专利号:US-2010022767-A1 优先权日:2008-07-25 标题 :Development of a synthesis of syringolin a and b and derivatives thereof 发明人:KAISER MARKUS; CLERC JEROME 权利人:MAX PLANCK GESELLSCHAFT 摘要:The synthesis of syringolin A and B and derivatives thereof as well as to pharmaceutical compositions containing the syringolin A or B or derivatives thereof and the use of syringolin A and B and derivatives thereof for prophylaxis and treatment of cancer.
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-6432933-B1 优先权日:1997-07-07 标 题 :Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases 发明人:CARROLL CAROLYN DIIANNI; DOLLE III ROLAND ELLWOOD; SHIMSHOCK YVONNE CLASS; HERPIN TIMOTHEE FELIX 权利人:PHARMACOPEIA INC 摘要:Compounds of Formula I n are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or α-hydroxyamide group and Z is an acyl or α-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
专利号:US-7125986-B2 优先权日:1997-12-29 标题:Penicillanic acid derivative compounds and methods of making 发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA 权利人:UNIV SOUTHERN METHODIST 摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
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-4808749-A 优先权日:1980-10-01 标 题:Cyclopropane carboxylic esters and acids 发明人:MARTEL JACQUES; TESSIER JEAN; TECHE ANDRE 权利人:ROUSSEL UCLAF 摘要:Novel esters in all possible isomeric forms of the formula ##STR1## wherein R is selected from the group consisting of (a) optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl or cycloalkyl-alkyl of 3 to 8 carbon atoms optionally substituted with at least one member of the group consisting of halogen, --OH, --SH, --OR', --SR', --NO 2 , ##STR2## --CN, --SO 3 H, --PO 4 H 2 , ##STR3## --SO 2 AlK 2 , --SO 3 AlK 3 , aryl optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF 3 , --OCF 3 , --SCF 3 and ##STR4## R' is alkyl of 1 to 8 carbon atoms, R' and R'' are individually selected from the group consisting of hydrogen and alkyl of 1 to 8 carbon atoms, AlK 1 , AlK 2 and AlK 3 are individually alkyl of 1 to 18 carbon atoms, (b) aryl of 6 to 14 carbon atoms optionally substituted with at least one substitutent selected from the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --OCF 3 , --CF 3 and --SCF 3 and (c) heterocycle optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF 3 , --OCF 3 and --SCF 3 , B is selected from the group consisting of optionally unsaturated alkyl of 1 to 18 carbon atoms, optionally unsaturated cycloalkyl of 3 to 18 carbon atoms and the remainder of an alcohol used in synthesis of pyrethrinoid esters, X is halogen and the ethylenic double bond may have Z or E geometry having parasitic activity, especially insecticidal acaricidal and nematocidal activity.
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 25. 摘要:Yliniemelä-Sipari, S. M.; Piisola, A.; Pihko, P. M., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 59.