专利号:US-5756790-A 优先权日:1995-09-29 标题 :Optically active cobalt (II) complexes and method for the preparation of optically active alcohols 发明人:MUKAIYAMA TERUAKI; YOROZU KIYOTAKA; NAGATA TAKUSHI; YAMADA TORU; SUGI KIYOAKI 权利人:MITSUI PETROCHEMICAL IND 摘要:The invention provides a method for preparing an optically active alcohol comprising the step of reacting a ketone compound with a hydride reagent in the presence of an optically active metal compound. The resulting optically active alcohols are useful as intermediates for the synthesis of physiologically active compounds such as drugs and pesticides, functional materials such as liquid crystals, and raw materials for synthesis in fine chemistry. A novel optically active cobalt (II) complex useful as a catalyst is also provided.
专利号:US-6825185-B2 优先权日:2000-12-21 标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D 权利人:NITROMED INC 摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-10179929-B2 优先权日:2014-06-26 标 题 :Water-soluble activatable molecular probes, intermediates for the synthesis thereof and associated detection methods 发明人:HASSERODT JENS; PROST MAXIME 权利人:ECOLE NORMALE SUPERIEURE LYON; UNIV CLAUDE BERNARD LYON; CENTRE NAT RECH SCIENT 摘要:The invention provides probes with formula (I): n nin which:n X 1 â•?NH, O, or S; X 2 â•?O or S; SE is a labile group, which may be eliminated under the action of a stimulus that may in particular be the presence of an enzyme, a chemical compound, or a physicochemical characteristic of the medium in which the probe is located; A is an aromatic group that, following cleavage of the C(X 2 )—O bond in aqueous solution, leads to the liberation of a chromophore or a fluorophore, R represents a hydrogen atom or -(L)n-GP, in which n is equal to 0 or 1, L is a linker arm, and GP is a hydrosolubilizing group; as well as their physiologically acceptable salts, solvates, or hydrates. The invention also provides intermediates for the synthesis thereof and detection methods employing them.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:EP-4520765-A1 优先权日:2023-09-08 标题:Ionizable cationic lipids incorporating silicon 发明人:RÉPÃ?SI JÓZSEF; SZILVÃ?GYI GÃ?BOR 权利人:ALDEXCHEM KFT 摘要:The present invention belongs to the field of biomedicine and drug delivery as well as pest and vector controls.The invention relates to a novel ionizable cationic lipid family incorporating silicon, which belongs to the trademark LipexSilâ„¢ 2nd generation lipids, wherein the tail is connected to the headgroup with biodegradable silyl acetal linker. Lipids containing silyl acetal linker(s) are state-of-the-art and are effective as ionizable cationic lipids in the formulation of empty or loaded lipid nanoparticles (LNPs). The novel linkers according to the invention are designed by means of proprietary borane catalysts [WO 2022/129966]. The invention describes the synthesis of the lipids of formula (I), formation and characterization of nanoparticles and biological experiments demonstrating that the lipid nanoparticles prepared with these novel lipids can efficiently deliver their cargo (e.g. RNA, DNA, mRNA, siRNA, dsRNA, pDNA, circular DNA, small biologically active molecules) into the cells.
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合成参考文献
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