CAS: 183204-74-2; 5-Chloro-6-((2-Iminopyrrolidin-1-yl)Methyl)Pyrimidine-2,4(1H,3H)-Dione

📜6-甲基尿嘧啶置于吡啶,Selenium(Iv) Oxide,Sodium Tetrahydroborate,氯化亚砜,溶剂黄146,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 16.0H,反应生成5-氯-6-[(2-亚氨基-1-吡咯烷基)甲基]-2,4(1H,3H)-嘧啶二酮
参考文献:5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4 (1H,3H)-嘧啶二酮或其盐的制备方法
标题:5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4 (1H,3H)-嘧啶二酮或其盐的制备方法
摘要:本发明提供一种5‑氯‑6‑[(2‑亚氨基‑1‑吡咯烷)甲基]‑2,4(1H,3H)‑嘧啶二酮或其盐的制备方法,以6‑甲基嘧啶‑2,4(1H,3H)‑二酮为起始原料,通过6位甲基氧化,5位氢发生氯代,再还原6位醛基,与2‑氨基吡咯烷或相应的盐缩合后得到目标产物.本发明操作简单,工艺稳定,适合工业化生产,且产率高,纯度高,成本低.

专利信息

专利号:US-11028057-B2
优先权日:2018-02-28
标题:Process for the synthesis of 6-chloromethyluracil
发明人：MORANA FABIO; GOBBATO STEFANO; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:The invention relates to a process for the synthesis of 6-chloromethyluracil (6-(chloromethyl)pyrimidin-2,4(1H,3H)-dione) from ethyl 4-chloroacetoacetate and S-methylisothiourea hemisulfate via isolation of the novel intermediate 6-(chloromethyl)-6-hydroxy-2-(methylthio)-5,6-dihydropyrimidin-4(1H)-one, and its subsequent treatment with aqueous sulfuric acid. Formula (I).

专利号:WO-2023245091-A1
优先权日:2022-06-15
标题 :Pyridazinone-derived compounds for the modulation of myc and for medical uses
发明人：ADANVE BERTRAND; NG YAO ZONG; LAI JONATHAN
权利人:GENETIC INTELLIGENCE INC
摘要:Compositions, systems, and methods are described herein for the modulation, and in particular the reduction or inhibition, of expression or activity of MYC in a cell, animal or human subject. Such compositions, systems, and methods are useful to prevent, ameliorate, or treat diseases, including cell proliferation diseases and disorders such as cancer, particularly MYC-driven cancer. Compositions are described comprising a compound of formula (I), as well as pharmaceutical compositions or medicaments thereof. Also described are methods of use of such compositions to treat, prevent, or ameliorate diseases, including cell proliferation diseases and disorders such as cancer, in particular MYC-driven cancer. Compositions comprising conjugates and complexes of a compound of formula (I) are also described, which are also useful in the methods described herein. Methods are described comprising the use of a compound of formula (I), or pharmaceutical compositions thereof, for the reduction or inhibition of MYC expression or activity, and/or for achieving one or more desirable phenotypic outcomes such as, for example, decrease in cancer cell growth or proliferation, decrease in cancer cell viability, decrease in tumor volume (i.e., tumor regression), decrease in cancer metastasis, increase in animal or human survival, or other desired outcome with respect to particular phenotypes (e.g., body weight, metabolism, etc.). Related medicaments, kits, and methods of delivery of such compositions are described. Methods are also described for the development, manufacture, and/or synthesis of a compound of formula (I), as well as pharmaceutical compositions thereof. Furthermore, methods for diagnostics and testing comprising detecting MYC expression or activity levels, as well as compositions comprising kits for diagnostics and testing, are described.

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-2024393689-A1
优先权日:2023-05-26
标题 :Compounds, monomers, polymers, photoresist compositions and pattern formation methods
发明人：CUI LI; AQAD EMAD; HOELZEL CONNER; PARK JONG KEUN; LEE CHOONG-BONG; POPERE BHOOSHAN
权利人:DUPONT ELECTRONIC MAT INTERNATIONAL LLC
摘要:Compounds comprise a C 6-30 aromatic or C 3-30 heteroaromatic core, wherein the core comprises a first substituent comprising (i) an enol ether group or (ii) a halomethyl ether group, wherein the halomethyl ether group is substituted or unsubstituted, a second substituent comprising an acid labile group, and a third substituent that is a halogen atom. The core is optionally further substituted. The compounds find use in the synthesis of monomers and polymers, which may be used in photoresist compositions for the manufacture of electronic devices.

专利号:IT-201800003134-A1
优先权日:2018-02-28
标 题:PROCESS FOR THE SYNTHESIS OF 6-CHLOROMETHYLURACIL

专利号:US-2020407330-A1
优先权日:2018-02-28
标 题:Process for the synthesis of 6-chloromethyluracil