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-2023212507-A1 优先权日:2020-06-12 标 题:Method for the synthesis of an edible and sterilizable porous 3d scaffold useful for cultured meat large-scale production 发明人:VILA MERCEDES; CORTIZO DIEGO 权利人:BIOTECH FOODS S L 摘要:The present invention relates to a method for the large-scale synthesis of an edible and hot steam sterilizable macroporous three-dimensional (3D) scaffold which comprises biocompatible polymers with interconnected pores as a support material for adherent cell growth, proliferation and differentiation, which may be used to obtain tissue with nutritive content and/or cultured meat. These scaffolds are suitable for supporting cell tissue growth for biomedical or food applications.
专利号:US-11155562-B2 优先权日:2014-06-30 标 题 :Synthesis of halichondrin analogs and uses thereof 发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE 权利人:HARVARD COLLEGE 摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-2014378538-A1 优先权日:2011-12-14 标 题:Methods of responding to a biothreat 发明人:BANCEL STEPHANE 权利人:MODERMA THERAPEUTICS INC 摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.
专利号:US-2023111600-A1 优先权日:2019-12-17 标题 :Polymeric fatty acid compounds for the treatment of fibrous amino acid-based substrates, especially hair 发明人:WAGNER ROLAND; STREICHER KATHARINA; ROHMANN LAURA; WENSKE CHRISTIAN; HAVELI SHRUTISAGAR DATTATRAYA 权利人:MOMENTIVE PERFORMANCE MAT GMBH 摘要:The present invention is directed at mono-, di- or polyquaternary ammonium compounds of the formula (I) wherein x is 1 to 50, and F can be the same or different and is represented by the general formula (II) wherein at least one of the optionally substituted and optionally functional-group-containing hydrocarbon radicals R 1 , R 2 , R 3 , R 4 or R 5 contains at least one estolide moiety comprising two or more ester or amide moieties. The invention also relates to a process for the synthesis of such compounds, the use of the compounds in cosmetic formulations for skin and hair care, cosmetic compositions for the treatment of fibers, and compositions containing one or more of the compounds for the treatment of hair.
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