CAS: 2222941-37-7; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-Dimethylisoxazol-4-yl)-1-(Trans-4-Methoxycyclohexyl)-1H-Benzo[d]Imidazol-2-yl)Piperidin-2-One

📜(S)-2-哌啶酮-6-羧基 酸 在 Potassium Carbonate,溶剂黄146,1-丙基磷酸酐,N,N-二异丙基乙胺体系中,用 1,4-二氧六环,二氯甲烷,水,甲苯作为反应溶剂,反应 37.77H,获得 (S)-6-(5-(3,5-Dimethylisoxazol-4-yl)-1-((1R,4S)-4-Methoxycyclohexyl)-1H-Benzo[D]Imidazol-2-yl)-1-(3,4-Difluorophenyl)Piperidin-2-One
参考文献:[En] Process For Preparing Modulators Of P300 And/Or Cbp[Fr] Pr°Cédé De Préparation De Modulateurs De P300 Et/Ou Cbp
标题:[En] Process For Preparing Modulators Of P300 And/Or Cbp[Fr] Pr°Cédé De Préparation De Modulateurs De P300 Et/Ou Cbp
摘要:生产以下化学式(I)所示化合物的方法,该方法包括:(A)用以下化学式(5)所示的化合物处理以下化学式(6)所示的化合物,获得以下化学式(7)所示的中间化合物;(B)用上述定义的化学式(7)所示的化合物处理以下化学式(8)所示的化合物;以及(C)回收上述定义的化学式(I)所示的化合物.化学式(I)所示的化合物是一种有望调节p300/Cbp活性的化合物,在治疗癌症方面具有潜在的用途,包括前列腺癌,血液系统癌症,膀胱癌和肺癌.

专利信息

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.