专利号:US-6515039-B1 优先权日:1998-08-28 标 题:Method for the parallel and combinatory synthesis of compounds bound to a continuous polymeric solid phase supporting material 发明人:ULBRICHT MATHIAS; VOLKMER-ENGERT RUDOLF; GERMEROTH LOTHAR; WENSCHUH HOLGER 权利人:POLY AN GMBH 摘要:The invention relates to a method for the parallel and combinatory synthesis of compounds bound to a continuous polymeric solid phase supporting material. According to the method, a continuous polymeric solid phase supporting material is prepared, the material comprising a matrix of a supporting polymeric material and graft copolymer chains covalently bound to the supporting matrix, the graft copolymer chains having reactive groups being able to react with organic compounds, thereby forming spatially defined reaction sites. The method then comprises the sequential spotting of synthesis building blocks or reagents at the various reaction sites on the continuous solid phase supporting material to yield a substrate library of compounds bound to the solid phase supporting material, whereby each reaction site on the continuous solid phase supporting material determines the composition of the synthesized compound, which is bound directly on the supporting matrix via the reactive groups of the graft polymer chain.
专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-5679773-A 优先权日:1995-01-17 标题 :Reagants and methods for immobilized polymer synthesis and display 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:Compounds and methods for solid phase synthesis of organic molecules including peptides, oligonucleotides, benzodiazepines, beta -turn mimetics, and prostaglandins. The present invention provides new reagents in the form of linking groups and resins and substrates having attached linking groups which are useful in solid phase synthesis of high density arrays of organic molecules. The invention also provides methods which increase yields of various organic synthesis strategies.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6245937-B1 优先权日:1996-11-29 标题 :Liquid phase parallel synthesis of chemical libraries 发明人:CHENG SOAN; SAUNDERS JOHN 权利人:DUPONT PHARMACEUTICALS RES LAB 摘要:This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.