专利号:US-2007293456-A9 优先权日:2004-12-30 标题:Method for the synthesis of 3-substituted indolizine and benzoindolizine compounds 发明人:HAYFORD ANTHONY; KALOKO JOSEPH 权利人:HAYFORD ANTHONY; KALOKO JOSEPH 摘要:A method of making a compound of Formula I: n n ncomprises reacting a compound of Formula II n n nwith a compound such as R 1 OH or R 1 SH, to produce said compound of Formula I. Compounds of Formula I are useful, among other things, as dyes, spectral sensitizers, glycosidase inhibitors, and as antibacterial, antiviral, and anti-inflammatory agents.
专利号:US-11629150-B2 优先权日:2016-07-01 标题:Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines 发明人:SMITH ALEXANDER; WHITE HANNAH S; TAVARES FRANCIS XAVIER; KRASUTSKY SERGIY; CHEN JIAN-XIE; DORROW ROBERTA L; ZHONG HUA 权利人:G1 THERAPEUTICS INC 摘要:This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
专利号:WO-2004087679-A1 优先权日:2003-04-01 标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases 发明人:OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-9845282-B1 优先权日:2016-08-12 标题 :Palladium catalyzed synthesis of ester compounds 发明人:EL ALI BASSAM M; IBRAHIM MANSUR B; SULEIMAN RAMI K 权利人:UNIV KING FAHD PET & MINERALS 摘要:A catalytic process for synthesizing an ester compound, and a catalytic process for synthesizing an amide compound, wherein a solid-supported palladium catalyst is used to catalyze an alkoxycarbonylation reaction of an aryl halide to form the ester compound, or to catalyze an aminocarbonylation reaction of an aryl halide to form the amide compound. Various embodiments of each of the processes are also provided.
专利号:US-2009247732-A1 优先权日:2003-11-04 标 题 :Synthesis of glycopeptides with superior pharmacokinetic properties 发明人:DUFFIELD JONATHAN; MARBY KENNETH; O'HARE SEAN; HWANG CHAN-KOU; ICHIKAWA YOSHITAKA 权利人:OPTIMER PHARMACEUTICALS INC 摘要:The present invention relates to novel glycopeptides having improved pharmacokinetic properties, improved stability, methods of preparing said novel glycopeptides, and methods to use said novel glycopeptides.
参考文献:10.1371/journal.pone.0009006 摘要:Suits MD, Zhu Y, Taylor EJ, Walton J, Zechel DL, Gilbert HJ, Davies GJ. Structure and kinetic investigation of Streptococcus pyogenes family GH38 alpha-mannosidase. PLoS One. 2010 Feb 03;5(2):e9006.