📜(+)-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.
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.
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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.