专利号:US-2024123076-A1 优先权日:2021-02-08 标题:Unsaturated dendrimers compositions, related formulations, and methods of use thereof 发明人:LEE SANG M; SIEGWART DANIEL J 权利人:UNIV TEXAS 摘要:Described herein are novel lipid compositions comprising unsaturated dendrimers and methods of synthesis of unsaturated dendrimers. The lipid composition can comprise an ionizable cationic lipid, a phospholipid, and a selective organ targeting lipid. Also described herein are pharmaceutical formulations comprising an unsaturated dendrimer, a lipid composition, and a therapeutic agent. Further described in here are methods of mRNA delivery comprising a lipid composition and a therapeutic agent. Further described herein are high-potency dosage forms of a therapeutic formulated with a lipid composition.
专利号:US-6051704-A 优先权日:1996-07-22 标题:Synthesis of macrocyclic tetraamido-N ligands 发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J 权利人:UNIV CARNEGIE MELLON 摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
专利号:WO-9815532-A1 优先权日:1996-10-09 标 题:Solid phase synthesis of heterocyclic compounds 发明人:MARZINZIK ANDREAS; FELDER EDUARD 权利人:CIBA GEIGY AG; MARZINZIK ANDREAS; FELDER EDUARD 摘要:Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
专利号:US-8551237-B2 优先权日:2007-12-10 标 题 :Synthesis of colorants in mixing apparatus 发明人:LOEBEL JOHANNES 权利人:LOEBEL JOHANNES; BASF SE 摘要:A process for preparing colorants of the general formula (Ia), (Ib) or (Ic) n nor mixtures thereof, comprises reactingn (a) tetracarboxylic acids or their functional derivatives with (b) at least one compound selected fromn i. aliphatic amines, ii. aromatic amines, iii. aliphatic diamines, iv. aromatic diamines, n (c) optionally in the presence of further additives, (d) optionally in the presence of wetting agentsn nin a mixing apparatus. These colorants are useful for coloration of macromolecular organic and inorganic materials of natural and synthetic origin.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-8334386-B2 优先权日:2007-07-03 标题:Aqueous synthesis of perylene pigments 发明人:LOEBEL JOHANNES; STOHR ANDREAS 权利人:LOEBEL JOHANNES; STOHR ANDREAS; BASF SE 摘要:A process for preparing perylene pigments of the general formula (Ia) or (Ib) n nor mixtures thereof, by reacting perylenetetracarboxylic acids or functional derivatives thereof with aromatic diamines, where R 1 , R 2 may be the same or different and may each independently be phenylene, naphthylene or pyridylene, where R 1 , R 2 may each be mono- or polysubstituted by C 1 -C 22 -alkyl, C 3 -C 22 -alkenyl, C 1 -C 22 -alkoxy, hydroxyl and/or halogen, X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 may be the same or different and may each independently be hydrogen or halogen, wherein the reaction is performed in the presence of a secondary or tertiary amine in an aqueous reaction medium.
1: Oh SJ, Shcherbakova N, Kostera-Pruszczyk A, Alsharabati M, Dimachkie M, Blanco JM, Brannagan T, Lavrnić D, Shieh P, Vial C, Meisel A, Komoly S, Schoser B, Sivakumar K, So Y; LEMS Study Group. Amifampridine phosphate (Firdapse®) is Effective and Safe in A Phase 3 Clinical Trial in LEMS. Muscle Nerve. 2016 Feb 6. doi: 10.1002/mus.25070. [Epub ahead of print] doi: 10.1007/s40120-015-0034-0. Epub 2015 Nov 2. 3: Haroldsen PE, Musson DG, Hanson B, Quartel A, O'Neill CA. Effects of Food Intake on the Relative Bioavailability of Amifampridine Phosphate Salt in Healthy Adults. Clin Ther. 2015 Jul 1;37(7):1555-63. doi: 10.1016/j.clinthera.2015.05.498. Epub 2015 Jun 20. doi: 10.1002/prp2.99. Epub 2014 Dec 9. 5: Dooms M, Pincé H, Simoens S. Do we need authorized orphan drugs when compounded medications are available? J Clin Pharm Ther. 2013 Feb;38(1):1-2. doi: 10.1111/jcpt.12006. Epub 2012 Sep 14. doi: 10.1097/WNF.0b013e31825a68c5. Review. doi: 10.2147/NDT.S10464. Epub 2011 May 30.
合成参考文献
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