专利号:US-9242925-B2 优先权日:2011-08-29 标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction 发明人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE 权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE 摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.
专利号:US-11390590-B2 优先权日:2016-08-16 标 题 :Methods and processes for the preparation of KDM1A inhibitors 发明人:TAPPER AMY E; CELATKA CASSANDRA; ROMERO ARTHUR GLENN; MCCALL JOHN M; CHANCELLOR TONI; CHEN JIAN-XIE; CHEN XUEMEI; ZHAO HE; BIOLATTO BETINA; BROT ELISABETH C A; LI ZHIHUA; LIAO XIAOMING 权利人:IMAGO BIOSCIENCES INC 摘要:Provided in this disclosure are methods for the synthesis of substituted 2-arylcyclopropylamines and 2-heteroarylcyclopropylamines and related compounds. Also provided are methods for reduction of thioesters to aldehydes, and methods for reductive animation of cyclopropylamines.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-4588825-A 优先权日:1983-10-11 标 题 :Intermediates for the synthesis of 4-amino-4,5-dihydro-2-furancarboxylic acid 发明人:BURKHART JOSEPH P; HOLBERT GENE W 权利人:MERRELL DOW PHARMA 摘要:This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C 1-6 lower alkyl esters thereof. These compounds are γ-aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.
专利号:US-9840457-B2 优先权日:2013-03-15 标题 :Lysine isotopologues, compositions comprising the same and methods of synthesis 发明人:BRADLEY JOEL CHANDLER; WOOD WILLIAM WAKEFIELD; BARKALLAH SALIM; RYAN WILLIAM JAMES; TITMAS RICHARD CHARLES; SCHWINDEN MARK DONALD; KOZAK JANUSZ KONRAD; ELMASRI MARWAN; TORKELSON STEVEN MICHAEL 权利人:CAMBRIDGE ISOTOPE LABORATORIES INC 摘要:This invention relates to lysine isotopologues of Formulas I and 1-A, as described herein, and processes for synthesizing the same and derivatives and intermediates involved therein. In one aspect, described herein is a chemical compound comprising an isotopically labeled analog, i.e., an isotopologue of a standard or naturally occurring lysine. The lysine isotopologue is synthetically formed to have stable isotopes of elements incorporated at selected positions. As such, the lysine isotopologue has a molecular mass different from the mass of a standard or naturally occurring lysine.
专利号:US-4824974-A 优先权日:1983-10-11 标 题 :Synthesis for the preparation of 4-amino-4,5-dihydro-2-furancarboxylic acid 发明人:BURKHART JOSEPH P; HOLBERT GENE W 权利人:MERRELL DOW PHARMA 摘要:This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C 1-6 lower alkyl esters thereof. These compounds are γ-aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.