专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:WO-2006052263-A1 优先权日:2004-11-10 标题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:RANADE VASANT V; SOMBERG JOHN CHARIN 权利人:RANADE VASANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effects mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and in the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in
专利号:US-2009325918-A1 优先权日:2008-06-16 标 题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:SOMBERG JOHN C; RANADE VASSANT V 权利人:SOMBERG JOHN C; RANADE VASSANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.
专利号:US-9573873-B2 优先权日:2014-06-03 标题:Catalytic method for dibenzocycloheptane synthesis and allocolchicinoid synthesis 发明人:GREEN JAMES; MEHDI MARIAM; DJURDJEVIC SINISA 权利人:UNIV OF WINDSOR 摘要:In a non-limiting embodiment, there is provided a compound of formula (I), which may permit for a method or use in treating or preventing a cancer, such as pancreatic cancer or leukemia. In one embodiment, there is also provide a method of preparing a compound of formula (Ia), the method including conducting a cyclization reaction of a compound of formula (III) to obtain a compound of formula (IV), wherein conducting the cyclization reaction comprises conducting a Michael reaction in the presence of a Lewis acid.
1: Dragoman MV, Gaffield ME. The safety of subcutaneously administered depot medroxyprogesterone acetate (104mg/0.65mL): A systematic review. Contraception. 2016 Sep;94(3):202-15. doi: 10.1016/j.contraception.2016.02.003. Epub 2016 Feb 10. Review. Review. doi: 10.1016/j.jsbmb.2015.08.013. Epub 2015 Aug 19. Review. doi: 10.1007/s00404-014-3417-z. Epub 2014 Aug 14. Review. doi: 10.1016/j.jsbmb.2013.11.011. Epub 2013 Nov 26. Review. doi: 10.1186/1742-4755-10-39. Review. 7: Guirguis-Blake J. Copper intrauterine device vs. depot medroxyprogesterone acetate for contraception. Am Fam Physician. 2011 Jan 1;83(1):35-6. Review. doi: 10.1016/j.clinthera.2011.02.008. Epub 2011 Mar 12. Review. doi: 10.1016/j.contraception.2009.03.023. Epub 2009 Jun 13. Review. doi: 10.1517/14656560902960162. Review. doi: 10.1016/j.contraception.2008.10.016. Epub 2009 Jan 15. Review. doi: 10.1038/ncpcardio1234. Epub 2008 Jun 3. Review. doi: 10.1007/s00404-007-0497-z. Epub 2008 May 10. Review. doi: 10.1016/j.contraception.2007.10.005. Review. Review. Review. Canadian contraception consensus--update on Depot Medroxyprogesterone Acetate (dmpa). J Obstet Gynaecol Can. 2006 Apr;28(4):305-13. English, French. Bone loss associated with long-term use of depot medroxyprogesterone acetate. Hong Kong Med J. 2005 Dec;11(6):491-5. Review. Review. German. Review. Erratum in: J Am Acad Nurse Pract. 2004 May;16(5):186.
合成参考文献
参考文献:10.7326/0003-4819-152-4-201002160-00002 摘要:Summaries for patients: The effect of estrogen plus progestin on coronary heart disease. Ann Intern Med. 2010 Feb 16;152(4):I–40. doi: 10.7326/0003-4819-152-4-201002160-00002. 参考文献:10.7326/0003-4819-152-4-201002160-00005 摘要:Toh S, Hernández-Díaz S, Logan R, Rossouw JE, Hernán MA. Coronary heart disease in postmenopausal recipients of estrogen plus progestin therapy: does the increased risk ever disappear A randomized trial. Ann Intern Med. 2010 Feb 16;152(4):211–7. 参考文献:10.1016/j.contraception.2009.11.001 摘要:Hillman JB, Negriff S, Dorn LD. Perceived competence and contraceptive use during adolescence. Contraception. 2010 Mar;81(3):249–53. doi: 10.1016/j.contraception.2009.11.001. 参考文献:10.1007/s10549-011-1605-0 摘要:Fu P, Ibusuki M, Yamamoto Y, Hayashi M, Murakami K, Zheng S, Iwase H. Insulin-like growth factor-1 receptor gene expression is associated with survival in breast cancer: a comprehensive analysis of gene copy number, mRNA and protein expression. Breast Cancer Res Treat. 2011 Nov;130(1):307–17. doi: 10.1007/s10549-011-1605-0. 摘要:Leonetti HB, Landes J, Steinberg D, Anasti JN. Transdermal progesterone cream as an alternative progestin in hormone therapy. Altern Ther Health Med. 2005 Nov;11(6):36–8.