CAS: 1009298-09-2; (5-(2,4-Bis((S)-3-Methylmorpholino)Pyrido[2,3-D]Pyrimidin-7-yl)-2-Methoxyphenyl)Methanol

该化合物是一种复杂的有机化合物,其特点是多环结构,包括一个基核和一种代氧代苯基.该化合物的特征是模光型组,有助于其潜在的生物活动,特别是在药用化学领域.多种功能组的存在表明,它可能表现出多种化学再活性和溶性.其立体化学特性和溶性(3S)配置表明,它意味着具体的空间安排可能影响它与生物目标的相互作用.该化合物的潜在用途可能包括作为制药剂的作用,因为其结构特征往往与生物活性分子有关.然而,有必要对其药用化学学,毒性和功效进行详细研究,以便充分了解其在治疗环境中的特点和潜在用途.

结构式图片

欧盟法规

C&L通报

上下游产品

(3S)-4-[7-chloro-2-[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d] pyrimidin-4-yl] 3-methyl-morpholine [2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methanol methyl 5-{2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl}-2-methoxybenzoate 5-{2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl}-2-methoxybenzyl pivalate

合成工艺路线路线简述

    2-氨基-6-氯烟酸置于四(三苯基膦)钯,氯化亚砜,氨,N,N-二异丙基乙胺,三氯氧磷体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基乙酰胺,甲苯 用作溶剂,化学反应生成[5-[2,4-二((3S)-3-甲基吗啉-4-基)吡啶并[2,3-D]嘧啶-7-基]-2-甲氧基苯基]甲醇
    参考文献:Optimization Of Potent And Selective Dual Mtorc1 And Mtorc2 Inhibitors: The Discovery Of Azd8055 And Azd2014
    标题:Optimization Of Potent And Selective Dual Mtorc1 And Mtorc2 Inhibitors: The Discovery Of Azd8055 And Azd2014
    摘要:The Optimization Of A Potent And Highly Selective Series Of Dual Mtorc1 And Mtorc2 Inhibitors Is Described. An Initial Focus On Improving Cellular Potency Whilst Maintaining Or Improving Other Key Parameters,Such As Aqueous Solubility And Margins Over Herg Ic50,Led To The Discovery Of The Clinical Candidate Azd8055 (14). Further Optimization,Particularly Aimed At Reducing The Rate Of Metabolism In Human Hepatocyte Incubations,Resulted In The Discovery Of The Clinical Candidate Azd2014 (21). (C) 2013 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2013.01.019

    海关参考信息

    专利信息


    专利号:US-2023295162-A1
    优先权日:2020-08-06
    标 题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity
    发明人:CSÃ?MPAI ANTAL; BÃ?RÃ?NY PÉTER; CZUCZI TAMÃ?S; Kovács Imre; ADAMIS BÃ?LINT; NÉMETH ZSÓFIA; MURÃ?NYI JÓZSEF; OLÃ?HNÉ SZABÓ RITA; BOSZE SZILVIA; MEZO GÃ?BOR; KOHIDAI LÃ?SZLÓ; LAJKÓ ESZTER; TAKÃ?CS ANGÉLA; Láng Orsolya; MEZO DIÃ?NA
    权利人:EOETVOES LORAND TUDOMANYEGYETEM; SEMMELWEIS EGYETEM
    摘要:The present invention relates to compounds of formula (I) (I) or pharmaceutically acceptable salts, and stereoisomers thereof, including enantiomers, racemic mixtures, mixtures of enantiomers, or combinations thereof, which are applicable for use in treating cancer diseases. The present invention further relates to a pharmaceutical composition comprising the above compounds.

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    专利号:US-12180228-B2
    优先权日:2019-06-05
    标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
    发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

    专利号:EP-4192467-A1
    优先权日:2020-08-06
    标题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity

    专利号:US-2022047711-A1
    优先权日:2018-12-10
    标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
    发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA
    权利人:GENENTECH INC
    摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.

    专利号:CN-116437925-A
    优先权日:2020-08-06
    标题 :Synthesis of novel elmidone derivatives and evaluation of anticancer activity thereof
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    成立日期:2023-3-17登记机关:武汉市江夏区市场监督管理局
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    平台资质认证✓营业执照✓
    CAS号:1009298-09-2
    中文名:AZD8055
    英文名:AZD-8055
    纯度:99% HPLC1G/5G/1KG
    产品图片备注:现货
    主打产品,生产工厂、精细化学品、医药中间体、材料中间体
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Holt SV, Logie A, Davies BR, Alferez D, Runswick S, Fenton S, Chresta CM, Gu Y, Zhang J, Wu YL, Wilkinson RW, Guichard S, Smith PD. Enhanced apoptosis and tumor growth suppression elicited by combination of MEK and mTOR kinase inhibitors. Cancer Res. 2012 Jan 23. [Epub ahead of print] Epub 2011 Sep 23.
    5: Shao H, Gao C, Tang H, Zhang H, Roberts LR, Hylander BL, Repasky EA, Ma WW, Qiu J, Adjei AA, Dy GK, Yu C. Dual targeting of mTORC1/C2 complexes enhances histone deacetylase inhibitor-mediated anti-tumor efficacy in primary HCC cancer in vitro and in vivo. J Hepatol. 2012 Jan;56(1):176-83. Epub 2011 Aug 9.
    7: Jiang Q, Weiss JM, Back T, Chan T, Ortaldo JR, Guichard S, Wiltrout RH. mTOR kinase inhibitor AZD8055 enhances the immunotherapeutic activity of an agonist CD40 antibody in cancer treatment. Cancer Res. 2011 Jun 15;71(12):4074-84. Epub 2011 May 3.

    合成参考文献


    参考文献:10.1158/0008-5472.can-09-1751
    摘要:Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res. 2010 Jan 01;70(1):288–98. doi: 10.1158/0008-5472.can-09-1751.
    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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