专利号:WO-2022170218-A1 优先权日:2021-02-05 标题:Intramolecular cyclization for general synthesis of bicyclic alkyl bioisostere boronates 发明人:QIN TIAN; YANG YANGYANG; TSIEN JET 权利人:UNIV TEXAS 摘要:Disclosed herein are methods of synthesizing compounds of the formula (I) wherein the variables are defined herein. Also provided are compounds produced using these methods. In some aspects, the methods provided herein may be used to install aryl bioisosteres.
专利号:WO-2024064745-A1 优先权日:2022-09-21 标 题:Synthesis of reldesemtiv 发明人:PETERSON MATTHEW W; LU QING; MORGAN BRADLEY P; ASHCRAFT LUKE W; ANDERSEN DENISE 权利人:CYTOKINETICS INC 摘要:Provided herein is a process for the preparation of reldesemtiv and salts thereof. Also provided herein are intermediates used in this process and their preparation.
专利号:WO-2024052739-A1 优先权日:2022-09-08 标 题 :Method for the synthesis of benzodioxepinone compounds and intermediates thereof 发明人:NANDAN DR SANTOSH RAGHU; KORI AMITKUMAR RAMBIHARI; SHARMA BASANTKUMAR RAJKUMAR; SATISH SOHAL; CHITRAL ROHAN KAILASH; S JAYASHREE PUTTUR 权利人:AMBERNATH ORGANICS PVT LTD 摘要:A method for the preparation of benzodioxepinone compounds of formula (I), and the intermediates thereof, wherein, R 1 is independently selected from the group consisting of hydrogen, halogen, C 1 -C 6 alkyl, C 2 - C 6 alkenyl and C 3 -C 6 cycloalkyl; n represents integer 0-3.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:CN-107739328-A 优先权日:2017-11-22 标 题 :The preparation method of the key intermediate 1 for the synthesis of baricitinib
专利号:US-7179794-B2 优先权日:1998-06-08 标题 :Multivalent macrolide antibiotics 发明人:GRIFFIN JOHN H; PACE JOHN L 权利人:THERAVANCE INC 摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
参考文献:10.1055/s-0029-1217355 摘要:Mykhailiuk P, Radchenko D, Bezdudny A, Komarov I. Trifluoromethyl-Substituted Analogues of 1-Aminocyclobutane-1-carboxylic Acid. Synlett. 2009 Jun 12;2009(11):1827–9. doi: 10.1055/s-0029-1217355. 参考文献:10.1055/s-0030-1259536 摘要:Cramer N, Seiser T. β-Carbon Elimination from Cyclobutanols: A Clean Access to Alkylrhodium Intermediates Bearing a Quaternary Stereogenic Center. Synlett. 2011 Feb 08;2011(04):449–60. doi: 10.1055/s-0030-1259536.