会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明专利
    • PROCESS FOR PRODUCING 4'-ETHYNYL d4T
    • 生产4'-乙基d4T的方法
    • JP2014148506A
    • 2014-08-21
    • JP2014008853
    • 2014-01-21
    • Oncolys Biopharma Incオンコリスバイオファーマ株式会社
    • NAGAI KATSUYUKIKIGUCHI SHINYAFURUYAMA HIROYAWILLIAM EWAN HUMETSUJIMOTO SATOSHI
    • C07D405/04
    • C07D307/32C07D307/33C07D405/04
    • PROBLEM TO BE SOLVED: To provide a process for producing a compound simply, at a low cost, and in a large quantity, which becomes an active ingredient of a therapeutic medicament for an HIV infection: 4'-ethynyl-2',3'-didehydro-3'-deoxythymidine (4'-ethynyl d4T).SOLUTION: Provided is a process for producing 4'-ethynyl d4T comprising reacting a compound represented by a formula (III) and thymine, the compound being obtained by reacting a furfuryl alcohol derivative or levoglucosenone with a triple bond compound having H or a tri-substituted silyl group on one end and Li, Al, or monohalogenated Mg on another end, and introducing triple bond containing group. [Ror Rrepresents, H, an acyl group, an alkyl group, an alkenyl group, an aryl group, an aralkyl group, a cycloalkyl group, a heterocyclic group, a heterocyclic alkyl group, or a tri-substituted silyl group; and Rrepresents H or a tri-substituted silyl group.]
    • 要解决的问题:提供简单地,低成本和大量地生成化合物的方法,其成为用于HIV感染的治疗药物的活性成分:4'-乙炔基-2',3' - 二脱氢-3'-脱氧胸苷(4'-乙炔基d4T)。溶液:提供一种生产4'-乙炔基d4T的方法,包括使由式(III)表示的化合物与胸腺嘧啶反应,该化合物是通过使糠基 醇衍生物或左旋葡萄糖酮与一端具有H或三取代甲硅烷基的三键化合物,另一端为Li,Al或单卤代Mg,并引入含三键的基团。 酰基,烷基,烯基,芳基,芳烷基,环烷基,杂环基,杂环烷基或三取代甲硅烷基; R代表H或三取代甲硅烷基。]
    • 3. 发明申请
    • COMBINATION MOLECULARLY TARGETED DRUG FOR TUMOR THERAPY AND PREVENTION
    • 用于肿瘤治疗和预防的组合分子靶向药物
    • WO2014115859A3
    • 2014-10-16
    • PCT/JP2014051589
    • 2014-01-25
    • SAKAI TOSHIYUKIONCOLYS BIOPHARMA INC
    • SAKAI TOSHIYUKI
    • A61K31/395A61K31/5377A61K45/00A61P35/00A61P43/00
    • A61K31/395A61K31/4439A61K31/4745A61K31/5377A61K45/06A61K2300/00
    • In order to provide a therapeutic and preventative means for a wide range of cancers and tumors including cancers exhibiting PI3K/Akt pathway activation or p53 loss, and tumors for which conventional therapies such as chemotherapy, radiotherapy and hormone therapy have low effectiveness, the present invention combines the use of OBP-801 and different molecularly targeted drugs that act as PI3K inhibitors, suitably LY294002, BKM120, GDC-0941, BEZ235, BYL719 or CH5132799. Thus enabled is the provision of a novel, clinically effective strategy for the therapy and prevention of tumors and applicable to a wide range of tumors, the strategy enabling the simultaneous achievement of various significant pharmacological effects, which could not be achieved by the prescription of the molecularly targeted drugs as a single agent, namely the synergistic activation of capsase pathways, enhanced Bim expression, increased accumulation of intracellular reactive oxygen species, and inhibited survivin and XIAP protein expression.
    • 为了提供广泛的癌症和肿瘤的治疗和预防手段,包括表现出PI3K / Akt通路激活或p53丧失的癌症,以及诸如化学疗法,放射疗法和激素疗法的常规治疗效果低的肿瘤,本发明 结合使用OBP-801和作为PI3K抑制剂的适当LY294002,BKM120,GDC-0941,BEZ235,BYL719或CH5132799的不同分子靶向药物。 因此,提供了一种新颖的临床有效的治疗和预防肿瘤的策略,适用于广泛的肿瘤,这种策略能够同时实现各种显着的药理作用,这些策略无法通过处方 分子靶向药物作为单一药剂,即协同活化的辣椒素途径,增强Bim表达,增加细胞内活性氧的积累,并抑制存活蛋白和XIAP蛋白的表达。