CAS: 1372540-25-4; 2-Methyl-1-(2-Methyl-3-(Trifluoromethyl)Benzyl)-6-Morpholino-1H-Benzo[d]Imidazole-4-Carboxylic Acid

该化合物是GlaxoSmithKline开发的一种化学化合物,主要调查其在治疗各种疾病包括某些癌症方面的潜在治疗用途,被归类为小分子抑制剂,具体针对细胞信号路径中的某些运动细胞;该化合物的结构包括有助于其生物活动和选择性的特定功能组;已经研究过其调控控制细胞扩散和生存的关键路径的能力,使其成为定向治疗的候选对象;在临床前研究中,该化合物显示出抑制肿瘤生长和提高其他治疗效果的前景;与许多调查药物一样,该化合物的安全性,功效和药用植物特性通过严格的临床试验得到评估;该化合物的发展反映了制药业为创造更有效和有针对性的癌症疗法而正在作出的努力,尽管其临床状况和具体行动机制可能随研究进展而变化.

结构式图片

上下游产品

methyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate 5-chloro-2-nitrobenzoic acid 3-amino-5-chloro-2-nitrobenzoic acid methyl ester methyl 3-amino-5-(4-morpholinyl)-2-nitrobenzoate2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxamide 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid 2-amino-2-(hydroxymethyl)-1,3-propanediol salt ethyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate 22H21ClF3N3O2C22H21ClF3N3O2

合成工艺路线路线简述

    📜3-氨基-5-氯-2-硝基苯甲酸置于水,铁粉,Potassium Carbonate,三乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-),Lithium Hydroxide体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 17.0H,反应生成2-甲基-1-[[2-甲基-3-(三氟甲基)苯基]甲基]-6-(4-吗啉基)-1H-苯并咪唑-4-羧酸
    参考文献:Benzimidazole Derivatives As Pi3 Kinase Inhibitors
    标题:Benzimidazole Derivatives As Pi3 Kinase Inhibitors
    摘要:这项发明涉及苯并咪唑衍生物在调节磷脂酰肌醇3' Oh激酶家族(以下简称pi3激酶)的活性或功能,特别是抑制其活性或功能方面的用途.适当地,本发明涉及苯并咪唑在治疗以下一种或多种疾病状态中的用途:自身免疫性疾病,炎症性疾病,心血管疾病,神经退行性疾病,过敏,哮喘,胰腺炎,多器官功能衰竭,肾脏疾病,血小板聚集,癌症,精子活动力,移植排斥,移植物排斥和肺部损伤.更适当地,本发明涉及选择性作用于pi3Kβ的苯并咪唑化合物用于治疗癌症.

    海关参考信息

    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:US-2017107577-A1
    优先权日:2014-03-11
    标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
    发明人:AL-EJEH FARES
    权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
    摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

    专利号:US-11285169-B2
    优先权日:2013-03-13
    标题 :Methods for modulating chemotherapeutic cytotoxicity
    发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R
    权利人:US HEALTH
    摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

    专利号:US-2022400732-A1
    优先权日:2019-03-21
    标题:Anti-fructose therapy for colorectal and small intestine cancers
    发明人:GONCALVES MARCUS; CANTLEY LEWIS C; YUN JIHYE
    权利人:UNIV CORNELL
    摘要:As described herein ingestion of high amounts of sugar, especially fructose, can increase the growth of intestinal tumors. Such cancer growth can be inhibited or prevented by limiting the amounts of sugar and amino acids ingested, by inhibiting ketohexokinase (KHK), fructose transport (via GLUT5), fatty acid synthesis (via FASN), phosphoinositide 3-kinases (PI3K), or by limiting amounts of sugar and amino acids ingested while also receiving KHK inhibitors, GLUT5 inhibitors, FASN inhibitors, PI3K inhibitors, or a combination of such inhibitors.

    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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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Weigelt B, Warne PH, Lambros MB, Reis-Filho JS, Downward J. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44. doi: 10.1158/1078-0432.CCR-12-3815. Epub 2013 May 14.

    合成参考文献


    摘要:Li BY, Wu JH. [PI3K/p110β-specific inhibitors in castration-resistant prostate cancer]. Zhonghua Nan Ke Xue. 2017 Mar;23(3):195–9.
    参考文献:10.1158/1078-0432.ccr-21-1115
    摘要:Sarker D, Dawson NA, Aparicio AM, Dorff TB, Pantuck AJ, Vaishampayan UN, Henson L, Vasist L, Roy-Ghanta S, Gorczyca M, York W, Ganji G, Tolson J, de Bono JS. A Phase I, Open-Label, Dose-Finding Study of GSK2636771, a PI3Kβ Inhibitor, Administered with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer. Clin Cancer Res. 2021 Oct 01;27(19):5248–57. doi: 10.1158/1078-0432.ccr-21-1115.
    参考文献:10.1128/jb.164.3.1182-1187.1985
    摘要:Tsukagoshi N, Iritani S, Sasaki T, Takemura T, Ihara H, Idota Y, Yamagata H, Udaka S. Efficient synthesis and secretion of a thermophilic alpha-amylase by protein-producing Bacillus brevis 47 carrying the Bacillus stearothermophilus amylase gene. J Bacteriol. 1985 Dec;164(3):1182–7. doi: 10.1128/jb.164.3.1182-1187.1985.
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