CAS: 202590-98-5; (S)-2-(4-(4-Chlorophenyl)-2,3,9-Trimethyl-6H-Thieno[3,2-F][1,2,4]Triazolo[4,3-A][1,4]Diazepin-6-yl)-N-(4-Hydroxyphenyl)Acetamide

该化合物是复杂的有机化合物,其特征是含有硫诺和三硝酸盐的多环结构.这种化合物具有一个气管中心的特点,它有助于其潜在的生物活动和药用特性.一个氯联苯组和一个氢苯基组的存在表明,它可能与生物目标发生重大互动,可能影响其溶解性和再活性.三甲基组和乙酰胺功能进一步加强了其结构多样性,有可能影响其在生物系统中的结合性和选择性.这种化合物经常被调查其治疗潜力,特别是在诸如医药化学等领域,其核心结构的改变可导致其潜在生物活动和药剂特性特性.从总体上看,这种功能性组的精密性发展.

结构式图片

上下游产品

(S)-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid pivaloyl chloride 4-amino-phenol (R)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetic acid

合成工艺路线路线简述

    📜(+)-Jq1羧酸,三甲基乙酰氯,对氨基苯酚置于三乙胺体系中,用 四氢呋喃,N-甲基乙酰胺 用作溶剂,化学反应生成(S)-4-(4-氯苯基)-N-(4-羟基苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-乙酰胺
    参考文献:Thienotriazolodiazepine Compounds And Their Pharmaceutical Use
    标题:Thienotriazolodiazepine Compounds And Their Pharmaceutical Use
    摘要:Thienotriazolodiazepine化合物的化学式(1)##str1##其中每个符号如规范中定义,其药用盐,以及其药用.本发明的化合物可用作预防和治疗细胞黏附参与的炎症性疾病和过敏疾病的药物.

    海关参考信息

    专利信息


    专利号:US-11427596-B2
    优先权日:2019-07-19
    标 题:Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications
    发明人:CHELVAM VENKATESH; DUDHE PREMANSH; KRISHNAN MENA ASHA; SONAWANE AVINASH
    权利人:INDIAN INSTITUTE OF TECH INDORE
    摘要:Embodiments herein provide fused-pyrido heterocycles such as azaindoles, carboline derivatives, furo[b]pyridines or furo[b]pyridine-isatin hybrids of Formula I.Embodiments also relate to a process for a synthesis of variety of complex pyrido-heterocycles The pyrido-heterocycles can be used for treating cancer (cervix, kidney, lung, breast and epidermal skin) and multi-drug resistant tuberculosis. These heterocycles can also be used as anti-biofilm agents against pathogenic strains, which will minimize the risk of secondary infections.

    专利号:US-2022118123-A1
    优先权日:2019-02-22
    标 题 :Combination of ar antagonists and targeted thorium conjugates
    发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
    权利人:BAYER AG; BAYER AS
    摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

    专利号:US-11319326-B2
    优先权日:2015-03-30
    标 题 :Tricyclic fused derivatives of 1-(cyclo)alkyl pyrtdin-2-one useful for the treatment of cancer
    发明人:VADIVELU SARAVANAN; RAJAGOPAL SRIDHARAN; CHINNAPATTU MURUGAN; GONDRALA PAVAN KUMAR; SIVANANDHAN DHANALAKSHMI; MULAKALA CHANDRIKA
    权利人:JUBILANT BIOSYS LTD
    摘要:The present disclosure described heterocyclic compounds of Formula I or, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivative thereof and pharmaceutical compositions containing them as the active ingredient. The present disclosure also describes the synthesis and characterization of aforementioned compounds to exhibit high anticancer activity. The compounds of the present disclosure are useful as medicaments and their use in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by one or more BET family of bromodomains.

    专利号:CN-112239468-B
    优先权日:2019-07-19
    标题 :Metal-free solvent-free synthesis of fused pyridine heterocycles and biomedical applications thereof

    专利号:US-12103929-B2
    优先权日:2018-06-25
    标题:Tricyclic compounds
    发明人:FANG HAIQUAN; CHEN MINGMING; YANG GUIQUN; DU YUELEI; WANG YANPING; WU TONG; LI QINGLONG; ZHANG LEI; HU SHAOJING
    权利人:JACOBIO PHARMACEUTICALS CO LTD
    摘要:Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

    专利号:US-11267820-B2
    优先权日:2015-09-09
    标 题 :Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors
    发明人:VADIVELU SARAVANAN; RAJAGOPAL SRIDHARAN; RAMAIAH MANJUNATHA M; GONDRALA PAVAN KUMAR; CHINNAPATTU MURUGAN; SIVANANDHAN DHANALAKSHMI; PARIKH PAYAL KIRAN; MULAKALA CHANDRIKA
    权利人:JUBILANT BIOSYS LTD
    摘要:The present disclosure describes heterocyclic compounds of Formula I or, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof and pharmaceutical compositions containing them as the active ingredient. The present disclosure also describes the synthesis and characterization of aforementioned compounds to exhibit high anticancer activity. The compounds of the present disclosure are useful as medicaments and their use in the manufacture of medicaments for treatment, prevention, or suppression of diseases, an conditions mediated b one or more BET family of bromodomains.

    供应商参考报价(招募中)

    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: Boi M, Todaro M, Vurchio V, Yang SN, Moon J, Kwee I, Rinaldi A, Pan H, Crescenzo R, Cheng M, Cerchietti L, Elemento O, Riveiro ME, Cvitkovic E, Bertoni F, Inghirami G; AIRC 5xMille Consortium ‘Genetics-Driven Targeted Management of Lymphoid Malignancies’.. Therapeutic efficacy of the bromodomain inhibitor OTX015/MK-8628 in ALK-positive anaplastic large cell lymphoma: an alternative modality to overcome resistant phenotypes. Oncotarget. 2016 Nov 29;7(48):79637-79653. doi: 10.18632/oncotarget.12876.
    4: Riveiro ME, Astorgues-Xerri L, Vazquez R, Frapolli R, Kwee I, Rinaldi A, Odore E, Rezai K, Bekradda M, Inghirami G, D'Incalci M, Noel K, Cvitkovic E, Raymond E, Bertoni F. OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations. Oncotarget. 2016 Dec 20;7(51):84675-84687. doi: 10.18632/oncotarget.13181. doi: 10.1002/ijc.30256. doi: 10.1016/S2352-3026(16)00021-1. doi: 10.1007/s40262-015-0327-6. doi: 10.1158/1078-0432.CCR-14-1561. doi: 10.1016/S2352-3026(15)00247-1. doi: 10.1002/ijc.30412. doi: 10.18632/oncotarget.10983.
    13: Lu P, Qu X, Shen Y, Jiang Z, Wang P, Zeng H, Ji H, Deng J, Yang X, Li X, Lu H, Zhu H. The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Sci Rep. 2016 Apr 12;6:24100. doi: 10.1038/srep24100.

    合成参考文献


    参考文献:10.1038/s41375-020-01011-5
    摘要:Adnan Awad S, Dufva O, Ianevski A, Ghimire B, Koski J, Maliniemi P, Thomson D, Schreiber A, Heckman CA, Koskenvesa P, Korhonen M, Porkka K, Branford S, Aittokallio T, Kankainen M, Mustjoki S. RUNX1 mutations in blast-phase chronic myeloid leukemia associate with distinct phenotypes, transcriptional profiles, and drug responses. Leukemia. 2020 Aug 11;35(4):1087–99. doi: 10.1038/s41375-020-01011-5.
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