专利号:US-9765027-B2 优先权日:2014-08-22 标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation 发明人:VARDANYAN RUBEN S; HRUBY VICTOR J 权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA 摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.
专利号:US-8728750-B2 优先权日:2006-09-06 标 题 :Process for preparation of optically active N-protected 3-aminopyrrolidine or optically active N-protected 3-aminopiperidine and the corresponding ketones by optical resolution of the racemic amine mixtures employing a bacterial omega-transaminase 发明人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS 权利人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS; LONZA AG 摘要:The present invention relates to the production of optically active amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.
专利号:US-2025163076-A1 优先权日:2022-02-18 标 题 :Synthesis of bruton's tyrosine kinase inhibitors 发明人:TRAN NGOC DUC; XIOURAS CHRISTOS; CLEATOR EDWARD; MATON WILLIAM MARC; RAMMELOO THOMAS JOACHIM LANDEWALD; FERNANDES PHILIPPE; BONGARTZ JEAN-PIERRE A; CAO DUY CHI TRUNG; HORWITZ MATTHEW ALLAN; JUSSEAU XAVIER JEAN-MARIE; LEMAIRE SÉBASTIEN FRANCOIS-EMMANUEL; SCHWEITZER-CHAPUT BERTRAND 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present disclosure is directed to methods of synthesizing a compound of Formula (I), where the R groups are defined herein, and to methods of synthesizing a compound of Formula (II). Some aspects of the present disclosure is directed to converting the compound of Formula (II) into its P form.
专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:US-9551018-B2 优先权日:2006-02-13 标 题 :Process for the preparation of optically active chiral amines 发明人:ROBINS KAREN; SCHEUER UWE; HOHNE MATTHIAS 权利人:LONZA AG 摘要:The present invention relates to the production of optically pure secondary amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.
摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 413. 摘要:DiRocco, D. A.; Schultz, D. M., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 621.