CAS: 1639417-53-0; (S)-2-(1-((9H-Purin-6-yl)Amino)Propyl)-3-(3-Fluorophenyl)-4H-Chromen-4-One

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    📜(R,S)-2-(1-(9H-Purin-6-Ylamino)Propyl)-3-(3-Fluorophenyl)-4H-Chromen-4-One 以35的收率获得泰那利塞
    参考文献:Dual Selective Pi3 Delta And Gamma Kinase Inhibitors
    标题:Dual Selective Pi3 Delta And Gamma Kinase Inhibitors
    摘要:本发明涉及双重δ和γ Pi3K蛋白激酶调节剂,制备它们的方法,包含它们的制药组合物以及使用它们治疗,预防和/或改善pi3K激酶介导的疾病或障碍的方法.

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    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-12390420-B1
    优先权日:2024-10-22
    标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
    发明人:EGUCHI MASAKATSU
    权利人:BRYET US INC
    摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

    专利号:US-2022411407-A1
    优先权日:2019-11-15
    标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
    发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
    权利人:UNIV NORTH CAROLINA CHAPEL HILL
    摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

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    主要参考文献


    1: Iyer SP, Huen A, Ai WZ, Jagadeesh D, Lechowicz MJ, Okada C, Feldman TA, Ghione P, Alderuccio JP, Champion R, Kim SH, Mohrbacher A, Routhu KV, Barde P, Nair AM, Haverkos BM. Safety and efficacy of tenalisib in combination with romidepsin in patients with relapsed/refractory T-cell lymphoma: results from a phase I/II open-label multicenter study. Haematologica. 2024 Jan 1;109(1):209-219. doi: 10.3324/haematol.2022.281875.
    2: Nguyen CN, Iyer SP, Duvic M, Barde PJ, Nair A, Routhu KV, Huen AO. Complete Response to tenalisib and romidepsin with long-term maintenance using tenalisib monotherapy in a patient with relapsed and refractory sézary syndrome. Invest New Drugs. 2023 Apr;41(2):350-355. doi: 10.1007/s10637-022-01315-6. Epub 2023 Apr 1. 12(8):2293. doi: 10.3390/cancers12082293.
    4: Carlo-Stella C, Delarue R, Scarfo L, Barde PJ, Nair A, Locatelli SL, Morello L, Magagnoli M, Vakkalanka S, Viswanadha S, Ferreri AJM. A First-in-human Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor, in Patients With Relapsed/Refractory Hematologic Malignancies: Results From the European Study. Clin Lymphoma Myeloma Leuk. 2020 Feb;20(2):78-86. doi: 10.1016/j.clml.2019.10.013. Epub 2019 Oct 23. 19(3):197-209. doi: 10.1080/14712598.2019.1572746. Epub 2019 Jan 29. 25(3):1098-1112. doi: 10.1158/1078-0432.CCR-18-1133. Epub 2018 Oct 23.

    合成参考文献


    参考文献:10.3390/cancers12082293
    摘要:Huen A, Haverkos BM, Zain J, Radhakrishnan R, Lechowicz MJ, Devata S, Korman NJ, Pinter-Brown L, Oki Y, Barde PJ, Nair A, Routhu KV, Viswanadha S, Vakkalanka S, Iyer SP. Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma. Cancers (Basel). 2020 Aug 15;12(8).
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