.
专利号:WO-2020043716-A1 优先权日:2018-08-27 标题 :Pharmacological targeting of de novo serine/glycine synthesis 发明人:CAMMUE BRUNO; DE KEERSMAECKER KIM; GEERAERTS SHAUNI; KAMPEN KIM; THEVISSEN KARIN 权利人:UNIV LEUVEN KATH 摘要:The invention relates to sertraline for use in the treatment of a cancer with increased serine/glycine synthesis, such as certain types of breast cancer or T-cell acute lymphoblastic leukaemia. Increased serine/glycine synthesis is for example obtained via increased expression of PSPH, PHGDH, PSAT1, SHMT1 or SHMT2.
专利号:US-11970551-B2 优先权日:2018-08-20 标题 :Solution phase routes for WNT hexapeptides 发明人:HENRIKSEN DENNIS 权利人:WNTRESEARCH AB 摘要:The present disclosure relates generally to the field of polypeptide synthesis, and more particularly, to the solution phase synthesis of the Wnt hexapeptide Foxy-5 and protected derivatives and peptide fragments thereof.
专利号:US-2024229047-A1 优先权日:2021-07-12 标 题 :Carboxylic acid platform for fuel and chemical production at high carbon and energy efficiency 发明人:GONZALEZ RAMON; CLOMBURG JAMES MACALLISTER; ZHU FAYIN; LEE SEUNG HWAN; NEZAMIRAD MOHAMMADREZA 权利人:MOJIA BIOTECH PTE LTD 摘要:This disclosure provides a new conceptual framework in which orthogonal, new-to-nature carbon and energy conversion pathways facilitate the synthesis of fuels and chemicals from carboxylic acid intermediates (CAis) driven by genetically altered microorganisms. This allows the CAi platform to generate diverse products at ≥100% carbon yield while retaining the established high product and energy efficiencies of fermentative metabolism. In another embodiment, a carboxylic acid platform for fuel and chemical production at high carbon and energy efficiency is also provided.
专利号:WO-2024262968-A1 优先权日:2023-06-20 标题 :Non-natural oligonucleotide-encoded library and screening method thereof 发明人:LIM HYUN SUK; PARK JUN HYUNG; KIM JUNG YEON; SEO CHANG DEOK 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:The present invention relates to a non-natural oligonucleotide-encoded library and a screening method thereof. More specifically, the PNA-encoded library technology of the present invention enables the synthesis of structurally diverse libraries by introducing various types of reactions that could not be implemented by conventional encoded library technology. Therefore, by utilizing the screening technology of the PNA-encoded library of the present invention, it is possible to screen for hit compounds at low cost and high efficiency, thereby not only securing new drug candidate materials, but also reducing the development period and development costs of new drugs.
专利号:CA-2731967-A1 优先权日:2008-08-15 标 题:Synthesis of cyclohexane derivatives useful as sensates in consumer products
1: Long Y, Chen W, Lin Z, Sun H, Xia M, Zheng W, Li Z. Inhibition of HERG potassium channels by domiphen bromide and didecyl dimethylammonium bromide. Eur J Pharmacol. 2014 Aug 15;737:202-9. doi: 10.1016/j.ejphar.2014.05.002. Epub 2014 May 15. 2: Podolska M, Kulik A, Białecka W, Kwiatkowska-Puchniarz B, Mazurek A. HPLC method for identification and quantification of three active substances in a dermatological preparation--Viosept ointment. Acta Pol Pharm. 2014 Sep-Oct;71(5):709-19. doi: 10.1111/j.1467-2494.1987.tb00473.x. Epub 2005 Oct 19. doi: 10.1016/j.ejphar.2012.08.012. Epub 2012 Sep 5. 8: Egashira T, Nakagawa K, Shimamoto M, Kaneko O, Sadaoka K. Proceedings: Pharmacological study of dodecyl dimethyl-2-phenoxyethyl ammonium bromide (domiphen). Jpn J Pharmacol. 1974;24(0):s:37. doi: 10.1088/0957-4484/23/46/465602. Epub 2012 Oct 24. doi: 10.1016/j.ijpharm.2010.08.042. Epub 2010 Sep 9. Chinese. Epub 2006 Jan 18. Greek, Modern.
合成参考文献
摘要:Handbook of Toxicology, 4 vols., Philadelphia, W.B. Saunders Co., 1956-59, 1(222), 1955 摘要:Federation Proceedings, Federation of American Societies for Experimental Biology., 6(307), 1947 摘要:Reynolds, J.E.F., Prasad, A.B. (eds.) Martindale-The Extra Pharmacopoeia. 28th ed. London: The Pharmaceutical Press, 1982., p. 561 摘要: 摘要:NIOSH; National Occupational Exposure Survey (NOES) (1983)