CAS: 1191995-00-2; (S)-2-(4-(2-Chlorophenoxy)-2-Oxo-2,5-Dihydro-1H-Pyrrol-1-yl)-N-(1-((R)-2,3-Dihydroxypropyl)-1H-Pyrazol-3-yl)-4-Methylpentanamide
该化合物是一流的双性甘油酶活化器(GKA),旨在调节2型糖尿病(T2DM)患者的葡萄糖代谢作用.它通过针对胰岛素和肝炎甘油酶,强化了葡萄糖刺激的胰岛素分泌,改进了肝糖的吸收,解决了葡萄糖软体保持中的关键缺陷.它的操作机制为控制糖糖浆提供了独特的方法,将其与常规抗糖尿病疗法区分开来.临床研究表明,它有可能恢复胃炎乙型细胞的葡萄糖敏感性,减少节食和后脑部高血糖.Dorzagliatin平衡地激活葡萄糖素可能会提供一种有利的安全配置,比其他葡萄糖降压剂更低的缺血糖风险.
- 英文名称(S)-2-(4-(2-Chlorophenoxy)-2-Oxo-2,5-Dihydro-1H-Pyrrol-1-yl)-N-(1-((R)-2,3-Dihydroxypropyl)-1H-Pyrazol-3-yl)-4-Methylpentanamide
- 中文名称多扎格列亚汀
- IUPAC名称(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-methylpentanamide
- CAS编号1191995-00-2
- MFCD编号:MFCD22376579
- FDA UNII编号:X59W6980E8
- 分子式:C22H27ClN4O5分子量:462.93
- 产品CID: 254712
- 同类组份化合物CAS1191995-14-8 (HCl)1191995-00-2 (free base)
- 产品分类有机原料 → 有机酸及其衍生物 → 羧酸及其衍生物
物理性质
- 沸点761.7±60.0 °C at 760 mmHg
- 闪点414.5±32.9 °C
- 密度1.4±0.1 g/cm3
- pKa:12.84±0.70(预测)
- LogP:2.78
- 折射率1.631
- 蒸汽压0.0±2.7 mmHg at 25°C
- 溶解性DMSO:108.5(Max Conc. mg/mL);234.38(Max Conc. Mm) Ethanol:92.0(Max Conc. mg/mL);198.73(Max Conc. Mm)
- 外观形态白色至类白色固体
- 储存条件-20°C，密闭，干燥环境
- 产品应用该化合物用作医治2型肺结核的成年病人.它通过激活甘油素(葡萄糖软糖中的一种关键酶),特别是加强葡萄糖后调节,改善了二型肝素患者的基因控制和细胞功能.
MSDS等安全信息
上下游产品
(S)-2-[4-(2-Chloro-Phenoxy)-2-Oxo-2,5-Dihydro-Pyrrol-1-Yl]-4-Methyl-Pentanoic Acid [1-((R)-2,2-Dimethyl-[1,3]Dioxolan-4-Yl-Methyl)-1H-Pyrazol-3-Yl]-Amide 1191994-99-6合成工艺路线路线简述
📜(S)-2-[4-(2-Chloro-Phenoxy)-2-Oxo-2,5-Dihydro-Pyrrol-1-Yl]-4-Methyl-Pentanoic Acid [1-((R)-2,2-Dimethyl-[1,3]Dioxolan-4-Yl-Methyl)-1H-Pyrazol-3-Yl]-Amide置于盐酸体系中,用 水,异丙醇 用作溶剂,化学反应 2.0H,以96.7%的收率获得无
参考文献:Pyrrolidinone Glucokinase Activators
标题:Pyrrolidinone Glucokinase Activators
摘要:提供的化合物为公式(i): 以及药学上可接受的盐,其中取代基如说明书中所披露.这些化合物以及包含它们的药物组合物,可用于治疗代谢性疾病和障碍,例如,2型糖尿病.
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2903919090-氯苯
2905122000-异丙醇 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-9388168-B2
优先权日:2012-12-25
标 题:Process for the preparation of 1-([1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-ylamine
发明人：CHEN JUNLI; REN YI; SHE JIN; WANG LIN
权利人:HUA MEDICINE
摘要:The present invention relates to a novel process for the preparation of of the formula (I) (I) wherein R 1 and R 2 are described herein. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds for treating diseases or conditions associated with inhibiting actin polymerization.
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Yang W, Zhu D, Gan S, Dong X, Su J, Li W, Jiang H, Zhao W, Yao M, Song W, Lu Y, Zhang X, Li H, Wang G, Qiu W, Yuan G, Ma J, Li W, Li Z, Wang X, Zeng J, Yang Z, Liu J, Liang Y, Lu S, Zhang H, Liu H, Liu P, Fan K, Jiang X, Li Y, Su Q, Ning T, Tan H, An Z, Jiang Z, Liu L, Zhou Z, Zhang Q, Li X, Shan Z, Xue Y, Mao H, Shi L, Ye S, Zhang X, Sun J, Li P, Yang T, Li F, Lin J, Zhang Z, Zhao Y, Li R, Guo X, Yao Q, Lu W, Qu S, Li H, Tan L, Wang W, Yao Y, Chen D, Li Y, Gao J, Hu W, Fei X, Wu T, Dong S, Jin W, Li C, Zhao D, Feng B, Zhao Y, Zhang Y, Li X, Chen L. Dorzagliatin add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled phase 3 trial. Nat Med. 2022 May;28(5):974-981. doi: 10.1038/s41591-022-01803-5. Epub 2022 May 12.
2: Syed YY. Dorzagliatin: First Approval. Drugs. 2022 Dec;82(18):1745-1750. doi: 10.1007/s40265-022-01813-0. 28(5):965-973. doi: 10.1038/s41591-022-01802-6. Epub 2022 May 12. 72(2):299-308. doi: 10.2337/db22-0708.
5: Zhu D, Gan S, Liu Y, Ma J, Dong X, Song W, Zeng J, Wang G, Zhao W, Zhang Q, Li Y, Fang H, Lv X, Shi Y, Tian H, Ji L, Gao X, Zhang L, Bao Y, Lei M, Li L, Zeng L, Li X, Hou X, Zhao Y, Hu T, Ge X, Zhao G, Li Y, Zhang Y, Chen L. Dorzagliatin monotherapy in Chinese patients with type 2 diabetes: a dose- ranging, randomised, double-blind, placebo-controlled, phase 2 study. Lancet Diabetes Endocrinol. 2018 Aug;6(8):627-636. doi: 10.1016/S2213-8587(18)30105-0. Epub 2018 May 4. Erratum in: Lancet Diabetes Endocrinol. 2018 May 10;: 80(5):467-475. doi: 10.1007/s40265-020-01278-z. 37(1):606-615. doi: 10.1080/14756366.2021.2025362.
合成参考文献
参考文献:10.1111/dom.13338
摘要:Zhu XX, Zhu DL, Li XY, Li YL, Jin XW, Hu TX, Zhao Y, Li YG, Zhao GY, Ren S, Zhang Y, Ding YH, Chen L. Dorzagliatin (HMS5552), a novel dual-acting glucokinase activator, improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes: A 28-day treatment study using biomarker-guided patient selection. Diabetes Obes Metab. 2018 Sep;20(9):2113–20. doi: 10.1111/dom.13338.
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