专利号:US-8604004-B2 优先权日:2007-10-04 标 题 :Moenomycin analogs, methods of synthesis, and uses thereof 发明人:KAHNE DANIEL; KAHNE SUZANNE WALKER; ADACHI MASAATSU; DOUD EMMA; FUSE SHINICHIRO; LIN XIAONAN; ZHANG YI; TSUKAMOTO HIROKAZU; OSTASH BOHDAN 权利人:KAHNE DANIEL; KAHNE SUZANNE WALKER; ADACHI MASAATSU; DOUD EMMA; FUSE SHINICHIRO; LIN XIAONAN; ZHANG YI; TSUKAMOTO HIROKAZU; OSTASH BOHDAN; HARVARD COLLEGE 摘要:The present invention provides novel moenomycin analogs as well as pharmaceutical compositions thereof, methods of synthesis, and methods of use in treating an infection by administering an inventive compound to a subject in need thereof. The moenomycin analogs may be prepared synthetically, biosynthetically, or semi-synthetically. The analogs are particularly useful in treating or preventing infections caused by Gram-positive organisms. Certain inventive compounds may have a broader spectrum of coverage, which includes Gram-negative organisms.
专利号:US-6787668-B2 优先权日:2000-04-13 标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors 发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH 权利人:PHARMACIA CORP 摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
专利号:RU-2399413-C2 优先权日:2008-09-02 标 题 :Catalyst for synthesis of 1-(dimethylamino)-3-alkyl-2-propines
专利号:RU-2440341-C2 优先权日:2009-12-07 标 题 :Method for combined synthesis of 4-alkylquinoline and (2,3-dialkyl-4-quinolinyl)-n, n-dimethylmethane amine
专利号:JP-2002522555-A 优先权日:1998-08-14 标题 :Chemical synthesis of exochelin
专利号:US-9403755-B2 优先权日:2013-01-18 标 题:Isometheptene isomer 发明人:LEDERMAN SETH; DAUGHERTY BRUCE; GERSHELL LELAND J; RIDEOUT DARRYL; KAWASAKI ANDREW 权利人:TONIX PHARMACEUTICALS INC; TONIX PHARMA HOLDINGS LTD (BERMUDA) 摘要:The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), n nor a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)-Isometheptene crystals data of X-ray crystallography are presented.
1: de Souza Carvalho D, Barea LM, Kowacs PA, Fragoso YD. Efficacy and tolerability of combined dipyrone, isometheptene and caffeine in the treatment of mild-to-moderate primary headache episodes. Expert Rev Neurother. 2012 Feb;12(2):159-67. doi: 10.1586/ern.11.193. doi: 10.1016/j.jflm.2009.07.006. Epub 2009 Aug 13. Epub 2006 Sep 25. Italian. Epub 2005 Oct 19. Italian.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1111/j.1526-4610.1980.hed2002103.x 摘要:Spierings EL, Saxena PR. Effect of isometheptene on the distribution and shunting of 15 microM microspheres throughout the cephalic circulation of the cat. Headache. 1980 Mar;20(2):103–6. doi: 10.1111/j.1526-4610.1980.hed2002103.x. 参考文献:10.1007/s11916-004-0043-7 摘要:Gladstein J. Children and adolescents with chronic daily headache. Curr Pain Headache Rep. 2004 Feb;8(1):71–5. doi: 10.1007/s11916-004-0043-7.