专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
专利号:US-9937151-B2 优先权日:2010-06-18 标题 :Carbapenem antibacterials with gram-negative activity 发明人:CHOI WOO-BAEG; GRUSZECKA-KOWALIK EWA; JOO HYUNG-YEUL; LIU SHUANGPEI; MAO SHULI; LI YONGFENG; KIM DEOG-IL 权利人:FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
专利号:US-2024109911-A1 优先权日:2017-10-04 标 题 :Synthesis of cantharidin
专利号:CN-111819182-A 优先权日:2017-10-04 标 题:Synthesis of cantharidin
专利号:CN-118084861-A 优先权日:2017-10-04 标 题 :Synthesis of cantharidin
1: Fu MC, Shang R, Cheng WM, Fu Y. Boron-Catalyzed N-Alkylation of Amines using Carboxylic Acids. Angew Chem Int Ed Engl. 2015 Jul 27;54(31):9042-6. doi: 10.1002/anie.201503879. Epub 2015 Jul 6. doi: 10.1007/s00403-015-1573-z. Epub 2015 May 26.
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