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-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-9220714-B2 优先权日:2006-03-16 标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis 发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG 权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND 摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
1: Rehm S, Solleveld HA, Portelli ST, Wier PJ. Histologic changes in ovary, uterus, vagina, and mammary gland of mature beagle dogs treated with the SERM idoxifene. Birth Defects Res B Dev Reprod Toxicol. 2007 Jun;80(3):225-32. Chinese. A cancer research (UK) randomized phase II study of idoxifene in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. Cancer Chemother Pharmacol. 2004 Apr;53(4):341-8. Epub 2004 Jan 13. 13: Omoya T, Shimizu I, Zhou Y, Okamura Y, Inoue H, Lu G, Itonaga M, Honda H, Nomura M, Ito S. Effects of idoxifene and estradiol on NF-kappaB activation in cultured rat hepatocytes undergoing oxidative stress. Liver. 2001 Jun;21(3):183-91. 28: Johnston SR, Riddler S, Haynes BP, A'Hern R, Smith IE, Jarman M, Dowsett M. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance. Br J Cancer. 1997;75(6):804-9.
合成参考文献
参考文献:10.7863/jum.1999.18.7.503 摘要:Fleischer AC, Wheeler JE, Yeh IT, Kravitz B, Jensen C, MacDonald B. Sonographic assessment of the endometrium in osteopenic postmenopausal women treated with idoxifene. J Ultrasound Med. 1999 Jul;18(7):503–12. doi: 10.7863/jum.1999.18.7.503. 参考文献:10.2165/00002512-199914050-00001 摘要:Haynes B, Dowsett M. Clinical pharmacology of selective estrogen receptor modulators. Drugs Aging. 1999 May;14(5):323–36. doi: 10.2165/00002512-199914050-00001. 参考文献:10.1007/bf02967993 摘要:Garin AM. Breast cancer in Russia. Breast Cancer. 2004;11(1):7–9. doi: 10.1007/bf02967993. 参考文献:10.1016/s0022-3565(24)35249-8 摘要:Badger AM, Blake SM, Dodds RA, Griswold DE, Swift BA, Rieman DJ, Stroup GB, Hoffman SJ, Gowen M. Idoxifene, a Novel Selective Estrogen Receptor Modulator, Is Effective in a Rat Model of Adjuvant-Induced Arthritis. The Journal of Pharmacology and Experimental Therapeutics. 1999 Dec;291(3):1380–6. doi: 10.1016/s0022-3565(24)35249-8. 参考文献:10.2165/00126839-199901030-00002 摘要:Peters DC, Coleman SG. Osteoporosis. Summary and table. Drugs R D. 1999 Mar;1(3):203–9. doi: 10.2165/00126839-199901030-00002.