专利号:US-2004014168-A1 优先权日:1998-06-11 标题:Reagents and methods for library synthesis and screening 发明人:SCHREIBER STUART L; BLACKWELL HELEN E; PEREZ FERNANDEZ LUCY; TALLARICO JOHN A 权利人:HUGHES HOWARD MED INST 摘要:The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 μm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. n The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
专利号:EP-0799313-A2 优先权日:1994-12-13 标 题 :Method and reagent for treatment of arthritic conditions, induction of graft tolerance and reversal of immune responses 发明人:BEIGELMAN LEONID; STINCHCOMB DANIEL T; JARVIS THALE; DRAPER KENNETH; PAVCO PAMELA; MCSWIGGEN JAMES; GUSTOFSON JOHN; USMAN NASSIM; WINCOTT FRANCINE; MATULIC-ADAMIC JASENKA; KARPEISKY ALEXANDER; THOMPSON JAMES D; MODAK ANIL; BURGIN ALEX 权利人:RIBOZYME PHARM INC 摘要:An enzymatic nucleic acid molecule which cleaves RNA associated with development or maintenance of an arthritic condition, induction of graft tolerance or reversal of an immune response. In particular, the ribozyme sequences are directed to an mRNA encoding B7-1, B7-2, B7-3, CD40 and/or stromelysin. Also provided are ribozymes where the uracil in positions 4 and/or 7 are substituted, as well as methods for the synthesis of 2'-alkylnucleotides, 2'-O-alkylthioalkyl, or 2'-alkylthioalkylnucleotides. The application further describes a method for diprotection of RNA with aqueous ethylamine, a method for synthesis of a basic ribonucleoside mimetics, and transcription units comprising an RNA polymerase II promoter, a U6 small nuclear promoter, or an adenovirus VA1 promoter system.
专利号:US-5468853-A 优先权日:1993-12-30 标题 :Synthesis of 5-radiohalo-2'-deoxyuridine 发明人:BARANOWSKA-KORTYLEWICZ JANINA 权利人:UNIV NEBRASKA 摘要:Method of synthesizing 5-radio-halogenated-2'-deoxyuridine from 5-trimethylstannyl-2'-deoxyuridine is described. The method consists of the steps of mixing 5-trimethylstannyl-2'-deoxyuridine with an aqueous solution consisting of a radiohalide and NaOH to form a first mixture, adding H 2 O 2 /CH 3 COOH to the first mixture to form a second mixture, sonicating the second mixture, evaporating the solvent from the second mixture to form a residue, reconstituting the residue, filtering the residue; and then purifying the filtered residue such that at least one of a radiohalogenated nucleoside and nucleotide is obtained. A kit consisting of the components required for the above synthesis is also described.
专利号:US-9605261-B2 优先权日:2008-09-06 标 题:RNA synthesis—phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end 发明人:SRIVASTAVA SURESH C; PANDEY DIVYA; BAJPAI SATYA P; SRIVASTAVA NAVEEN P 权利人:CHEMGENES CORP 摘要:The present invention relates to novel phosphoramidites, A-n-bz, C-n-bz, C-n-ac, G-n-ac and U are produced with an HPLC purity of greater than 98% and 31 P NMR purity greater than 99%. A novel process of reverse 5′→3′ directed synthesis of RNA oligomers has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.
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-7510852-B2 优先权日:2002-10-18 标题:Biosynthetic genes and host cells for the synthesis of polyketide antibiotics and method of use 发明人:ROYER MONIQUE; GABRIEL DEAN W; FRUTOS ROGER; ROTT PHILIPPE 权利人:CIRAD; UNIV FLORIDA 摘要:Three gene clusters that together encode albicidin biosynthesis, the complete gene DNA sequences, and the deduced protein sequences for the enzymes and methods for using the DNA sequences are disclosed and discussed as well as methods for plant protection and creating new antibiotics. The novel Albicidin family of antibiotics is disclosed and their structure deduced.
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合成参考文献
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