CAS: 1353900-92-1; Dimethyl ((2S,2'S,3R,3'R)-((2S,2'S)-(((2R,5R)-1-(3,5-Difluoro-4-(4-(4-Fluorophenyl)Piperidin-1-yl)Phenyl)Pyrrolidine-2,5-Diyl)Bis(5-Fluoro-1H-Benzo[d]Imidazole-6,2-Diyl))Bis(Pyrrolidine-2,1-Diyl))Bis(3-Methoxy-1-Oxobutane-1,2-Diyl))Dicarbamate

上下游产品

(2S,2'S)-[[(2R,5R)-1-[3,5-二氟-4-(4-(4-氟苯基)哌啶-1-基)苯胺]-2,5-双四氢吡咯基]双[6-氟-2-(2S)-2-四氢吡咯-1H-苯并咪唑-2,5-二基)]双(1-四氢吡咯甲酸叔丁酯) (2S,2'S)-Di-Tert-Butyl 2,2'-(6,6'-((2R,5R)-1-(3,5-Difluoro-4-(4-(4-Fluorophenyl)Piperidin-1-yl)Phenyl)Pyrrolidine-2,5-Diyl)Bis(5-Fluoro-1H-Benzo[d]Imidazole-6,2-Diyl))Bis(Pyrrolidine-1-Carboxylate) 1890114-11-0
5,5'-[(2R,5R)-1-[3,5-二氟-4-(4-(4-氟苯基)哌啶-1-基)苯胺]-2,5-双四氢吡咯啉基]双[6-氟-2-(2S)-2-四氢吡咯-1H-苯并咪唑] (S)-6,6'-((2R,5R)-1-(3,5-Difluoro-4-(4-(4-Fluorophenyl)Piperidin-1-yl)Phenyl)Pyrrolidine-2,5-Diyl)Bis(5-Fluoro-2-((S)Pyrrolidin-2-yl)-1Hbenzo[d]Imidazole) 1332357-14-8
(2S,2'S)-Di-Tert-Butyl 2,2'-(((((2R,5R)-1-(3,5-Difluoro-4-(4-(4-Fluorophenyl)Piperidin-1-yl)Phenyl)Pyrrolidine-2,5-Diyl)Bis(5-Fluoro-2-Nitro-4,1-Phenylene))Bis(Azanediyl))-Bis(Carbonyl))Bis(Pyrrolidine-1-Carboxylate) 1890114-10-9
1-(4-((2R,5R)-2,5-Bis(4-Chloro-2-Fluoro-5-Nitrophenyl)Pyrrolidin-1-yl)-2,6-Difluorophenyl)-4-(4-Fluorophenyl)Piperidine 1332356-86-1

O-甲基-L-苏氨酸置于碳酸氢钠,N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.42H,反应生成匹布他韦
参考文献:苯并咪唑连接的吡咯烷的结构与活性关系的重点,导致发现丙型肝炎病毒ns5A抑制剂哌布那斯韦(abt-530)
标题:苯并咪唑连接的吡咯烷的结构与活性关系的重点,导致发现丙型肝炎病毒ns5A抑制剂哌布那斯韦(abt-530)
摘要:丙型肝炎病毒(hcv)感染患者的治疗性干扰素和利巴韦林保留疗法需要机械正交的直接作用抗病毒药的组合.这些治疗的共同成分通常是hcv Ns5A抑制剂.包括成分ns5A抑制剂在内的第一代fda批准的治疗方法,对hcv病毒基因型1-6的疗效均不相同.特别地,这些第一代ns5A抑制剂倾向于选择病毒药物抗性.Ombitasvir是第一代hcv Ns5A抑制剂,被列为viekira Pak的关键成分,用于治疗hcv基因型1感染的患者.自从推出下一代hcv治疗以来,已经实现了针对1-6型hcv基因型感染的功能性治愈,并且缩短了更广泛基因型范围内的治疗时间.
Doi:10.1021/acs.Jmedchem.8B00082

专利信息

专利号:US-2024207302-A1
优先权日:2021-04-01
标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
发明人：CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.