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-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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-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-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
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.
1: Slawson MH, Johnson-Davis KL. Quantitation of Haloperidol, Fluphenazine, Perphenazine, and Thiothixene in Serum or Plasma Using Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS). Methods Mol Biol. 2016;1383:49-57. doi: 10.1007/978-1-4939-3252-8_6. doi: 10.1097/JCP.0000000000000359. doi: 10.1002/14651858.CD003443.pub3. Review. doi: 10.3390/ijms151223909. 5: Tardy M, Huhn M, Engel RR, Leucht S. Perphenazine versus low-potency first-generation antipsychotic drugs for schizophrenia. Cochrane Database Syst Rev. 2014 Oct 7;10:CD009369. doi: 10.1002/14651858.CD009369.pub2. Review. doi: 10.4088/JCP.13m08695. doi: 10.1097/EJA.0000000000000048. 8: Activation of PP2A by perphenazine induces apoptosis in T-ALL. Cancer Discov. 2014 Mar;4(3):OF14. doi: 10.1158/2159-8290.CD-RW2014-017. Epub 2014 Jan 23. doi: 10.1111/jphp.12174. Epub 2013 Nov 10. doi: 10.1016/j.talanta.2013.09.048. Epub 2013 Oct 5. doi: 10.1007/s11060-013-1308-y. Epub 2013 Nov 17. Review. doi: 10.1097/NMD.0000000000000065.
合成参考文献
参考文献:10.2165/11592020-000000000-00000 摘要:Pringsheim T, Lam D, Ching H, Patten S. Metabolic and neurological complications of second-generation antipsychotic use in children: a systematic review and meta-analysis of randomized controlled trials. Drug Saf. 2011 Aug 01;34(8):651–68. doi: 10.2165/11592020-000000000-00000. 参考文献:10.1007/s00216-011-5187-9 摘要:Remane D, Meyer MR, Wissenbach DK, Maurer HH. Ultra high performance liquid chromatographic-tandem mass spectrometric multi-analyte procedure for target screening and quantification in human blood plasma: validation and application for 31 neuroleptics, 28 benzodiazepines, and Z-drugs. Analytical and Bioanalytical Chemistry. 2011 Jul 21;401(4):1341. doi: 10.1007/s00216-011-5187-9.