4-乙酰基氨基苯硼酸频哪醇酯置于水体系中,用 乙醇 用作溶剂,化学反应生成4-乙酰胺基苯硼酸 参考文献:Susceptibility To Hydrolysis Of Phenylboronic Pinacol Esters At Physiological Ph 标题:Susceptibility To Hydrolysis Of Phenylboronic Pinacol Esters At Physiological Ph 摘要:摘要:硼酸及其酯是设计新药物和药物输送装置的高度考虑化合物,特别是作为适用于中子俘获疗法的硼载体.然而,这些化合物在水中只具有较小的稳定性.本文描述了一些苯硼酸酯的水解过程.动力学取决于芳香环中的取代基.此外,Ph值强烈影响反应速率,这在生理ph下会显著加快.因此,在考虑将这些硼酸酯用于药理学目的时,必须谨慎对待. Doi:10.2478/s11532-012-0159-2
专利信息
专利号:US-2012077802-A1 优先权日:2009-06-10 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-7250410-B2 优先权日:2001-06-07 标题:Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof 发明人:BOURGUIGNON JEAN-JACQUES; LAGOUGE YAN; LUGNIER CLAIRE; KLOTZ EVELINE; MACHER JEAN-PAUL; RABOISSON PIERRE; SCHULTZ DOMINIQUE 权利人:VIA PHARMACEUTICALS INC 摘要:The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates. The inventive compounds more particularly correspond to general formula (I):
专利号:CN-111892519-A 优先权日:2020-08-12 标题:Synthesis method of diaryl disulfide compound