专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound 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 invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-11384044-B2 优先权日:2017-08-03 标 题 :Method for introducing substituent into α,β-unsaturated ketone and method for synthesizing prostaglandin using the same 发明人:SUZUKI MASAAKI; KOYAMA HIROKO 权利人:NAT CT GERIATRICS & GERONTOLOGY 摘要:The present invention provides a method for introducing substituents into the α-position and the β-position of an α,β-unsaturated ketone, which not only can be used for the synthesis of a prostaglandin by a three-component coupling process, but also enables synthesis of a prostaglandin in a high yield by one-pot operation without requiring the use of a large excess amount of any of the three components required for the synthesis or using a highly toxic heavy metal as a catalyst or a solvent that is highly toxic to living bodies, and a method for synthesizing a prostaglandin using the same technical means. n The method for introducing substituents into an α,β-unsaturated ketone according to the present invention is a method for introducing substituents into the carbon at the α-position and the carbon at the β-position of an α,β-unsaturated ketone, including: a first step of mixing alkyllithium and trialkylalkenyl tin in which tin atom binds to the vinyl position of the alkenyl group; a second step of mixing the mixture of the first step and dialkylzinc; a third step of mixing the mixture of the second step and an α,β-unsaturated ketone; and a fourth step of mixing the mixture of the third step and a trifluoromethanesulfonate compound.
专利号:US-6653345-B2 优先权日:1997-09-16 标题 :C-C chemokine synthesis inhibitor 发明人:KURUMATANI HAJIMU; SASAKI RIE; KUMAGAI HIROKI 权利人:TORAY INDUSTRIES 摘要:A method of inhibiting mammalian C-C chemokine production by using a mammalian C-C chemokine synthesis inhibitor containing a prostaglandin I derivative as an active component to treat a variety of circulatory diseases, inflammation, allergic diseases, and renal diseases.
专利号:US-2014114086-A1 优先权日:2012-10-22 标 题:Clinprost, Isocarbacyclin And Analogs Thereof And Methods Of Making The Same 发明人:CROATT MITCHELL 权利人:UNIV NORTH CAROLINA AT GREENSBORO 摘要:In one aspect, methods of synthesizing clinprost, isocarbacyclin and analogs thereof are described herein which, in some embodiments, permit an abbreviated synthetic pathway in comparison to one or more prior synthetic methods. By providing a compact synthetic scheme, methods described herein can reduce cost, waste and time of clinprost and isocarbacyclin synthesis while facilitating the development and investigation of analogs of these compounds.
专利号:US-6087395-A 优先权日:1997-10-21 标题 :Isocarbacyclin derivatives as apoptosis inhibitors 发明人:WATANABE YASUYOSHI; HAZATO ATSUO; SUZUKI MASAAKI; WATANABE YUMIKO; SATO TAKUMI 权利人:JAPAN SCIENCE & TECH CORP; ATSUO HAZATO 摘要:The present invention provides an apoptosis inhibitor containing a 15R-isocarbacyclin derivative or a 15-deoxy-isocarbacyclin derivative, which can be manufactured easily and economically by means of chemical synthesis.
1: Umekubo N, Hayashi Y. Pot-Economical Total Synthesis of Clinprost. Org Lett. 2020 Dec 4;22(23):9365-9370. doi: 10.1021/acs.orglett.0c03616. Epub 2020 Nov 24. 48(10):1016-22. doi: 10.1111/j.2042-7158.1996.tb05893.x. 3(3):CD011033. doi: 10.1002/14651858.CD011033.pub3. Update in: Cochrane Database Syst Rev. 2020 May 4;5:CD011033. 4: Cacione DG, Macedo CR, do Carmo Novaes F, Baptista-Silva JC. Pharmacological treatment for Buerger's disease. Cochrane Database Syst Rev. 2020 May 4;5(5):CD011033. doi: 10.1002/14651858.CD011033.pub4. 5: Nagy EE, Hyatt IF, Gettys KE, Yeazell ST, Frempong SK Jr, Croatt MP. Sequential Pd(0)-, Rh(I)-, and Ru(II)-catalyzed reactions in a nine-step synthesis of clinprost. Org Lett. 2013 Feb 1;15(3):586-9. doi: 10.1021/ol303402e. Epub 2013 Jan 17.
合成参考文献
摘要:Kiso to Rinsho. Clinical Report., 29(2961), 1995