专利号:US-9656927-B2 优先权日:2013-11-01 标题 :Process for the synthesis of carboxylic acid derivatives 发明人:KISHORE PRASAD PRAGATI; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES; COUNCIL SCIENT IND RES 摘要:The present invention discloses one-pot synthesis of various carboxylic acid derivatives using copper catalyst and sodium cyanide as the cyanide source for bringing in carbonylative coupling in a single step.
专利号:US-9018371-B2 优先权日:2007-03-07 标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient 发明人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH 权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO 摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
专利号:US-7968752-B2 优先权日:2003-06-16 标 题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-2001024798-A1 优先权日:1998-06-11 标题:Biomimetic combinatorial synthesis 发明人:SHAIR MATTHEW D; LINDSLEY CRAIG W; PELISH HENRY E; SHEEHAN SCOTT M; GOESS BRIAN C; LAYTON MARK E; CHAN LAWRENCE K; CHEN CHUO; WESTWOOD NICHOLAS J 摘要:The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can then be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo [n. 3.1 ] ring systems, medium ring systems, and fused ring systems. In addition to compounds, libraries and methods for their production, the present invention also provides pharmaceutical compositions and methods and kits for determining one or more biological activities of the library members.
专利号:US-4734495-A 优先权日:1985-07-17 标 题 :Process and intermediates for beta-lactam antibiotics 发明人:EVANS DAVID A; SJOGREN ERIC B 权利人:HARVARD COLLEGE 摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.
专利号:CN-1500769-A 优先权日:1996-12-19 标 题 :Process for the solid phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds