专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2024299311-A1 优先权日:2022-04-05 标题 :Ionizable cationic lipids and lipid nanoparticles 发明人:KARMALI PRIYA PRAKASH; TANIS STEVEN 权利人:KARMALI PRIYA PRAKASH; TANIS STEVEN; CAPSTAN THERAPEUTICS INC 摘要:Ionizable cationic lipids, methods for synthesizing them, as well as intermediates useful in synthesis of these lipids and methods of synthesizing the intermediates are disclosed. The ionizable cationic lipids are useful as a component of lipid nanoparticles (LNP), which in turn can be used for the delivery of nucleic acids into cells in vivo or ex vivo. LNP compositions are also disclosed, including LNP comprising a functionalized lipid to enable conjugation of a binding moiety, and targeted LNP (tLNP), that is a LNP in which a binding moiety has been conjugated to the functionalized lipid and can serve as a targeting moiety to direct the tLNP to a desired tissue or cell type.
专利号:US-2023250056-A1 优先权日:2020-06-24 标 题 :Process for synthesizing lipids 发明人:BEUTNER GREGORY LOUIS; LORA GONZALEZ FEDERICO; CHO PATRICIA Y; SMITH MICHAEL J 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present application provides processes for synthesizing lipids of Formula I useful in the synthesis of fat-soluble compounds for targeting and enhancing activity of therapeutic molecules, including siRNA.
专利号:US-2023265050-A1 优先权日:2020-06-24 标 题 :Process for synthesizing cationic lipids 发明人:BEUTNER GREGORY LOUIS; CARRASQUILLO-FLORES RONALD; LORA GONZALEZ FEDERICO; SMITH MICHAEL J 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present application provides processes for synthesizing cationic lipids of Formula I useful in the synthesis of fat-soluble compositions for targeting and enhancing activity of therapeutic molecules, including siRNA.
专利号:US-8043786-B2 优先权日:2003-03-05 标题 :Acid generators, sulfonic acids, sulfonyl halides, and radiation sensitive resin compositions 发明人:EBATA SATOSHI; WANG YONG; NISHIMURA ISAO 权利人:JSR CORP 摘要:The invention provides novel acid generators which are unproblematic in combustibility and accumulation inside the human body and can generate acids having high acidities and high boiling points and exhibiting properly short diffusion lengths in resist coating films and which permit the formation of resist patterns excellent smoothness with little dependence on the denseness of a mask pattern; sulfonic acids generated from the acid generators; sulfonyl halides useful as raw material in the synthesis of the acid generators; and radiation-sensitive resin compositions containing the acid generators. The acid generators have structures represented by the general formula (I), n nwherein R 1 is a monovalent substituent such as alkoxycarbonyl, alkylsulfonyl, or alkoxysulfonyl; R 2 to R 4 are each hydrogen or alkyl; k is an integer of 0 or above; and n is an integer of 0 to 5. Among the radiation-sensitive resin compositions, a positive one contains a resin having acid-dissociable groups in addition to the above acid generator, while a negative one contains an alkali-soluble resin and a crosslinking agent in addition to the acid generator.
专利号:WO-2025076113-A1 优先权日:2023-10-05 标题:Ionizable cationic lipids with conserved spacing and lipid nanoparticles 发明人:KARMALI PRIYA PRAKASH; TANIS STEVEN; BAO YANJIE 权利人:CAPSTAN THERAPEUTICS INC 摘要:Ionizable cationic lipids, methods for synthesizing the same, intermediates useful in synthesis of the ionizable cationic lipids, and methods of synthesizing the intermediates are disclosed. The ionizable cationic lipids are useful as a component of lipid nanoparticles (LNP), which in turn can be used for delivering nucleic acids into cells in vivo or ex vivo. LNP compositions are also disclosed, including LNP comprising a functionalized lipid to enable conjugation of a binding moiety, and targeted LNP (tLNP), that is a LNP in which a binding moiety has been conjugated to the functionalized lipid and can serve as a targeting moiety to direct the tLNP to a desired tissue or cell type.
1: Brown A, Patel S, Ward C, Lorenz A, Ortiz M, DuRoss A, Wieghardt F, Esch A, Otten EG, Heiser LM, Korolchuk VI, Sun C, Sarkar S, Sahay G. PEG-lipid micelles enable cholesterol efflux in Niemann-Pick Type C1 disease-based lysosomal storage disorder. Sci Rep. 2016 Aug 30;6:31750. doi: 10.1038/srep31750. 2: Saifer MG, Williams LD, Sobczyk MA, Michaels SJ, Sherman MR. Selectivity of binding of PEGs and PEG-like oligomers to anti-PEG antibodies induced by methoxyPEG-proteins. Mol Immunol. 2014 Feb;57(2):236-46. doi: 10.1016/j.molimm.2013.07.014. Epub 2013 Nov 5. doi: 10.1517/17425247.2012.720969. Epub 2012 Aug 30.
合成参考文献
摘要:Sasano, Y.; Iwabuchi, Y., Science of Synthesis: Special Topics, (2022) 1, 338.