专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-10065985-B2 优先权日:2015-02-03 标题 :Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT) 发明人:MURPHY JENNIFER MARIE; LAZARI MARK SAUL 权利人:UNIV CALIFORNIA 摘要:The automated synthesis of clinically relevant amounts of 16β- 18 F-fluoro-5α-dihydrotestosterone ( 18 F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 29±5%. The specific activity was 4.6 Ci/μmol (170 GBq/μmol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated 18 F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.
专利号:US-11427530-B2 优先权日:2018-02-09 标 题 :Synthesis of 4-chlorokynurenines and intermediates 发明人:LEVIN DANIEL; LEEMING PETER; EISENREICH EMERICH; LIU XUEJUN KARL 权利人:VISTAGEN THERAPEUTICS INC 摘要:The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
专利号:US-2011245503-A1 优先权日:2008-11-28 标题 :Enantioselective synthesis of asymmetric beta-carboline intermediates 发明人:SANTOS LEONARDO; ESPINOZA MORAGA MARLENE; SHANKARAJAH NAGULA 权利人:UNIV TALCA 摘要:Described herein is a new asymmetric synthesis of imines to obtain β-carboline derivatives useful as key intermediate compounds for the synthesis of phosphodiesterase inhibitors using a new process with palladium or ruthenium hydride and/or nickel boride to reduce chiral intermediates. The use of chloroformate chiral auxiliaries is further described for the reduction and asymmetric hydrogenation of imines to obtain β-carboline derivatives and intermediate compounds used in the preparation thereof.
专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
1: Matera MG, Ora J, Cavalli F, Rogliani P, Cazzola M. New Avenues for Phosphodiesterase Inhibitors in Asthma. J Exp Pharmacol. 2021 Mar 15;13:291-302. doi: 10.2147/JEP.S242961.
合成参考文献
参考文献:10.1128/jb.01571-09 摘要:Monds RD, Newell PD, Wagner JC, Schwartzman JA, Lu W, Rabinowitz JD, O'Toole GA. Di-adenosine tetraphosphate (Ap4A) metabolism impacts biofilm formation by Pseudomonas fluorescens via modulation of c-di-GMP-dependent pathways. J Bacteriol. 2010 Jun;192(12):3011–23. 参考文献:10.1089/adt.2009.0254 摘要:Staeben M, Kleman-Leyer KM, Kopp AL, Westermeyer TA, Lowery RG. Development and Validation of a Transcreener Assay for Detection of AMP- and GMP-Producing Enzymes. ASSAY and Drug Development Technologies. 2010 Jun;8(3):339–50. doi: 10.1089/adt.2009.0254. 参考文献:10.1007/s00360-005-0041-z 摘要:Yamada T, Matsuda K, Uchiyama M. Atrial natriuretic peptide and cGMP activate sodium transport through PKA-dependent pathway in the urinary bladder of the Japanese tree frog. Journal of Comparative Physiology B. 2005 Dec 01;176(3):203–12. doi: 10.1007/s00360-005-0041-z. 参考文献:10.1007/s00213-005-0232-z 摘要:Devan BD, Bowker JL, Duffy KB, Bharati IS, Jimenez M, Sierra-Mercado D, Nelson CM, Spangler EL, Ingram DK. Phosphodiesterase inhibition by sildenafil citrate attenuates a maze learning impairment in rats induced by nitric oxide synthase inhibition. Psychopharmacology (Berl). 2006 Jan;183(4):439–45. doi: 10.1007/s00213-005-0232-z. 参考文献:10.1113/jphysiol.2011.210831 摘要:Iadecola C, Kahles T, Gallo EF, Anrather J. Neurovascular protection by ischaemic tolerance: role of nitric oxide. The Journal of Physiology. 2011 Aug 30;589(17):4137–45. doi: 10.1113/jphysiol.2011.210831.