专利号:US-2024024497-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-8519168-B2 优先权日:2007-07-03 标 题 :Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds 发明人:FU XIAOYONG; GUENTER FRANK BRUNO; KIM-MEADE AGNES S; MATTHEWS KENNETH STANLEY; MAUST MATHEW THOMAS; MCALLISTER TIMOTHY L; WERNE GERALD; WINTERS JASON L; YIN JIANGUO; ZHANG SHUYI 权利人:FU XIAOYONG; GUENTER FRANK BRUNO; KIM-MEADE AGNES S; MATTHEWS KENNETH STANLEY; MAUST MATHEW THOMAS; WERNE GERALD; WINTERS JASON L; YIN JIANGUO; ZHANG SHUYI; MOLOZNIK DAVID J; MERCK SHARP & DOHME 摘要:This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
专利号:US-7910775-B2 优先权日:2003-04-18 标题 :Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide 发明人:YIN JIANGUO; FU XIAOYONG; ZHANG SHUYI; MCALLISTER TIMOTHY L; KIM-MEADE AGNES S; WINTERS JASON L; SUDHAKAR ANANTHA; SCHUMACHER DORIS P 权利人:SCHERING CORP 摘要:Disclosed is a process for making the compound of formula I: n nusing the compounds of formulas II, Q, and XI or XII:n n nwherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C 1 -C 10 )alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:RU-2205834-C2 优先权日:1997-08-01 标题 :Method of synthesis of [2-((8,9)-dioxo-2,6-diazobi-cyclo-[5,2,0]non-1(7)-en-2-yl)ethyl]phosphonic acid, method of synthesis of n-[3-(tertiary butyloxy- carbonylamino)propyl]-2-aminoethylphosphonic acid di-c1-c6-alkyl ester, compounds
[参考文献]: E F Sherertz, Et Al. Percutaneous Penetration Of Squaric Acid And Its Esters In Hairless Mouse And Human Skin In Vitro. Arch Dermatol Res. 1988;280(1):57-60. [参考文献]: Frederik Wurm, Et Al. Squaric Acid Mediated Synthesis And Biological Activity Of A Library Of Linear And Hyperbranched Poly(Glycerol)-Protein Conjugates. Biomacromolecules. 2012 Apr 9;13(4):1161-71. [参考文献]: L F Tietze, Et Al. Conjugation Of P-Aminophenyl Glycosides With Squaric Acid Diester To A Carrier Protein And The Use Of Neoglycoprotein In The Histochemical Detection Of Lectins. Bioconjug Chem. 1991 May-Jun;2(3):148-53. [参考文献]: M G Wilkerson, Et Al. Squaric Acid And Esters: Analysis For Contaminants And Stability In Solvents. J Am Acad Dermatol. 1985 Aug;13(2 Pt 1):229-34. [参考文献]: O Blixt, Et Al. Enzymatic Glycosylation Of Reducing Oligosaccharides Linked To A Solid Phase Or A Lipid Via A Cleavable Squarate Linker. Carbohydr Res. 1999 Jun 30;319(1-4):80-91.
合成参考文献
摘要:Collier, S. J.; Singh, S. K., Science of Synthesis, (2010) 45, 91. 摘要:Collier, S. J.; Singh, S. K., Science of Synthesis, (2010) 45, 77. 摘要:Collier, S. J.; Singh, S. K., Science of Synthesis, (2010) 45, 83. 摘要:Takeda, T.; Tsubouchi, A., Science of Synthesis, (2009) 46, 69.