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-3906004-A 优先权日:1968-12-09 标题 :Stereoselective synthesis of intermediate for preparation of meso-nordihydroguaiaretic acid 发明人:PERRY CLARK WILLIAM 权利人:HOFFMANN LA ROCHE 摘要:This invention is directed to the stereoselective synthesis of the food additive meso-nordihydroguaiaretic acid from a protected ortho dihydroxy benzene and intermediates in this synthesis.
专利号:US-7507864-B2 优先权日:2006-08-01 标题:Method for the synthesis of curcumin analogues 发明人:MILLER JEFFREY CHRISTOPHER; MITCHELL MIGUEL O 权利人:SALISBURY UNIVERSITY 摘要:The present invention relates to improved methods for achieving the synthesis of 1,7-diaryl-1,6-heptadiene-3,5-diones, and in particular curcumin and its analogues. The invention provides a process for synthesizing such compounds in substantial yield and purity using environmentally benign processes and materials. The invention also relates to the use of such synthesized products in the treatment of Alzheimer's Disease and other diseases.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-2025235415-A1 优先权日:2022-02-23 标 题:Modulation of human breast milk composition 发明人:ROSS MICHAEL G; DESAI MINA 权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER 摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.
1: Gowri MS, Azhar RK, Kraemer FB, Reaven GM, Azhar S. Masoprocol decreases rat lipolytic activity by decreasing the phosphorylation of HSL. Am J Physiol Endocrinol Metab. 2000 Sep;279(3):E593-600. doi: 10.1152/ajpendo.2000.279.3.E593. 49(9):1106-10. doi: 10.1053/meta.2000.8604. 24(5 Pt 1):738-43. doi: 10.1016/0190-9622(91)70113-g. 25(1):183. doi: 10.3390/molecules25010183. 5: Gowri MS, Reaven GM, Azhar S. Effect of masoprocol on glucose transport and lipolysis by isolated rat adipocytes. Metabolism. 1999 Apr;48(4):411-4. doi: 10.1016/s0026-0495(99)90096-3. 346(1):77-9. doi: 10.1016/s0014-2999(98)00139-3. 31(2 Pt 1):295-7. doi: 10.1016/s0190-9622(08)81988-3. 69(1):49-59. doi: 10.33549/physiolres.934335. Epub 2019 Dec 19. 9(1):2937. doi: 10.1038/s41598-019-39480-z. 10: Mundhe N, Kumar P, Arora I, Ahmed S, Lahkar M. Differential effect of NDGA on cisplatin-induced nephrotoxicity in Spargue-Dawley rats. Immunopharmacol Immunotoxicol. 2019 Feb;41(1):68-75. doi: 10.1080/08923973.2018.1547741. Epub 2019 Jan 3.
合成参考文献
参考文献:10.1007/s10549-005-9081-z 摘要:Altundag K, Altundag O, Karakaya E, Akyurek S. Overcoming trastuzumab resistance with nordihydroguaiaretic acid Breast Cancer Research and Treatment. 2005 Dec 01;96(3):301. doi: 10.1007/s10549-005-9081-z. 参考文献:10.1093/jxb/err143 摘要:Dong H, Zhen Z, Peng J, Chang L, Gong Q, Wang NN. Loss of ACS7 confers abiotic stress tolerance by modulating ABA sensitivity and accumulation in Arabidopsis. J Exp Bot. 2011 Oct;62(14):4875–87. 参考文献:10.1155/2011/385780 摘要:Burnett BP, Bitto A, Altavilla D, Squadrito F, Levy RM, Pillai L. Flavocoxid inhibits phospholipase A2, peroxidase moieties of the cyclooxygenases (COX), and 5-lipoxygenase, modifies COX-2 gene expression, and acts as an antioxidant. Mediators Inflamm. 2011;2011():385780. 参考文献:10.1016/j.cellsig.2011.07.002 摘要:Walters JN, Bickford JS, Beachy DE, Newsom KJ, Herlihy JH, Peck MV, Qiu X, Nick HS. cPLA2α gene activation by IL-1β is dependent on an upstream kinase pathway, enzymatic activation and downstream 15-lipoxygenase activity: A positive feedback loop. Cellular Signalling. 2011 Dec;23(12):1944–51. doi: 10.1016/j.cellsig.2011.07.002. 参考文献:10.1155/2011/467305 摘要:Babich H, Schuck AG, Weisburg JH, Zuckerbraun HL. Research Strategies in the Study of the Pro-Oxidant Nature of Polyphenol Nutraceuticals. Journal of Toxicology. 2011;2011():1–12. doi: 10.1155/2011/467305.