在 N-甲基吗啉,Benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate体系中,用 N,N-二甲基甲酰胺作为反应溶剂,反应 3.0H,获得 Carbetoin 参考文献:[En] Process For Large Scale Liquid Phase Synthesis Of Carbetoin And Its Novel Intermediates[Fr] Pr°Cédé De Synthèse En Phase Liquide Et à Grande échelle De La Carbétoine Et Ses Nouveaux Intermédiaires 标题:[En] Process For Large Scale Liquid Phase Synthesis Of Carbetoin And Its Novel Intermediates[Fr] Pr°Cédé De Synthèse En Phase Liquide Et à Grande échelle De La Carbétoine Et Ses Nouveaux Intermédiaires 摘要:揭示了一种用于大规模液相合成卡贝托辛的方法.还揭示了公式(A),公式(B)的新型中间体以及它们的制备方法.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:WO-2017175233-A1 优先权日:2016-04-04 标 题:Process for large scale liquid phase synthesis of carbetocin and its novel intermediates 发明人:Mohammed Khalid Anwer; Mohammed Mohosin Layek 权利人:DAVULURI RAMAMOHAN RAO 摘要:A process for large scale liquid phase synthesis of Carbetocin is disclosed. Novel intermediates of formula (A), formula (B), and processes for their preparation are also disclosed.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2003147958-A1 优先权日:2002-01-29 标题 :Biodegradable multi-block copolymers of poly(amino acid)s and poly(ethylene glycol) for the delivery of bioactive agents 发明人:AHN CHEOL-HEE; CHAE SU YOUNG 摘要:This patent discloses the synthesis of a multi-block copolymer containing poly(amino acids) (PAA) and a hydrophilic polymer which are degradable under physiological conditions. Control over the degradation rate of the obtained copolymers is achieved by introducing ester, amide or urethane groups as a biodegradable linkage connecting the PAA and the hydrophilic polymer. The biodegradable multi-block copolymers display high transfection efficiency in plasmid delivery with low cytotoxicity.
专利号:WO-0054773-A1 优先权日:1999-03-12 标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use 发明人:GARVEY DAVID S 权利人:NITROMED INC; GARVEY DAVID S 摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
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合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from 参考文献:10.1038/s41388-020-01415-8 摘要:Liu H, Gruber CW, Alewood PF, Möller A, Muttenthaler M. The oxytocin receptor signalling system and breast cancer: a critical review. Oncogene. 2020 Aug 11;39(37):5917–32. doi: 10.1038/s41388-020-01415-8. 参考文献:10.1186/s13063-022-06140-z 摘要:Brenner A, Roberts I, Balogun E, Bello FA, Chaudhri R, Fleming C, Javaid K, Kayani A, Lubeya MK, Mansukhani R, Olayemi O, Prowse D, Vwalika B, Shakur-Still H. Postpartum haemorrhage in anaemic women: assessing outcome measures for clinical trials. Trials. 2022 Mar 18;23(1):220.