枸橼酸托法替尼背景及作用机理:
枸橼酸托法替尼是由美国辉瑞制药公司开发一种治疗类风湿关节炎药物,商品名Xeljanz,用于对氨甲喋呤治疗应答不充分或不耐受的中至重度活动性类风湿关节炎(RA)成人患者。本产品是一种Janus激酶抑制剂,每日服用两次。
2012年11月6日,美国食品药品管理局(FDA)和辉瑞公司联合宣布,枸橼酸托法替尼获准用于对氨甲喋呤治疗应答不充分或不耐受的中至重度活动性类风湿关节炎(RA)成人患者。
Xeljanz可作为单一治疗或与氨甲喋呤或其他非生物疾病缓解性抗风湿药物(DMARD)联合使用。该药不应与生物性DMARD或强免疫抑制剂(如硫唑嘌呤和环孢菌素)联合使用。经核准的Xeljanz剂量为每日2次,每次5mg。
深圳远扬化学可提供托法替尼申报所用全套杂质, 随货附CoA证书,HNMR,MS,HPLC图谱,纯度符合申报要求,托法替尼杂质为我司优势杂质,长期备有库存,发货快。如需托法替尼杂质相关详细信息,欢迎我司业务人员获取~
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附:托法替尼申报用杂质列表:
Tofacitinib | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 1 | N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-1H-indol-4-amine |
Tofacitinib Impurity 2 | 2-chloro-N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
Tofacitinib Impurity 3 | 3-((3R,4R)-3-((2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)(methyl)amino)-4-methylpiperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 4 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)piperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 5 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxoprop* |
Tofacitinib Impurity 6 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanoic acid |
Tofacitinib Impurity 7 | N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-2-chloro-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
Tofacitinib Impurity 8 | N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride |
Tofacitinib Impurity 9 | 3-((3R,4S)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile compound with 3-((3S,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (1:1) |
Tofacitinib Impurity 10 | 3-((3S,4S)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 11 | (3R,4S)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride |
Tofacitinib Impurity 12 | (3S,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride |
Tofacitinib Impurity 13 | (3S,4S)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride |
Tofacitinib Impurity 14 | (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride |
Tofacitinib Impurity 15 | 3-((3R,4R)-3-(7H-[4,7'-bipyrrolo[2,3-d]pyrimidin]-4'-yl(methyl)amino)-4-methylpiperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 16 | (3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidine-1-carbaldehyde |
Tofacitinib Impurity 17 | N-methyl-N-((3R,4R)-4-methyl-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
Tofacitinib Impurity 18 | 3,3'-((3R,3'R,4R,4'R)-3,3'-((7H-pyrrolo[2,3-d]pyrimidine-2,4-diyl)bis(methylazanediyl))bis(4-methylpiperidine-3,1-diyl))bis(3-oxopropanenitrile) |
Tofacitinib Impurity 19 | 3-(4-(((3R,4R)-1-(2-cyanoacetyl)-4-methylpiperidin-3-yl)(methyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 20 | 3-((3R,4R)-3-((6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)(methyl)amino)-4-methylpiperidin-1-yl)-3-oxopropanenitrile |
Tofacitinib Impurity 21 | N-((3R,4R)-1-(2-cyanoacetyl)-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine oxide |
Tofacitinib Impurity 22 | (3R,4R)-1-(2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N,4-dimethylpiperidin-3-amine hydrochloride |
Tofacitinib Impurity 23 | (3R,4R)-N,4-dimethyl-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-amine |
Tofacitinib Impurity 24 | N-((3R,4R)-1,4-dimethylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride |
Tofacitinib Impurity 25 | 1-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)ethanone |
Tofacitinib Impurity 26 | N-((3R,4S)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine compound with N-((3S,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (1:1) |
Tofacitinib Impurity 27 | N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine |