CAS: 170364-57-5; 3-(1-Methyl-1H-Indol-3-yl)-4-(1-(1-(Pyridin-2-Ylmethyl)Piperidin-4-yl)-1H-Indol-3-yl)-1H-Pyrrole-2,5-Dione

该化合物是合成的双丁二醇基麦基胺化合物,具有很强的选择性蛋白质C类(PKCβ)抑制剂的作用,它通过干扰细胞扩散,血管生成和血吸附等细胞细胞内信号路径,表现出抗突扰活动. Enzastaurin因其能够抑制肿瘤的生长和转移,在治疗各种恶性肿瘤方面的潜力受到调查,包括传播大型B细胞淋巴瘤(DLBCL)和血浆瘤(Glioblasma),因为它能够抑制肿瘤的生长和转移.它的口服生物利用率和有利的药用植物基因特征使它成为临床发展的候选体.该化合物的行动机制针对诱因途径的关键,为治疗患有受创伤的癌症提供了合理的治疗方法.

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号151490-40-3 甲基(1-甲基吲哚基)-3-乙醛酸酯 | CAS号616898-57-8 2-(1-(1-(pyridi... | CAS号150114-41-3 2-(1-甲基-1H-吲哚-3... | CAS号616898-64-7 2-氧代-2-(1-(1-(吡... | CAS号31106-82-8 2-(溴甲基)吡啶氢溴酸盐 | CAS号150760-45-5 2-(2,2-二甲氧基乙基)苯胺 | CAS号32989-69-8 1-[2-(2-nitroph... | CAS号79844-33-0 1-(2,2-二甲氧基乙基)-2-硝基苯 | CAS号359017-79-1 Unii-kx7K68Z2uh

合成工艺路线路线简述

    2-氨甲基吡啶置于盐酸,Lithium Hydroxide,Potassium Tert-Butylate,三乙酰氧基硼氢化钠,2,3-二氯-5,6-二氰基-1,4-苯醌体系中,用 四氢呋喃,乙醇,水,溶剂黄146,乙腈 用作溶剂,化学反应 7.5H,反应生成丁胺苯丙酮
    参考文献:Strategies For The Synthesis Of N-(Azacycloalkyl)Bisindolylmaleimides: Selective Inhibitors Of Pkcβ
    标题:Strategies For The Synthesis Of N-(Azacycloalkyl)Bisindolylmaleimides: Selective Inhibitors Of Pkcβ
    摘要:N-(Azacycloalkyl)Bisindolylmaleimides 1 Have Been Identified To Be Selective Inhibitors Of Pkcbeta. This Manuscript Will Describe The Synthetic Approaches Employed To Prepare This Class Of Compounds That Resulted In Development Of Efficient Methods For Preparation Of N-(Azacycloalkyl) Indole 5,Indole-3-Acetamide 8 And Indole-3-Glyoxylate Ester 4 Derivatives. (C) 2003 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/s0040-4020(03)00973-6

    海关参考信息

    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    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:US-9365532-B1
    优先权日:2011-02-14
    标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
    发明人:ISAACMAN STEVEN
    权利人:ISAACMAN STEVEN; NANOMETICS LLC
    摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.
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    主要参考文献


    1: Li ZY, Liang C, Ding M, Weng XQ, Sheng Y, Wu J, Lu H, Cai X. Enzastaurin enhances ATRA-induced differentiation of acute myeloid leukemia cells. Am J Transl Res. 2020 Dec 15;12(12):7836-7854.
    2: Nowakowski GS, Zhu J, Zhang Q, Brody J, Sun X, Maly J, Song Y, Rizvi S, Song Y, Lansigan F, Jing H, Cao J, Lue JK, Luo W, Zhang L, Li L, Han I, Sun J, Jivani M, Liu Y, Heineman T, Smith SD. ENGINE: a Phase III randomized placebo controlled study of enzastaurin/R-CHOP as frontline therapy in high-risk diffuse large B-cell lymphoma patients with the genomic biomarker DGM1. Future Oncol. 2020 May;16(15):991-999. doi: 10.2217/fon-2020-0176. Epub 2020 Apr 6. 59(1):87-103. doi: 10.1002/mc.23131. Epub 2019 Nov 6. 236(11):3243. doi: 10.1007/s00213-019-05312-1. Erratum for: Psychopharmacology (Berl). 2019 Nov;236(11):3231-3242. 9(5):906-926.
    6: Altshuler RD, Carpenter CA, Franke TJ, Gnegy ME, Jutkiewicz EM. The protein kinase Cβ-selective inhibitor, enzastaurin, attenuates amphetamine-stimulated locomotor activity and self-administration behaviors in rats. Psychopharmacology (Berl). 2019 Nov;236(11):3231-3242. doi: 10.1007/s00213-019-05278-0. Epub 2019 May 27. Erratum in: Psychopharmacology (Berl). 2019 Jul 3;:

    合成参考文献


    参考文献:10.1093/neuonc/nop070
    摘要:Butowski N, Chang SM, Lamborn KR, Polley MY, Parvataneni R, Hristova-Kazmierski M, Musib L, Nicol SJ, Thornton DE, Prados MD. Enzastaurin plus temozolomide with radiation therapy in glioblastoma multiforme: a phase I study. Neuro Oncol. 2010 Jun;12(6):608–13.
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