📜对三氟甲氧基苯胺置于三乙基硅烷,三甲基铝,三氟乙酸体系中,用 二氯甲烷,甲苯 作为反应溶剂,化学反应 58.0H,反应生成 3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺 参考文献:3-(Benzo[d][1,3]Dioxol-5-Ylamino)-N-(4-Fluorophenyl)Thiophene-2-Carboxamide Overcomes Cancer Chemoresistance Via Inhibition Of Angiogenesis And P-Glycoprotein Efflux Pump Activity 标题:3-(Benzo[d][1,3]Dioxol-5-Ylamino)-N-(4-Fluorophenyl)Thiophene-2-Carboxamide Overcomes Cancer Chemoresistance Via Inhibition Of Angiogenesis And P-Glycoprotein Efflux Pump Activity 摘要:噻吩-2-甲酰胺显示出对血管反应生成和p-Gp外流泵的双重抑制作用. DOI:10.1039/c5Ob00233H
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
专利号:US-2024400576-A1 优先权日:2021-09-03 标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof 发明人:RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM 权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV 摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.
专利号:US-2025250280-A1 优先权日:2021-09-03 标 题 :Nitrogen-containing derivatives of narasin, synthesis and uses thereof 发明人:RODRIGUEZ RAPHAËL; CAÑEQUE TATIANA; MÜLLER SEBASTIAN; ANTOSZCZAK MICHAL 权利人:CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; INST CURIE 摘要:The present invention relates to nitrogen-containing derivatives of narasin having the formula (I), as well as synthesis and uses thereof, in particular for the treatment and/or prevention of cancer. Also disclosed are medicaments including the nitrogen-containing derivatives of narasin, which include medicaments for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
1. Dihel, Larry; Kittleson, Christine; Mulvihill, Kristen; Johnson, William W. Oxidative metabolism of the trifluoromethoxy moiety of OSI-930. Drug Metabolism and Drug Interactions (2009), 24(2-4), 95-121. CODEN: DMDIEQ ISSN:0792-5077. AN 2010:437994 2. Gruber, Harry E.; Jolly, Douglas; Perez, Omar. Recombinant replication-competent retroviral vectors expressing therapeutic products for treatment of proliferative disorders. PCT Int. Appl. (2010), 194pp. CODEN: PIXXD2 WO 2010036986 A2 20100401 CAN 152:423197 AN 2010:402977 3. Patel, Jay; Korlipara, Vijaya L. Design, synthesis, and evaluation of OSI-930 analogs as dual c-Kit and KDR (VEGFR-2) tyrosine kinase inhibitors. Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), MEDI-144. CODEN: 69LVCL AN
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749