专利号:US-7169589-B2 优先权日:2000-07-28 标题 :Silicatein-mediated synthesis of amorphous silicates and siloxanes and use thereof 发明人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI 权利人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI 摘要:Silicatein is an enzyme of silicate-forming organisms used for the synthesis of their silicate scaffold. The present invention relates to the use of highly-expressed and highly active recombinant silicatein, silicatein isolated from natural sources after gene induction as well as silicatein-fusion proteins for the synthesis of amorphous silicon dioxide (silicic acids and silicates), siloxanes as well as modification of these compounds and their technical use.
专利号:US-9034624-B2 优先权日:2009-06-16 标 题 :Process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules, polymeric conjugates and relative uses thereof 发明人:D ESTE MATTEO; RENIER DAVIDE; PASUT GIANFRANCO; ROSATO ANTONIO 权利人:D ESTE MATTEO; RENIER DAVIDE; PASUT GIANFRANCO; ROSATO ANTONIO; FIDIA FARMACEUTICI 摘要:The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones. n An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.
专利号:US-6630602-B1 优先权日:1998-04-16 标题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I:wherein R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group; and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2S and 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-5443978-A 优先权日:1993-03-11 标 题 :Chrysanthemyl diphosphate synthase, corresponding genes and use in pyrethrin synthesis 发明人:ELLENBERGER SUZANNE R; PEISER GALEN D; BELL RUSSELL N; HUSSEY JR CHARLES E; SHATTUCK-EIDENS DONNA M; SWEDLUND BRADLEY D 权利人:AGRIDYNE TECH INC 摘要:This invention provides a purified chrysanthemyl diphosphate synthase (CDS), a method for the purification of CDS from Chrysanthemum cinerariaefolium, and an amino acid sequence of the isolated CDS. Also provided is a cDNA encoding the CDS, a nucleotide sequence of the CDS gene, and a derived amino acid sequence of the encoded CDS protein. The CDS gene is useful in the enzymatic production of the natural stereospecific configuration of chrysanthemyl derivatives which are useful for the synthesis of pyrethrins, pyrethroids, derivatives thereof, as well as other classes of metabolites.
专利号:US-8563261-B2 优先权日:2009-09-28 标 题:Method of diagnosing and treating interstitial cystitis 发明人:CHACKO SAMUEL K 权利人:CHACKO SAMUEL K; UNIV PENNSYLVANIA 摘要:A method for diagnosing, or differentially diagnosing, interstitial cystitis (IC) involves detecting or measuring increased expression of a biomarker Endothelin 1 (ET-1) in a biological sample from a mammalian subject, particularly in the urine or urothelial tissue. An increased level of expression of ET-1 above the level of expression in the same sample of a healthy mammalian subject is an indication of a diagnosis of IC. Such diagnosis may further involve identify other clinical symptoms of IC. Additionally the method may use additional biomarkers, such as Hb-EFG, EGF, APF, IL-8, IL-6, and cGMP. Assay methods and diagnostic reagents and kits for such diagnosis are provided. Methods and compositions for treating IC by reducing the action, production or synthesis of ET-1 in the urine or urothelium and/or inhibiting its binding to its ET A and/or ET B receptors are also provided.
专利号:US-6319695-B1 优先权日:1991-10-15 标 题:Production of fucosylated carbohydrates by enzymatic fucosylation synthesis of sugar nucleotides; and in situ regeneration of GDP-fucose 发明人:WONG CHI-HUEY; ICHIKAWA YOSHITAKA; SHEN GWO-JENN; LIU KUN-CHIN 权利人:SCRIPPS RES INSITUTE 摘要:This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.
1: Nakae K, Kojima F, Sawa R, Kubota Y, Igarashi M, Kinoshita N, Adachi H, Nishimura Y, Akamatsu Y. Antipain Y, a new antipain analog that inhibits neurotransmitter release from rat dorsal root ganglion neurons. J Antibiot (Tokyo). 2010 Jan;63(1):41-4. doi: 10.1038/ja.2009.109. Epub 2009 Nov 13. 3: Afzal V, Wiencke JK, Wolff S. Antipain-mediated suppression of X-ray-induced chromosomal aberrations in human lymphocytes. Carcinogenesis. 1989 Jul;10(7):1193-6. Review. Russian. 20: Suzuki K, Tsuji S, Ishiura S. Effect of Ca2+ on the inhibition of calcium-activated neutral protease by leupeptin, antipain and epoxysuccinate derivatives. FEBS Lett. 1981 Dec 21;136(1):119-22.
合成参考文献
参考文献:10.1073/pnas.2005463117 摘要:Abrams RPM, Yasgar A, Teramoto T, Lee MH, Dorjsuren D, Eastman RT, Malik N, Zakharov AV, Li W, Bachani M, Brimacombe K, Steiner JP, Hall MD, Balasubramanian A, Jadhav A, Padmanabhan R, Simeonov A, Nath A. Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. Proc Natl Acad Sci U S A. 2020 Dec 08;117(49):31365–75.