盐酸氯普噻吨置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应生成氯普噻吨 参考文献:Photophysics And Photochemistry Ofz-Chlorprothixene In Acetonitrile 标题:Photophysics And Photochemistry Ofz-Chlorprothixene In Acetonitrile 摘要:Abstractchlorprothixene (Cptx,Taractan®) Is A Low Potency Antipsychotic Mainly Used For The Treatment Of Psychotic Disorders (E.G. Schizophrenia) And Acute Mania occurring As Part Of Bipolar Disorders. As In The Case Of Other Numerous Drugs Used In The Treatment Of Psychiatric Disorders,Cptx Presents Geometric Isomerism. Therefore,In Vitro Irradiation Induces A Rapid Z/e Isomerization,Which Can Affect Its Pharmacokinetic Properties. This Photoisomerization Is Not Dependent On The Oxygen Concentration. The Z/e Quantum Yields Determined For Zcptx In Acetonitrile Are 0.22 And 0.21 In Anaerobic And Aerobic Environments,Respectively. In The Presence Of Water,Both Isomers Decompose To Produce 2‐chlorothioxanthone (Ctx) After Prolonged Irradiation. This Process Strongly Depends On The Water Concentration And The Irradiation Time,I.E. It Is Autocatalyzed By The Ctx Through A Triplet‐energy Transfer Mechanism. The Protonation State Of The Terminal Amino Group,On The Other Hand,Has No Effect On The Isomerization Process,But Inhibits The Formation Of Ctx. These Results Indicate That The Phototoxicity Of Zcptx Is Somehow Affected By The Formation Of Ctx. Doi:10.1111/j.1751-1097.2009.00584.X
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: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-4310535-A 优先权日:1976-11-30 标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens 发明人:PIERPAOLI WALTER 权利人:PIERPAOLI WALTER 摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.
专利号:US-2012282255-A1 优先权日:2011-04-07 标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence 发明人:PLUCINSKI GREG 权利人:PLUCINSKI GREG 摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.
专利号:US-2015352230-A1 优先权日:2013-01-11 标 题:Synthesis and isolation of dendrimer based imaging systems 发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK 权利人:UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).
专利号:US-2012232225-A1 优先权日:2009-08-26 标 题:Synthesis and isolation of dendrimer systems 发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL 权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well 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) diagnosis and/or therapy, pain therapy, etc.)).
1: Günther KN, Johansen SS, Wicktor P, Banner J, Linnet K. Segmental Analysis of Chlorprothixene and Desmethylchlorprothixene in Postmortem Hair. J Anal Toxicol. 2018 Jun 26. doi: 10.1093/jat/bky038. [Epub ahead of print] doi: 10.1016/j.ejphar.2016.03.009. Epub 2016 Mar 3. doi: 10.1093/jat/bku121. Epub 2014 Oct 22. Epub 2013 Apr 28. doi: 10.1016/j.ejphar.2012.07.039. Epub 2012 Aug 21. doi: 10.1111/j.1751-1097.2011.00906.x. Epub 2011 Mar 8. 7: Piñero LE, García C, Lhiaubet-Vallet V, Oyola R, Miranda MA. Photophysics and photochemistry of z-chlorprothixene in acetonitrile. Photochem Photobiol. 2009 Jul-Aug;85(4):895-900. doi: 10.1055/s-2007-1004590. doi: 10.1016/j.talanta.2007.09.018. Epub 2007 Sep 29.
合成参考文献
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