专利号:US-2009253913-A1 优先权日:2008-03-06 标题:Process for the preparation of sorafenib and salts thereof 发明人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 权利人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 摘要:Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.
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-11130764-B2 优先权日:2017-02-17 标题 :Analogs of vincamine and uses thereof 发明人:HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK 权利人:UNIV FLORIDA 摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.
专利号:WO-2014002108-A1 优先权日:2012-06-27 标 题:A core-shell nanostructure on the basis of proteins with corresponding therapeutic agents 发明人:MANZOOR KOYAKUTTY; ARCHANA RETNAKUMARI; SHANTIKUMAR V NAIR 权利人:AMRITA VISHWA VIDYAPEETHAM UNIVERSITY; MANZOOR KOYAKUTTY; ARCHANA RETNAKUMARI; SHANTIKUMAR V NAIR 摘要:The present invention is related to the design and synthesis of nanomedicine comprising of a protein-protein composite or core-shell nanoparticle, where one protein carries one type of therapeutic molecule and second protein carries another type of therapeutic molecule. This nanomedicine formulation is intended for the treatment of diseases including cancer. To be specific, the current invention is designed to deliver two different types of therapeutic molecules in sequence or in combination using a single entity of nanoparticle formed by two different proteins that carry two therapeutic molecules separately
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: Davies JM, Dhruva NS, Walko CM, Socinski MA, Bernard S, Hayes DN, Kim WY, Ivanova A, Keller K, Hilbun LR, Chiu M, Dees EC, Stinchcombe TE. A phase I trial of sorafenib combined with cisplatin/etoposide or carboplatin/pemetrexed in refractory solid tumor patients. Lung Cancer. 2010 Jun 24. [Epub ahead of print] [Epub ahead of print] [Epub ahead of print] Early alpha-fetoprotein response predicts treatment efficacy of antiangiogenic systemic therapy in patients with advanced hepatocellular carcinoma. Cancer. 2010 Jun 22. [Epub ahead of print] Sorafenib, a Multikinase Inhibitor, Enhances the Response of Melanoma to Regional Chemotherapy. Mol Cancer Ther. 2010 Jun 22. [Epub ahead of print]
合成参考文献
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