专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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-5194666-A 优先权日:1992-07-30 标 题 :Process for preparing esters of 3,5,6-trichlorosalicyclic acid 发明人:SEDLAK JOHN A; HIGGINS MARK A; ESSENFELD AMY P 权利人:AMERICAN CYANAMID CO 摘要:An improved process for the synthesis of esters of 3,5,6-trichlorosalicylic acid in quantitative yield comprises reacting the acid with an alcohol under distillation conditions in the presence of a titanium ester or chelate catalyst, whereby byproduct ether formation from the alcohol is suppressed. The process is especially applicable to a process by which salicylic acid is chlorinated first in concentrated sulfuric acid and then with iodine catalyst to make the trichlorosalicylic acid which is extracted and then reacted with an alcohol and a titanium catalyst to make the ester.
专利号:US-2015361124-A1 优先权日:2013-01-22 标 题:Method for the solid-phase based synthesis of phosphate-bridged nucleoside conjugates 发明人:SARAC IVO; MEIER CHRIS 权利人:UNIVERSITÄT HAMBURG; UNIV HAMBURG 摘要:A method for producing phosphate-bridged nucleoside conjugates, in particular poly- or oligonucleosides. In the method, an immobilized cyclosaligenyl derivative of a nucleoside, nucleotide, poly- or oligonucleotide, poly- or oligonucleoside, or an analog thereof, is synthesized, and the subsequent reaction with a nucleophile yields the desired phosphate-bridged nucleoside conjugate, which may subsequently be released from the solid phase.
专利号:US-7411031-B2 优先权日:2001-11-23 标 题 :Synthesis of polyanhydrides 发明人:UHRICH KATHRYN E; SCHMELTZER ROBERT C; ANASTASIOU THEODORE JAMES 权利人:UNIV RUTGERS 摘要:The present invention provides a method for forming compounds of Formulan nHO—C(â• O)R 1 —X—R 2 —X—R 1 —C(â• O)—O—Hn nwherein compound (I) can be polymerized to provide a polymer that contains therapeutically active compounds. In the compounds of the invention, each R 1 is group that will provide the therapeutically active compound upon hydrolysis of the polymer; each X is independently an ester linkage or an amide linkage; and R 2 is a linking group.
专利号:US-4621160-A 优先权日:1983-06-23 标题 :Process for the chlorination of aromatic derivatives 发明人:DESBOIS MICHEL; DISDIER CAMILLE 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the chlorination of aromatic derivatives. The aromatic derivative is reacted with chlorine gas in liquid hydrofluoric acid. The products obtained are useful as intermediates for the synthesis of compounds having a plant-protecting or pharmaceutical activity.
[参考文献]: C Malaveille, Et Al. Genotoxicity Of Ochratoxin A And Structurally Related Compounds In Escherichia Coli Strains: Studies On Their Mode Of Action. Iarc Sci Publ. 1991:(115):261-6. [参考文献]: Debarati Ray, Et Al. Effect Of Biological Confinement On The Photophysics And Dynamics Of A Proton-Transfer Phototautomer: An Exploration Of Excitation And Emission Wavelength-Dependent Photophysics Of The Protein-Bound Drug. Phys Chem Chem Phys. 2012 Sep 21;14(35):12182-92. [参考文献]: Esra Bayram, Et Al. In Vitro Inhibition Of Salicylic Acid Derivatives On Human Cytosolic Carbonic Anhydrase Isozymes I And Ii. Bioorg Med Chem. 2008 Oct 15;16(20):9101-5. [参考文献]: J J Espinosa-Aguirre, Et Al. Mutagenic Activity Of 2-Chloro-4-Nitroaniline And 5-Chlorosalicylic Acid In Salmonella Typhimurium: Two Possible Metabolites Of Niclosamide. Mutat Res. 1991 Nov;264(3):139-45. [参考文献]: Jihye Kim, Et Al. Structure-Activity Relationship Of Salicylic Acid Derivatives On Inhibition Of Tnf-α Dependent Nfκb Activity: Implication On Anti-Inflammatory Effect Of N-(5-Chlorosalicyloyl)Phenethylamine Against Experimental Colitis. Eur J Med Chem. 2012 Feb:48:36-44.
合成参考文献
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 572. 摘要:Gagnon, A.; Benoit, E.; Le Roch, A., Science of Synthesis Knowledge Updates, (2018) 4, 52. 摘要:González-Bello, C., Science of Synthesis Knowledge Updates, (2018) 1, 215. 摘要:Hitomi, Y.; Arakawa, K., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 297. 摘要:Li, D.-D.; Wang, G.-W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 355.