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-11485721-B2 优先权日:2017-11-21 标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses 发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN 权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST 摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.
专利号:US-8183409-B2 优先权日:2004-05-06 标题:High yield and rapid synthesis methods for producing metallo-organic salts 发明人:CHRISTGAU STEPHAN; ANDERSEN JENS E T 权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T; OSTEOLOGIX AS 摘要:A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.
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.)).
专利号:WO-2023075715-A1 优先权日:2021-10-26 标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids) 发明人:OYTUN FARUK; CAN EFE 权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI 摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
1: Payandemehr B, Khoshneviszadeh M, Varastehmoradi B, Gholizadeh R, Bahremand T, Attar H, Bahremand A, Dehpour AR. A COX/5-LOX Inhibitor Licofelone Revealed Anticonvulsant Properties Through iNOS Diminution in Mice. Neurochem Res. 2015 Sep;40(9):1819-28. doi: 10.1007/s11064-015-1669-z. Epub 2015 Jul 28. doi: 10.1007/s12031-014-0414-4. Epub 2014 Sep 10. doi: 10.1007/s00590-014-1534-9. Epub 2014 Sep 9. doi: 10.1158/1940-6207.CAPR-14-0087. Epub 2014 May 2. 6: Kus G, Oztopcu-Vatan P, Uyar R, Kabadere S. Cytotoxic and apoptotic functions of licofelone on rat glioma cells. Acta Biol Hung. 2013 Dec;64(4):438-52. doi: 10.1556/ABiol.64.2013.4.4. doi: 10.3109/01480545.2013.806525. Epub 2013 Jul 8. doi: 10.1523/JNEUROSCI.6128-11.2013. 9: Kumar A, Vashist A, Kumar P, Kalonia H, Mishra J. Potential role of licofelone, minocycline and their combination against chronic fatigue stress induced behavioral, biochemical and mitochondrial alterations in mice. Pharmacol Rep. 2012;64(5):1105-15. doi: 10.1089/neu.2012.2587. Epub 2013 Jan 23.
合成参考文献
参考文献:10.1002/art.10357 摘要:Paredes Y, Massicotte F, Pelletier JP, Martel-Pelletier J, Laufer S, Lajeunesse D. Study of the role of leukotriene B()4 in abnormal function of human subchondral osteoarthritis osteoblasts: effects of cyclooxygenase and/or 5-lipoxygenase inhibition. Arthritis Rheum. 2002 Jul;46(7):1804–12. doi: 10.1002/art.10357. 摘要:Boileau C, Martel-Pelletier J, Jouzeau JY, Netter P, Moldovan F, Laufer S, Tries S, Pelletier JP. Licofelone (ML-3000), a dual inhibitor of 5-lipoxygenase and cyclooxygenase, reduces the level of cartilage chondrocyte death in vivo in experimental dog osteoarthritis: inhibition of pro-apoptotic factors. J Rheumatol. 2002 Jul;29(7):1446–53. 参考文献:10.2165/00063030-200418010-00003 摘要:Malemud CJ. Cytokines as therapeutic targets for osteoarthritis. BioDrugs. 2004;18(1):23–35. doi: 10.2165/00063030-200418010-00003. 参考文献:10.1097/01.hco.0000136130.95746.14 摘要:Hinz B, Brune K. Pain and osteoarthritis: new drugs and mechanisms. Curr Opin Rheumatol. 2004 Sep;16(5):628–33. doi: 10.1097/01.hco.0000136130.95746.14. 参考文献:10.1016/j.ejphar.2006.06.052 摘要:Rotondo S, Dell'Elba G, Manarini S, Cerletti C, Evangelista V. The lipoxygenase-cyclooxygenase inhibitor licofelone prevents thromboxane A2-mediated cardiovascular derangement triggered by the inflammatory peptide fMLP in the rabbit. Eur J Pharmacol. 2006 Sep 28;546(1-3):95–101. doi: 10.1016/j.ejphar.2006.06.052.