专利号:US-7041479-B2 优先权日:2000-09-06 标题 :Enhanced in vitro synthesis of active proteins containing disulfide bonds 发明人:SWARTZ JAMES ROBERT; KIM DONG-MYUNG 权利人:TRUSTESS OF THE LELAND STANFOR 摘要:Compositions and methods are provided for the enhanced in vitro synthesis of polypeptides containing disulfide bonds. In order to improve the performance of in vitro protein synthesis reactions, pre-treatment and redox buffering of the reaction mix is performed in order to optimize the redox potential. Exogenous enzymes that enhance protein folding and disulfide bond formation may also be added to the reaction.
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6136984-A 优先权日:1996-04-22 标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-4895922-A 优先权日:1988-05-05 标 题 :Low temperature synthesis of polyesteramides 发明人:OGATA NAOYA 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention disclosed a process for the synthesis of polyesteramides. By utilizing the phosphorus containing catalyst systems of the present invention, such polyesteramides can be synthesized at relatively low temperatures. The present invention specifically discloses a process for the synthesis of a polyesteramide which comprises polymerizing at least one diamine, at least one diol, and at least one dicarboxylic acid in the presence of (1) at least one acid acceptor; (2) at least one halogenated organic compound; and (3) at least one phosphorus containing compound selected from the group consisting of (a) triphenylphosphine, (b) triphenylphosphine oxide, (c) triphenylphosphine sulfide, (d) polymeric agents having pendant diphenylphosphine groups, (e) silicon-phosphorus compositions which contain at least one divalent oxygen atom which is bonded directly to a tetravalent silicon atom and a trivalent or pentavalent phosphorus atom; (f) compounds with the structural formula (C 6 H 5 ) 3 P=N-R, wherein R is a hydrogen atom or an alkyl group containing from 1 to 10 carbon atoms; and (g) compounds with the structural formula (C 6 H 5 )PR 1 R 2 wherein R 1 and R 2 can be the same or different, wherein R 1 is selected from the group consisting of alkyl groups containing from 1 to 10 carbon atoms and phenyl groups, and wherein R 2 is an alkyl group containing from 1 to 10 carbon atoms.
专利号:US-2012208232-A1 优先权日:2009-07-15 标 题:Cell-Free Synthesis of Active Reprogramming Transcription Factors 发明人:YANG WILLIAM; PATEL KEDAR; GHEBREMARIAM YOHANNES T; LEE JI EUN; WONG HANN-CHUNG; COOKE JOHN P; SWARTZ JAMES ROBERT 权利人:YANG WILLIAM; PATEL KEDAR; GHEBREMARIAM YOHANNES T; LEE JI EUN; WONG HANN-CHUNG; COOKE JOHN P; SWARTZ JAMES ROBERT 摘要:Compositions and methods are provided for the cell-free synthesis of active reprogramming factor polypeptides. The reprogramming factors may be synthesized as fusion proteins comprising a permeant domain, such as polyarginme. The cell free-synthesis may be conducted at about 25 C in a bacterial cell extract from genetically alterd cells having decreased endogenous protease activity Further, the proteins may comprise a fusion partner which enhances solubility and may be refolded on a column.
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