专利号:US-8536318-B2 优先权日:2008-05-29 标题 :Chemical RNA synthesis method 发明人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS 权利人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 2 摘要:The invention relates to a method for the chemical synthesis of RNA, comprising the following steps: a) bonding to a solid support of a monomer having formula (II) in which—X 1 is a dimethoxytrityl group,—X 6 is H or an OAc group or OX 3 , in which X 3 is a group having formula (A), in which X is O or S, R′ is H or CH 3 and R is selected from a linear or branched alkyl group at C 1 to C 4 and a R 1 —O—R 2 group in which R 1 is an alkyl group at C 1 to C 2 and R 2 is a CH 3 group or CH 2 CH 2 —O—CH 3 or aryl; b) assembly with the monomer having formula (II) bound to the support thereof obtained in step (a) of at least one monomer having formula (III) in which X 1 , Bp, X 3 are as defined for formula (II) and X 5 is a hydrogen phosphonate monoester or phosphoramidite group, preferably a 2-cyanoethyl-N,N-diisopropylphosphoramidite group, which is used to obtain a protected single-strand RNA bound to a support.
专利号:US-9018371-B2 优先权日:2007-03-07 标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient 发明人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH 权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO 摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
专利号:US-4355184-A 优先权日:1980-05-02 标题:Synthesis of α, β-unsaturated-ketones 发明人:KAKU TSUTOMU; KATSUURA KIYOSHI; SAWAKI MIKIO 权利人:NIPPON SODA CO 摘要:alpha , beta -unsaturated-ketones are synthesized by reacting with an aldehyde and an alkali metal salt of acetoacetic acid in the presence of an aliphatic secondary amine in the mixture of heterogeneous solvents producing an oil layer and a water layer.
专利号:US-7776971-B2 优先权日:2003-05-06 标题:Processes for the synthesis of dentritic macromolecules from conventional monomers 发明人:PERCEC VIRGIL 权利人:UNIV PENNSYLVANIA 摘要:The inventive subject matter relates to novel synthetic processes which use a multifunctional compound (the “TERMINI compoundâ€?) having a masked or protected functional group, wherein the TERMINI compound is capable of quantitatively and irreversibly interrupting a living polymerization or a chain organic reaction. After deprotection or demasking of the functional group of the TERMINI compound, the same living polymerization or organic reaction resumes with 100% efficiency, or a different living polymerization or organic reaction resumes with 100% chemoselectivity, respectively. Once incorporated into a growing molecule, the TERMINI compound generates a branching point upon resumption of the polymerization or reaction.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6506286-B1 优先权日:1995-02-24 标题 :Reactant, compound and process for the perfluoroalkylation of a nucleophile, and the derivatives obtained 发明人:LANGLOIS BERNARD; ROQUES NICOLAS; WAKSELMAN CLAUDE; TORDEUX MARC; FORAT GERARD 权利人:RHODIA CHIMIE SA 摘要:A reagent comprising a compound of formula (I): R f —M(X)(Z) n —Y—R, wherein R is a hydrocarbon radical advantageously having at most 10 carbon atoms and being selected from alkyls and aryls; R f is a radical of formula II: R 1 —(CΞ 2 ) m —CF 2 —, where R 1 is a fluorine or chlorine atom or a carbon radical, m is 0 or a integer from 0-12, and each Ξ, which may be the same or different, is a chlorine or preferably fluorine atom, with the proviso that when m is 0, R 1 is electroattractive, preferably a fluorine atom; n is 0 or 1; M is a non-metal selected from carbon and chalcogens with an atomic number than oxygen; and each of X, Y and Z, which are the same or different, is a chalcogen; as well as a generator, for consecutive or simultaneous addition. The reagent is useful for organic synthesis.