CAS: 1000669-72-6; (4-(2-(1H-Indazol-3-yl)Vinyl)Phenyl)(Piperazin-1-yl)Methanone

该化合物是一种化学化合物,在医学化学领域,特别是其潜在的治疗用途方面引起注意,被归类为小分子,并被视为某些生物途径的选择性抑制剂,可能有助于其治疗特定疾病的效力;该化合物展示了一个独特的结构框架,使其能够与目标蛋白进行互动,影响其活动;其溶性,稳定性和生物利用率是决定其药用动力学特征的关键特征;此外,KW-2449进行了各种研究,以评估其安全和毒性,这对于评估其是否适合临床使用至关重要;随着研究的继续,该化合物的全部潜力和行动机制正在探索之中,使其成为药物发展和治疗创新的一个关注对象.

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    专利信息


    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-2024132278-A1
    优先权日:2022-12-20
    标题:Synthesis, pharmacology and use of new water-soluble and selective fms-like tyrosine kinase 3 (flt3) inhibitors
    发明人:MAHBOOBI SAVOSH; WIRTH LUKAS; PONGARTZ HERWIG; SELLMER ANDREAS
    权利人:UNIV REGENSBURG
    摘要:The present application relates to compounds of formula (I) for inhibiting FLT3. The present application further relates to a composition, preferably pharmaceutical composition, comprising a compound or a pharmaceutically acceptable salt thereof and comprising a pharmaceutically acceptable excipient and/or carrier. The present application also relates to a compound or composition for use in medicine. The present application also relates to a compound or composition for use in a method of preventing or treating cancer, preferably blood cancer, more preferably leukemia, even more preferably acute myeloid leukemia (AML). Furthermore, the present application relates to a method of preparing a compound.

    专利号:US-11384076-B2
    优先权日:2017-08-18
    标 题:Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors
    发明人:MAHBOOBI SIAVOSH; SELLMER ANDREAS; PONGRATZ HERWIG; PILSL BERNARDETTE; KRÄMER OLIVER; KINDLER THOMAS; BEYER MANDY
    权利人:UNIV REGENSBURG; UNIV DER JOHANNES GUTENBERG UNIV MAINZ
    摘要:The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.

    专利号:CN-108379591-B
    优先权日:2018-04-03
    标 题 :Synthesis of Immune Agonist Targeting Compounds and Their Applications

    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.

    专利号:EP-4389223-A1
    优先权日:2022-12-20
    标 题 :Synthesis, pharmacology and use of new water-soluble and selective fms-like tyrosine kinase 3 (flt3) inhibitors

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    主要参考文献

    1. Pratz, Keith W.; Sato, Takashi; Murphy, Kathleen M.; Stine, Adam; Rajkhowa, Trivikram; Levis, Mark. FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML. Blood (2010), 115(7), 1425-1432. CODEN: BLOOAW ISSN:0006-4971. AN
    2010:301893 2. Shiotsu, Yukimasa; Kiyoi, Hitoshi; Akinaga, Shiro; Naoe, Tomoki. Screening of molecular target therapy of cancer and generation of new kinase inhibitor, KW-2449. Saibo (2009), 41(9), 381-384. CODEN: SAIBC7 ISSN:1346-7557. AN
    2009:1319160 3. Verma, Dushyant; Kantarjian, Hagop M.; Jones, Dan; Luthra, Rajyalakshmi; Borthakur, Gautam; Verstovsek, Srdan; Rios, Mary Beth; Cortes, Jorge. Chronic myeloid leukemia (CML) with P190BCR-ABL: analysis of characteristics, outcomes, and prognostic significance. Blood (2009), 114(11), 2232-2235. CODEN: BLOOAW ISSN:0006-4971. CAN
    152:188988 AN

    合成参考文献


    参考文献:10.1182/blood-2009-09-242859
    摘要:Pratz KW, Sato T, Murphy KM, Stine A, Rajkhowa T, Levis M. FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML. Blood. 2010 Feb 18;115(7):1425–32.
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