📜2-三氟甲基吩噻嗪置于potassium Phosphate,Sodium Hydride体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 52.0H,反应生成三氟拉嗪 参考文献:Synthesis And Antitubercular Activity Of Phenothiazines With Reduced Binding To Dopamine And Serotonin Receptors 标题:Synthesis And Antitubercular Activity Of Phenothiazines With Reduced Binding To Dopamine And Serotonin Receptors 摘要:Analogs Of The Psychotropic Phenothiazines Were Synthesized And Examined As Antitubercular Agents Against Mycobacterium Tuberculosis H37Rv. The Compounds Were Subsequently Counter-Screened For Binding To The Dopaminergic-Receptor Subtypes D1,D2,D3 And The Serotonergic-Receptor Subtypes 5-Ht1A,5-Ht2A,And 5-Ht2C. The Most Active Compounds Showed Mics From 2 To 4 Mu G/ml And Had Overall Reduced Binding To The Dopamine And Serotonin Receptors Compared To Chlorpromazine And Trifluoperazine. (C) 2007 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2007.03.064
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
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-6264962-B1 优先权日:1997-12-19 标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition 发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE 权利人:OREAL 摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-6660283-B2 优先权日:1997-12-19 标 题 :Use of cinnamic acid, or of at least one of its derivatives in a cosmetic composition 发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE 权利人:OREAL 摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids.The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.
1: Tse WS, Wong AS, Chan F, Pang AH, Bond AJ, Chan CK. Different mechanisms of risperidone result in improved interpersonal trust, social engagement and cooperative behavior in patients with schizophrenia compared to trifluoperazine. Psychiatry Clin Neurosci. 2016 May;70(5):218-26. doi: 10.1111/pcn.12382. Epub 2016 Apr 5. doi: 10.4103/0972-3919.178256. 3: Howland RH. Trifluoperazine: A Sprightly Old Drug. J Psychosoc Nurs Ment Health Serv. 2016 Jan 1;54(1):20-2. doi: 10.3928/02793695-20151223-01. doi: 10.1002/prot.24781. Epub 2015 Mar 25. 5: Guo J, Ni C, Liu X, Liu T. Ganoderic acid B's influence towards the therapeutic window of trifluoperazine (TFP). Afr Health Sci. 2015 Mar;15(1):146-9. doi: 10.4314/ahs.v15i1.20.
合成参考文献
参考文献:10.2165/11530130-000000000-00000 摘要:Hasnain M, Vieweg WV, Fredrickson SK. Metformin for atypical antipsychotic-induced weight gain and glucose metabolism dysregulation: review of the literature and clinical suggestions. CNS Drugs. 2010 Mar;24(3):193–206. doi: 10.2165/11530130-000000000-00000. 参考文献:10.4103/0019-5545.82558 摘要:Andrade C. How to write a good abstract for a scientific paper or conference presentation. Indian J Psychiatry. 2011 Apr;53(2):172–5. 参考文献:10.4103/0019-5545.82562 摘要:Kumar PN, Thomas B. Hyperglycemia associated with olanzapine treatment. Indian J Psychiatry. 2011 Apr;53(2):176–7. 参考文献:10.1186/1476-0711-10-30 摘要:Riordan JT, Dupre JM, Cantore-Matyi SA, Kumar-Singh A, Song Y, Zaman S, Horan S, Helal NS, Nagarajan V, Elasri MO, Wilkinson BJ, Gustafson JE. Alterations in the transcriptome and antibiotic susceptibility of Staphylococcus aureus grown in the presence of diclofenac. Annals of Clinical Microbiology and Antimicrobials. 2011 Jul 21;10(1):30. doi: 10.1186/1476-0711-10-30.