专利号:US-10844081-B2 优先权日:2015-08-07 标题 :Protected organoboronic acids with tunable reactivity, and methods of use thereof 发明人:BURKE MARTIN D; SCHMIDT MICHAEL; MOREHOUSE GREG; PIPAL ROBERT W 权利人:UNIV ILLINOIS 摘要:Disclosed are a range of protected organoboronic acid reagents useful in the modular assembly of complex organic compounds. The reactivities of the protected organoboronic acid reagents may be varied predictably by changes to the number and identities of their substituents. Also disclosed are methods of using the protected organoboronic acid reagents in the synthesis of organic compounds.
专利号:US-5922906-A 优先权日:1997-09-05 标 题:Side chains synthesis for an anthiarrhythmic compound 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC 摘要:The present invention is directed to an improved process for preparing the phenylacetic acid side chain of the compound of the formula This compound exhibits utility as a Class III antiarrhythmic agent.
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
专利号:US-12227528-B2 优先权日:2017-11-09 标 题:Glucose-sensitive albumin-binding derivatives 发明人:KRUSE THOMAS; KOFOD-HANSEN MIKAEL; MUENZEL MARTIN WERNER BORCHSENIUS; THOEGERSEN HENNING; SAUERBERG PER; EWALD JAKOB; BEHRENS CARSTEN; HOEG-JENSEN THOMAS; BALSANEK VOJTECH; DROBNAKOVA ZUZANA; DROZ LADISLAV; HAVRANEK MIROSLAV; KOTEK VLADISLAV; STENGL MILAN; SNAJDR IVAN; DRUSANOVA HANA 权利人:NOVO NORDISK AS 摘要:This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.
专利号:WO-2007002173-A1 优先权日:2005-06-22 标 题:Hiv-1 protease inhibitors, and methods of making and using them 发明人:RANA TARIQ M; ALI AKBAR; CAO HONG; SAI KIRAN KUMAR REDDY GA; ANJUM SAIMA GHAFOOR 权利人:UNIV MASSACHUSETTS; RANA TARIQ M; ALI AKBAR; CAO HONG; SAI KIRAN KUMAR REDDY GA; ANJUM SAIMA GHAFOOR 摘要:One aspect of the invention relates to the design, synthesis and biological activity of novel HIV-1 protease inhibitors incorporating N-phenyloxazolidine-5-carboxamides into the (hydroxyethylamino)sulfonamide scaffold as P2 ligands. For example, the present invention relates to inhibitors with variations at the P2 phenyloxazolidine and the P2' phenylsulfonamide moieties. Remarkably, compounds with an (S)-enantiomer of substituted phenyloxazolidines at P2 show highly potent inhibitory activities against wild-type HIV-1 protease. In certain embodiments, the inhibitors of the invention have Ki values in low picomolar (pM) range. In certain embodiments, the inhibitors of the invention were shown to be active against a variety of multi-drug resistant (MDR) HIV-1 proteases, each representing different paradigm of drug resistance.
专利号:CN-1829673-A 优先权日:2001-12-14 标 题 :Synthesis of alpha, beta-trifluorostyrene by in situ formation of trifluorovinyl metal halide