合成目标产物 Regorafenib 主要起始原料 4-(4-Amino-3-Fluorophenoxy)-N-Methylpicolinamide And Methyl Isobutyrylacetate And 4-Chloro-Alpha,Alpha,Alpha-Trifluoro-M-Toluidine
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-11649285-B2 优先权日:2016-08-03 标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy 发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN 权利人:BIO TECHNE CORP 摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-10370455-B2 优先权日:2014-12-05 标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists 发明人:MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL 权利人:IMMUNEXT INC 摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
专利号:US-2018140724-A1 优先权日:2015-05-27 标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer 发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A 权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA 摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.
1: Victorino APOS, Meton F, Mardegan L, Festa J, Piranda DN, Araujo KB. Trifluridine/tipiracil (FTD/TPI) and regorafenib in older patients with metastatic colorectal cancer. J Geriatr Oncol. 2023 May;14(4):101477. doi: 10.1016/j.jgo.2023.101477. Epub 2023 Mar 27. 14(9):e28665. doi: 10.7759/cureus.28665. 3: Blay JY, Duffaud F, George S, Maki RG, Penel N. Regorafenib for the Treatment of Sarcoma. Curr Treat Options Oncol. 2022 Nov;23(11):1477-1502. doi: 10.1007/s11864-022-00990-0. Epub 2022 Sep 30. 13:992611. doi: 10.3389/fimmu.2022.992611.
合成参考文献
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