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-9278919-B1 优先权日:2015-03-13 标题:Synthesis of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide 发明人:XU YONG 权利人:XU YONG 摘要:A method for preparing BTK inhibitor CC-292 of formula 1, comprising: (1) contacting a compound of formula 2 with a compound of formula 3 to obtain a compound of formula 4; (2) contacting the compound of formula 4 with a compound of formula 5 to obtain a compound of formula 6; (3) contacting the compound of formula 6 with trifluoromethanesulfonic anhydride to obtain a compound of formula 7; and (4) contacting the compound of formula 7 with a compound of formula 8 to obtain the compound of formula 1,
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:CN-118922420-A 优先权日:2022-03-25 标题 :Synthesis of TYK2 inhibitors and their intermediates
参考文献:10.1007/s00894-020-04512-3 摘要:Pery N, Rizvi NB, Shafiq MI. Development of piperidinyl dipyrrrolopyridine-based dual inhibitors of Janus kinase and Bruton’s tyrosine kinase: a potential therapeutic probability to deal with rheumatoid arthritis. Journal of Molecular Modeling. 2020 Aug 17;26(9):235. doi: 10.1007/s00894-020-04512-3. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749