📜3-溴-2,6-二甲氧基苯甲酸置于sodium Hydroxide,氯化亚砜体系中,用 氯仿 作为反应溶剂,化学反应 0.67H,反应生成 瑞莫必利 参考文献:Potential Neuroleptic Agents. 2,6-Dialkoxybenzamide Derivatives With Potent Dopamine Receptor Blocking Activities 标题:Potential Neuroleptic Agents. 2,6-Dialkoxybenzamide Derivatives With Potent Dopamine Receptor Blocking Activities 摘要:A Series Of Some Novel N-(L-Ethyl-2-Pyrrolidinylmethyl)Benzamides Was Synthesized And Tested For Dopamine Receptor Blockade In Vivo By The Ability To Block The Apomorphine Syndrome In The Rat. Several Compounds Were Considerably More Potent Than Sulpiride As Dopamine Receptor Blockers And Displayed Low Liability To Induce Extrapyramidal Side Effects (Catalepsy) In The Rat. The Blockade Of Dopamine Receptor Activity In Vivo Was Mainly Confined To The Levorotatory Isomers Having The S Absolute Configuration. The Structure-Activity Relationships Are Discussed. DOI:10.1021/jm00353A003
专利号:US-9884844-B2 优先权日:2012-12-31 标 题:Heterocyclic compounds and methods of use thereof 发明人:FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:US-9670230-B2 优先权日:2012-11-29 标题 :Heteroaryl compounds and methods of use thereof 发明人:CAMPBELL JOHN EMMERSON; JONES PHILIP 权利人:SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
专利号:CN-101535336-A 优先权日:2006-11-10 标题 :Synthesis of Phthalamide and Its Dimer
专利号:US-9617230-B2 优先权日:2014-12-22 标题:Creatine prodrugs, compositions and methods of use thereof 发明人:BRUBAKER WILLIAM F 权利人:FARMINGTON PHARMA DEV 摘要:The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.
专利号:US-11021501-B2 优先权日:2015-03-30 标题:Creatine phosphate analog prodrugs, compositions and methods of use thereof 发明人:BRUBAKER WILLIAM F 权利人:FARMINGTON PHARMA DEV 摘要:The invention describes membrane permeable creatine phosphate analog prodrugs, pharmaceutical compositions comprising membrane permeable creatine phosphate analog prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof.
1: Yisak W, Farde L, von Bahr C, Nilsson LB, Fredriksson G, Ogenstad S. Interaction study between remoxipride and biperiden. Psychopharmacology (Berl). 1993;111(1):27-32. doi: 10.1111/j.1365-2125.2010.03758.x. 3: Stevens J, Ploeger BA, van der Graaf PH, Danhof M, de Lange EC. Systemic and direct nose-to-brain transport pharmacokinetic model for remoxipride after intravenous and intranasal administration. Drug Metab Dispos. 2011 Dec;39(12):2275-82. doi: 10.1124/dmd.111.040782. Epub 2011 Sep 8. 6: Wålinder J, Holm AC. Experiences of long-term treatment with remoxipride: efficacy and tolerability. Acta Psychiatr Scand Suppl. 1990;358:158-63. Review.