📜3-氨基-2,6-哌啶二酮盐酸盐置于咪唑,10 Wt% Pd(Oh)2 On Carbon,氢气体系中,用 N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 48.0H,反应生成3-(5-氨基-2-甲基-4-氧喹唑啉-3(4H)-基)哌啶-2,6-二酮 参考文献: Bromodomain Targeting Degronimers For Target Protein Degradation[fr] Dégronimères Ciblant Un Bromodomaine Pour La Dégradation De Protéines Cibles 标题: Bromodomain Targeting Degronimers For Target Protein Degradation[fr] Dégronimères Ciblant Un Bromodomaine Pour La Dégradation De Protéines Cibles 摘要:这项发明提供了一种degronimer,它具有可与靶向配体连接的e3泛素连接酶靶向部位(degron),该靶向配体选择用于体内降解溴结构域蛋白以实现治疗效果,并提供了使用方法,组合物以及它们的制备方法.
专利信息
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-9303014-B2 优先权日:2013-05-01 标题:Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione 发明人:RUCHELMAN ALEXANDER L; COHEN BENJAMIN M; CHOUDHURY ANUSUYA; KREILEIN MATTHEW M; LEONG WILLIAM W; MAN HON-WAH 权利人:CELGENE CORP 摘要:Provided herein are processes for the preparation of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt thereof.
专利号:US-11623929-B2 优先权日:2018-06-04 标 题 :Spirocyclic compounds 发明人:NASVESCHUK CHRISTOPHER G; DEY FABIAN; GOERGLER ANNICK; NORCROSS ROGER; SCHMID PHILIPP 权利人:C4 THERAPEUTICS INC 摘要:The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
专利号:US-9067912-B2 优先权日:2013-05-01 标 题 :Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,8-dione
专利号:CA-2910971-A1 优先权日:2013-05-01 标题:Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl)piperidine-2,6-dione
专利号:US-2016009685-A1 优先权日:2013-05-01 标 题 :Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl)piperidine-2,6-dione
1: Tsang M, Cleveland J, Rubenstein JL. On point in primary CNS lymphoma. Hematol Oncol. 2020 Dec;38(5):640-647. doi: 10.1002/hon.2761. Epub 2020 Jul 3. 2: Renneville A, Gasser JA, Grinshpun DE, Jean Beltran PM, Udeshi ND, Matyskiela ME, Clayton T, McConkey M, Viswanathan K, Tepper A, Guirguis AA, Sellar RS, Cotteret S, Marzac C, Saada V, De Botton S, Kiladjian JJ, Cayuela JM, Rolfe M, Chamberlain PP, Carr SA, Ebert BL. Avadomide induces degradation of ZMYM2 fusion oncoproteins in hematologic malignancies. Blood Cancer Discov. 2021 May;2(3):250-265. doi: 10.1158/2643-3230.BCD-20-0105. Epub 2021 Mar 10. 3: Fuchs O. Targeting cereblon in hematologic malignancies. Blood Rev. 2023 Jan;57:100994. doi: 10.1016/j.blre.2022.100994. Epub 2022 Jul 31. 135(13):996-1007. doi: 10.1182/blood.2019002395. Erratum in: Blood. 2021 Apr 15;137(15):2126.
合成参考文献
参考文献:10.1038/s41589-019-0362-y 摘要:Chamberlain PP, Hamann LG. Development of targeted protein degradation therapeutics. Nat Chem Biol. 2019 Oct;15(10):937–44. doi: 10.1038/s41589-019-0362-y. 参考文献:10.1007/s15004-023-0050-7 参考文献:10.1007/978-3-662-67510-6_11 参考文献:10.1007/s11094-024-03236-5 摘要:Kurkin DV, Bakupin DA, Morkovin EI, Krysanov IS, Makarova EV, Tsaplina AP, Klabukova DL, Ivanova OV, Gorbunova YV, Dzhavakhyan MA, Zvereva VI, Kolosov YA, Aleshnikova KY. Thalidomide: History of Research and Perspectives for Its Medical Use (Review). Pharm Chem J. 2024 Oct;58(7):1001–10. doi: 10.1007/s11094-024-03236-5. 参考文献:10.1007/978-981-97-7022-9_3 摘要:Vishwakarma K, Shrivastav M, Kausar A, Mishra S, Anitha K, Shrivastav A, Kesharwani S, Verma A. Novel Immunotherapeutic Approaches for Cancer Therapy. 2024. In: Nanotechnology Based Strategies for Cancer Immunotherapy.