专利号:US-9353112-B2 优先权日:2012-03-07 标 题 :Synthesis of polycyclic alkaloids 发明人:GOFF DANE; PAYAN DONALD G; BRASELMANN SYLVIA 权利人:RIGEL PHARMACEUTICALS INC 摘要:Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
专利号:US-2023220381-A1 优先权日:2020-06-30 标 题 :Dna-encoded functionalized aptamers 发明人:SLEIMAN HANADI; LACROIX DE VIMEUR DE ROCHAME DONATIEN PHILIPPE MARIE; MCKEAGUE MAUREEN; HIRKA SERHII; SALIBA DANIEL; ANDERSON SHAUN IAN 权利人:THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIV 摘要:It is provided the synthesis of an aptamer-like encoded oligomer (ALEnOmer), method of producing same and method of preparing a library of ALEnOmes. More particularly, the method of preparing ALEnOmer comprises coupling at least one phosphoramidite monomer with an orthogonal protecting group, and the ALEnOmer produces comprises a DNA coding strand covalently attached to an oligomer through a branching unit, wherein the oligomer has a degree of polymerization at least 5 and is an aptamer.
专利号:WO-0053545-A1 优先权日:1999-03-10 标 题 :Process for the synthesis of dihydropyridones 发明人:BUNIN BARRY A; TUSHUP STEVEN P 权利人:AXYS PHARM INC; BUNIN BARRY A; TUSHUP STEVEN P 摘要:This invention relates to a process of synthesizing dihydropyridone compounds of Formula (I). The process of the present invention can also be used to synthesize a library of dihydropyridone compounds represented by Formula (I).
专利号:US-8703951-B2 优先权日:2011-07-15 标 题 :Synthesis of 4H-benzo[D]pyrrolo[1,2-A]thiazoles and indolizino[6,7-b]indole derivatives and their use as antitumor therapeutic agents 发明人:SU TSANN-LONG; CHOU TING-CHAO; LEE TE-CHANG 权利人:SU TSANN-LONG; CHOU TING-CHAO; LEE TE-CHANG; ACADEMIA SINICA 摘要:The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.
专利号:US-5780603-A 优先权日:1996-11-15 标题:Combinatorial synthesis of carbohydrate libraries 发明人:HINDSGAUL OLE 权利人:SYNSORB BIOTECH INC 摘要:Disclosed are methods for synthesizing very large collections of diverse thiosaccaride derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccaride derviatives.
专利号:US-5965719-A 优先权日:1996-11-15 标 题:Combinatorial synthesis of carbohydrate libraries 发明人:HINDSGAUL OLE 权利人:SUNSORB BIOTECH INC 摘要:Disclosed are methods for synthesizing very large collections of diverse thiosaccharide derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccharide derivatives.
参考文献:10.1371/journal.pone.0021774 摘要:Blaschitz A, Gauster M, Fuchs D, Lang I, Maschke P, Ulrich D, Karpf E, Takikawa O, Schimek MG, Dohr G, Sedlmayr P. Vascular Endothelial Expression of Indoleamine 2,3-Dioxygenase 1 Forms a Positive Gradient towards the Feto-Maternal Interface. PLoS ONE. 2011 Jul 06;6(7):e21774. doi: 10.1371/journal.pone.0021774. 参考文献:10.3797/scipharm.1011-13 摘要:Jenny M, Wondrak A, Zvetkova E, Tram NT, Phi PT, Schennach H, Culig Z, Ueberall F, Fuchs D. Crinum latifolium leave extracts suppress immune activation cascades in peripheral blood mononuclear cells and proliferation of prostate tumor cells. Sci Pharm. 2011 Apr;79(2):323–35.