专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-9776966-B2 优先权日:2011-03-03 标 题:Synthesis of 2-carboxamide cycloamino urea derivatives 发明人:ERB BERNHARD; GALLOU ISABELLE SYLVIE; KLEINBECK FLORIAN KARL 权利人:NOVARTIS AG 摘要:Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.
专利号:US-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
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:WO-2025019775-A1 优先权日:2023-07-19 标题 :Endoxifen compositions and methods of use thereof and synthesis thereof 发明人:QUAY STEVEN 权利人:ATOSSA THERAPEUTICS INC 摘要:Described herein are endoxifen compositions comprising novel compounds and methods of use thereof. Methods of synthesis for the compositions are described herein. The endoxifen compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The endoxifen compositions described herein may be useful in the treatment of a condition in a subject, such as cancer.
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.
1: Holzhauser S, Lukoseviciute M, Papachristofi C, Vasilopoulou C, Herold N, Wickström M, Kostopoulou ON, Dalianis T. Effects of PI3K and FGFR inhibitors alone and in combination, and with/without cytostatics in childhood neuroblastoma cell lines. Int J Oncol. 2021 Jan 5. doi: 10.3892/ijo.2021.5167. Epub ahead of print. 3: Zhao M, Scott S, Evans KW, Yuca E, Saridogan T, Zheng X, Wang H, Korkut A, Cruz Pico CX, Demirhan ME, Kirby B, Kopetz S, Diala I, Lalani AS, Piha-Paul S, Meric-Bernstam F. Combining neratinib with CDK4/6, mTOR and MEK inhibitors in models of HER2-positive cancer. Clin Cancer Res. 2021 Jan 7:clincanres.3017.2020. doi: 10.1158/1078-0432.CCR-20-3017. Epub ahead of print.
合成参考文献
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