合成目标产物 Cabozantinib Malate 主要起始原料 L-Malic Acid And Cabozantinib
(文献来源)合成步骤主要原料 L-Malic Acid 和 Cabozantinib
6,7-Dimethoxy-4-(4-Nitro-Phenoxy)-Quinoline置于甲酸,Palladium 10% On Activated Carbon,Potassium Formate,Potassium Carbonate体系中,用 四氢呋喃,水,丁酮 用作溶剂,化学反应 17.33H,反应生成卡博替尼苹果酸盐 参考文献: A Dual Met-Vegf Modulator For Treating Osteolytic Bone Metastases[fr] Double Modulateur Met-Vegf Pour Traiter Des Métastases Osseuses Ostéolytiques 标题: A Dual Met-Vegf Modulator For Treating Osteolytic Bone Metastases[fr] Double Modulateur Met-Vegf Pour Traiter Des Métastases Osseuses Ostéolytiques 摘要:这项发明旨在使用met和vegf的双重抑制剂治疗癌症,特别是去势抵抗性前列腺癌和溶骨性骨转移.
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-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.
专利号:US-2023391824-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent 发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL 权利人:NARENDRAN ARUMUGAVADIVEL 摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
专利号:US-2024262829-A1 优先权日:2021-04-21 标 题:Peptide nucleic acids, synthesis, and uses thereof 发明人:ROTHMAN JEFFREY 权利人:ONCOGENUITY INC 摘要:The present disclosure provides peptide nucleic acids (PNAs) including cyclic structural moieties such as tetrahydrofuran, pyrrolidinium, pyrrolidine, or N-methyl pyrrolidine, which have surprisingly improved the water solubility and binding affinity of PNA oligomers to ribose-phosphate nucleic acid oligomers. Pharmaceutical compositions including the disclosed PNAs, synthetic methods thereof, and methods of use thereof are also disclosed.
专利号:CN-116490201-A 优先权日:2020-07-02 标题 :Inhibitors of YAP/TAZ-TEAD tumor proteins, their synthesis and use
1: Graham J, Vogel A, Cheng AL, Bjarnason GA, Neal JW. Cabozantinib after prior checkpoint inhibitor therapy in patients with solid tumors: A systematic literature review. Cancer Treat Rev. 2022 Nov;110:102453. doi: 10.1016/j.ctrv.2022.102453. Epub 2022 Aug 10. 14:17588359221108691. doi: 10.1177/17588359221108691. 3: Maroto P, Porta C, Capdevila J, Apolo AB, Viteri S, Rodriguez-Antona C, Martin L, Castellano D. Cabozantinib for the treatment of solid tumors: a systematic review. Ther Adv Med Oncol. 2022 Jul 13;14:17588359221107112. doi: 10.1177/17588359221107112.
合成参考文献
参考文献:10.1016/j.bmc.2023.117561 摘要:Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM. Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors. Bioorg Med Chem. 2024 Jan 15;98():117561. doi: 10.1016/j.bmc.2023.117561.