专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:WO-2022170218-A1 优先权日:2021-02-05 标题:Intramolecular cyclization for general synthesis of bicyclic alkyl bioisostere boronates 发明人:QIN TIAN; YANG YANGYANG; TSIEN JET 权利人:UNIV TEXAS 摘要:Disclosed herein are methods of synthesizing compounds of the formula (I) wherein the variables are defined herein. Also provided are compounds produced using these methods. In some aspects, the methods provided herein may be used to install aryl bioisosteres.
专利号:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-3940393-A 优先权日:1974-06-21 标题 :Synthesis of 2,6-diaminopyrimidines 发明人:GREENSPAN GEORGE; REES RICHARD W; RUSSELL PETER B 权利人:AMERICAN HOME PROD 摘要:New, substituted, 2,6-diaminopyrimidines are disclosed. These compounds are useful as anti-malarial agents. The oxygenation of pyrimethamine by fungi is also disclosed.
专利号:US-2007135437-A1 优先权日:2005-03-04 标题:Modulation of neurodegenerative diseases 发明人:BENJAMIN DANIEL E; HENRIE ROBERT N II; ERRICO MONICA A; REX BRIAN T; BRACKEN JUSTIN D; SCOTT SEAN 权利人:ALSGEN INC 摘要:Methods and compositions are disclosed for selectively decreasing protein levels in a central nervous system, meningial, immune system, blood, or muscle cell by administrating a pharmacological agent. In particular, methods and compositions that interfere with SOD-1 protein synthesis or stability, and decrease cellular levels of the protein are disclosed.
专利号:WO-2021078995-A1 优先权日:2019-10-25 标 题 :Selective polypeptide synthesis stalling assay and compound 发明人:STROUS GERARDUS JACOBUS ANTONIUS MARIA; MOL JAN ADRIANUS; VAN DER VELDEN LIEKE MARIE; KLUMPERMAN JUDITH; MAAS PETRUS EMMANUEL MARIE; PIET DENNIS PATRICK; DE KLERK-SPRENKELS NANDA ELISABETH; TIJHUIS JOHANN HEINRICH; VIÉTOR HENDRIK ENGELBERTUS; MAURICE MADELON MARIA; VAN DER KRIFT FELIX 权利人:UMC UTRECHT HOLDING BV; UNIV UTRECHT HOLDING BV; BIMINI BIOTECH B V 摘要:The invention relates to compounds, in particular pyrimidine-2,4-diamines, analogues and salts thereof and pharmaceutical compositions comprising pyrimidine-2,4-diamines analogues and salts thereof for use in the treatment and prevention of a disease, in particular a growth hormone receptor-dependent condition. The invention also relates to methods of using these compounds and compositions to treat physiological disorders related to the amount or activity of growth hormone. In a particular embodiment, the invention relates to a compound according to formula 1 for use in the treatment or prevention of a disease in a subject.
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 419. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 60. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 124. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 399. 摘要:Castle, S. L., Science of Synthesis Knowledge Updates, (2011) 4, 349.