专利号:US-6444820-B1 优先权日:1995-04-07 标题:Process for the manufacture of camptothecin derivatives 发明人:HENEGAR KEVIN E; SIH JOHN C 摘要:This invention discloses and claims novel intermediates and procedures for the synthesis of camptothecin derivatives, such as irinotecan, and other compounds related to the synthesis of CPT-11. Related procedures and compounds are also disclosed, such as a novel method of making mappicine.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-4118384-A 优先权日:1976-02-21 标题 :Process for preparation of azo dyestuffs by coupling in presence of aromatic sulphonic acid-formaldehyde reaction product 发明人:MOLLS HANS-HEINZ; SCHIWY WILLY; HORNLE REINHOLD; NEBELING REINHARD 权利人:BAYER AG 摘要:Dyestuff dispersions and dyestuff solutions free from salt or at least having a low salt content are obtained in that the diazotization is carried out with addition of free dispersing agent acid to which, after the synthesis, either no basic agents are added or basic agents are added only up to a pH value of 3. The disclosed process gives dyestuff compositions of low salt content and results in readily dispersible dyestuffs when water insoluble dyestuffs are prepared and stable solutions when water soluble dyestuffs are prepared. The process is widely applicable and chemical constitution of the dyestuffs is conventional.
专利号:FR-3044311-A1 优先权日:2015-11-30 标 题 :PROCESS FOR THE SYNTHESIS OF ENANTIOMERICALLY PURE N- (PYRIDIN-4-YL) -2-HYDROXY-ALKYLAMIDE DERIVATIVES
专利号:WO-9102040-A1 优先权日:1989-08-04 标 题:Cyclodextrin labels for nucleic acid and biochemical analysis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention provides a method of qualitative and quantitative nucleic acid sequence analysis using luminescent cyclodextrin (CD), labels for dideoxy-nucleotide chain terminators and oligonucleotide primers. The CD labels are nonradioactive and detected in a ''black'' background, avoiding problems of fluorescence and allowing more sensitivity. Through formation of inclusion complexes with various fluorophores, the CD labels provide the versatility of different colored labels, with potentially higher signal efficiency in aqueous solutions. The CD labels have similar structures and thereby provide simplicity of synthesis and use, with more uniform chemical/physical properties, even with different colored labels. The invention is intended for high volume nucleic sequencing employing photomultipliers or charge-coupled device cameras for detection. Through the combination of these features, this invention provides advantages of speed, sensitivity, simplicity and versatility previously unknown or suggested in the art of nucleic acid sequence analysis.