专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-2009176740-A1 优先权日:2007-11-30 标题:Treatment of neurological conditions by the co-administration of aniracetam and l-alpha glycerylphosphorylcholine 发明人:PHILLIPS II DAUGLAS JAMES 权利人:PHILLIPS II DAUGLAS JAMES 摘要:Aniracetam (1-[(4-methoxybenzoyl)]-2-pyrrolidinone) is co-administered with the acetylcholine precursor 1-alpha glycerylphosphorylcholine (Alpha GPC, choline alfoscerate, choline alphoscerate) to potentiate cognition enhancing effects in healthy subjects and patients suffering from neurological conditions including Alzheimer's Disease (AD), attention deficit disorder (ADD), Parkinson's Disease, schizophrenia, vascular dementia, post stroke aphasia, anxiety disorders, cerebral atrophy, chronic alcoholism, Down syndrome, dyslexia, and various other neurodegenerative conditions. The co-administration of aniracetam (and other racetam derivatives including oxiracetam) with the acetylcholine precursor 1-alpha glycerylphosphorylcholine decreases negative side-effects such as severe headaches while increasing the synthesis and release of the neurotransmitters acetylcholine and glutamate to facilitate proper brain functioning.
专利号:WO-2009094569-A2 优先权日:2008-01-25 标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
专利号:US-2005222431-A1 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
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合成参考文献
参考文献:10.1016/s0021-5198(19)39754-9|10.1254/jjp.58.117 摘要:Iwasaki K, Matsumoto Y, Fujiwara M. Effect of Nebracetam on the Disruption of Spatial Cognition in Rats. Japanese Journal of Pharmacology. 1992;58(2):117–26. doi: 10.1016/s0021-5198(19)39754-9.