CAS: 1260907-17-2; 2-((4S)-6-(4-Chlorophenyl)-8-Methoxy-1-Methyl-4H-Benzo[f][1,2,4]Triazolo[4,3-A][1,4]Diazepin-4-yl)-N-Ethylacetamide

上下游产品

(4-chlorphenyl)magnesium bromide [(4S)-6-(4-chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]acetic acid ethylamine 2-Amino-5-methoxybenzoic acid2-{(4S)-6-(4-chlorophenyl)-1-methyl-8-[4-(methyloxy)phenyl]-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl}-N-ethylacetamide 2-[(4S)-6-(4-chlorophenyl)-1-methyl-8-(1H-pyrazol-5-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide 2-[(4S)-6-(4-chlorophenyl)-1-methyl-8-(1H-pyrazol-4-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide 2-[(4S)-6-(4-chlorophenyl)-1-methyl-8-(2-methylphenyl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide

📜在 溶剂黄146体系中,用 2-甲基四氢呋喃,甲醇,水 用作溶剂,化学反应 40.0H,反应生成Gsk 525762A; (4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺
参考文献:氧化活化硫内酰胺制备甲基三唑并[1,4]苯二氮卓用于合成bet抑制剂molibresib
标题:氧化活化硫内酰胺制备甲基三唑并[1,4]苯二氮卓用于合成bet抑制剂molibresib
摘要:开发了一种硫内酰胺的新型氧化活化方法,用于一步制备甲基三唑并[1,4]苯二氮卓类药物.建议使用次磺酸 (R-Soh) 作为活化中间体,同时从乙酰肼生成乙酰腙,并环缩合生成三唑.作为合成 Bet 抑制剂 Molibresib (Gsk525762) 的新路线的一部分,该方法的一个版本使用 35% 过氧乙酸被放大至 40 Kg.硫内酰胺由市售的(2-氨基-5-甲氧基苯基)(4-氯苯基)甲酮分两步制备,产率为66%.简洁的四步合成提供了 52 Kg 的 Molibresib,其 Ee > 99.9%,酮的总产率为 41%.甲基三唑的条件温和且没有敏感立体中心的外消旋化.氧化法,
Doi:10.1021/acs.Joc.1C00563

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-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-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.