CAS: 117707-40-1; (S)-9-Fluoro-3-Methyl-7-Oxo-10-(Piperazin-1-yl)-3,7-Dihydro-2H-[1,4]Oxazino[2,3,4-Ij]Quinoline-6-Carboxylic Acid

上下游产品

CAS号110-85-0 哌嗪 | CAS号100986-89-8 左旋氧氟沙星羧酸 | CAS号60-29-7 乙醚

📜(-)-Ethyl 2-<<<(R)-1-Hydroxyprop-2-Yl>Amino>Methylene>-3-Oxo-3-(2,3,4,5-Tetrafluorophenyl)Propionate置于水,Potassium Carbonate,Sodium Hydroxide体系中,用 乙醇,N,N-二甲基乙酰胺,二甲基亚砜 用作溶剂,化学反应 17.42H,反应生成9-氟-3-甲基-7-氧代-10-(1-哌嗪基)-2,3-二氢-7H-[1,4]恶嗪并[2,3,4-Ij]喹啉-6-羧酸
参考文献: Antibiotic Resistance Breakers[fr] Agents De Rupture De Résistance Aux Antibiotiques
标题: Antibiotic Resistance Breakers[fr] Agents De Rupture De Résistance Aux Antibiotiques
摘要:该发明涉及公式(a1)的抗生素化合物及其药学上可接受的盐,溶剂化合物,互变异构体和它们的组合,其中x和l是可选的连接物,Ra或r1中的一个包括ar1,其中ar1是一种抗生素耐药性破坏基团,包括可选择取代的c6-10芳基,C7-13芳基烷基,C5-10杂芳基,C6-13杂芳基烷基,C5-10杂环烷基,C6-13杂环烷基,C3-10碳环烷基,C4-13碳环烷基,-C(=nr')-Nr'R''或-ch2-Ch=ch2基团;在将该化合物用于细菌感染后,该基团减少或预防外流.该发明还公开了包括公式(a1)化合物的药物组合物以及将这些化合物用作药物的用途,特别是用于治疗细菌感染,如耐药性细菌感染.

专利信息

专利号:US-2010273787-A1
优先权日:2007-11-15
标题:Kynurenine-aminotransferase inhibitors
发明人：SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO
权利人:SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO
摘要:Compounds of formula (I): prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3-hydroxy kynurenine.