📜N-α-(Benzyloxycarbonyl)-L-γ-Glutamyl-3-[[2-[[bis[bis(2-Chloroethyl)Amino]Phosphinyl]Oxy]Ethyl]Sulfonyl]-L-Alanyl-2-Phenyl-(2R)-Glycine置于5%-Palladium/activated Carbon 氢气体系中,用 醋酸异丙酯,水 用作溶剂,30.0 °C,340.01 Kpa 条件下,反应 7.7H,反应生成(2R)-L-Gamma-谷氨酰-3-((2-((二(二(2-氯乙基)氨基)亚膦酰)氧基)乙基)磺酰基)-L-丙氨酰-2-苯基甘氨酸 参考文献:Process For And Intermediates In The Preparation Of Canfosfamide And Its Salts 标题:Process For And Intermediates In The Preparation Of Canfosfamide And Its Salts 摘要:一种制备坎福膦酰胺及其盐的过程和中间体.其中一些中间体具有抗癌活性.
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-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
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-2022143183-A1 优先权日:2019-02-23 标题:Photoswitchable protacs and synthesis and uses thereof 发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE 权利人:UNIV NEW YORK 摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.
专利号:KR-20160017105-A 优先权日:2008-01-15 标题:Synthesis of resorcylic acid lactones useful as therapeutic agents
专利号:KR-20110003468-A 优先权日:2008-01-15 标题:Synthesis of resorcylic acid lactones useful as therapeutic agents
1: Kavanagh JJ, Levenback CF, Ramirez PT, Wolf JL, Moore CL, Jones MR, Meng L, Brown GL, Bast RC Jr. Phase 2 study of canfosfamide in combination with pegylated liposomal doxorubicin in platinum and paclitaxel refractory or resistant epithelial ovarian cancer. J Hematol Oncol. 2010 Mar 11;3:9. 2: Sequist LV, Fidias PM, Temel JS, Kolevska T, Rabin MS, Boccia RV, Burris HA, Belt RJ, Huberman MS, Melnyk O, Mills GM, Englund CW, Caldwell DC, Keck JG, Meng L, Jones M, Brown GL, Edelman MJ, Lynch TJ. Phase 1-2a multicenter dose-ranging study of canfosfamide in combination with carboplatin and paclitaxel as first-line therapy for patients with advanced non-small cell lung cancer. J Thorac Oncol. 2009 Nov;4(11):1389-96. Phase 3 randomised study of canfosfamide (Telcyta, TLK286) versus pegylated liposomal doxorubicin or topotecan as third-line therapy in patients with platinum-refractory or -resistant ovarian cancer. Eur J Cancer. 2009 Sep;45(13):2324-32. Epub 2009 Jun 8. Review. Review. Review. Review. Review. Review. Review. 16: Rosen LS, Brown J, Laxa B, Boulos L, Reiswig L, Henner WD, Lum RT, Schow SR, Maack CA, Keck JG, Mascavage JC, Dombroski JA, Gomez RF, Brown GL. Phase I study of TLK286 (glutathione S-transferase P1-1 activated glutathione analogue) in advanced refractory solid malignancies. Clin Cancer Res. 2003 May;9(5):1628-38. Review.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749