CAS: 911637-19-9; (S)-1-(2-Amino-4-(2,4-Bis(Trifluoromethyl)-5,8-Dihydropyrido[3,4-D]Pyrimidin-7(6H)-yl)-4-Oxobutyl)-5,5-Difluoropiperidin-2-One

该化合物是一种新的二型糖尿病抗抑制剂(DPP-4),主要用于管理二型糖尿病.作为Glippin类药物的成员,该抗抑制剂通过提高胰岛素激素水平发挥作用,这反过来又增加了胰岛素分泌,并减少以依赖葡萄糖的方式释放的葡萄卡酮.这一机制有助于改进血糖控制,同时又不会造成重大的低血糖症.Gemiglippin的特征是选择性抑制DPP-4,这有助于提高其功效和安全性能.该化合物通常通过口服管理,并经常与其他抗糖尿病剂结合使用,以实现更好的血糖管理.其致癌性能特性包括有利的吸收特征和相对较长的半衰期,允许一次性的消毒.此外,Gemigliptin已经研究其潜在的心血管功能,从而成为治疗2型糖尿病患者的宝贵选择,因为2型糖尿病可能引发心血管并发症.

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合成工艺路线路线简述

    📜(R)-1-(2β-Amino-4-(2,4-Bis(Trifluoromethyl)-5,8-Dihydropyrido[3,4-D]Pyrimidin-7(6H)-yl)-4-Oxobutyl)-5,5-Difluoropiperidin-2-One置于三羟甲基丙烷 三(3-巯基丙酸酯),偶氮二异丁腈体系中,用 对二甲苯 作为反应溶剂,化学反应生成 吉格列汀
    参考文献:Us2023/142248
    标题:Us2023/142248

    海关参考信息

    专利信息


    专利号:US-2012282255-A1
    优先权日:2011-04-07
    标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
    发明人:PLUCINSKI GREG
    权利人:PLUCINSKI GREG
    摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

    专利号:US-9963685-B2
    优先权日:2013-02-28
    标题 :Engineered transaminase polypeptides for industrial biocatalysis
    发明人:QUINTANAR-AUDELO MARTINA; EBERHARD ELLEN; NAZOR JOVANA; SMITH DEREK; WANG CUIXIA
    权利人:CODEXIS INC
    摘要:The present disclosure provides engineered transaminase polypeptides useful for the synthesis of chiral amine compounds under industrially relevant conditions. The disclosure also provides polynucleotides encoding the engineered transaminase polypeptides, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases for the production of chiral amine compounds.

    专利号:WO-2025096684-A1
    优先权日:2023-10-30
    标题 :Err modulators
    发明人:ELGENDY BAHAA; HEGAZY LAMEES; BURRIS THOMAS
    权利人:UNIV OF HEALTH SCIENCES AND PHARMACY IN ST LOUIS
    摘要:In one aspect, the present disclosure describes compounds which may be used to modulate the activity of an estrogen receptor-related orphan receptor (EER). Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

    专利号:WO-2025096683-A1
    优先权日:2023-10-30
    标 题:Err modulators
    发明人:ELGENDY BAHAA; HEGAZY LAMEES SHAMSELDIN; BURRIS THOMAS PATRICK
    权利人:UNIV OF HEALTH SCIENCES AND PHARMACY IN ST LOUIS
    摘要:In one aspect, the present disclosure describes compounds that may be used to modulate the activity of an estrogen receptor-related orphan receptor (EER). Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

    专利号:US-2020255394-A1
    优先权日:2018-09-26
    标题 :Crystalline solid forms of n-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl)phenyl)butanamide and methods of their synthesis

    专利号:CA-3113037-A1
    优先权日:2018-09-26
    标 题 :Crystalline forms of n-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oopropan-2-yl)-4-(4-(2-methyl-5-(2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl)phenl)butanamide and methods of their synthesis

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    主要参考文献


    1: Jung E, Kim J, Kim CS, Kim SH, Cho MH. Gemigliptin, a dipeptidyl peptidase-4 inhibitor, inhibits retinal pericyte injury in db/db mice and retinal neovascularization in mice with ischemic retinopathy. Biochim Biophys Acta. 2015 Dec;1852(12):2618-29. doi: 10.1016/j.bbadis.2015.09.010. Epub 2015 Sep 21. doi: 10.1016/j.vph.2015.07.005. Epub 2015 Jul 15. doi: 10.1016/j.ejphar.2015.04.055. Epub 2015 May 11. doi: 10.2147/DDDT.S75980. eCollection 2015.
    5: Jung E, Kim J, Kim SH, Kim S, Cho MH. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102. doi: 10.1016/j.ejphar.2014.10.008. Epub 2014 Oct 18. doi: 10.1185/03007995.2014.980886. Epub 2014 Nov 6. doi: 10.1007/s40268-014-0054-8.
    8: Hwang HJ, Jung TW, Ryu JY, Hong HC, Choi HY, Seo JA, Kim SG, Kim NH, Choi KM, Choi DS, Baik SH, Yoo HJ. Dipeptidyl petidase-IV inhibitor (gemigliptin) inhibits tunicamycin-induced endoplasmic reticulum stress, apoptosis and inflammation in H9c2 cardiomyocytes. Mol Cell Endocrinol. 2014 Jul 5;392(1-2):1-7. doi: 10.1016/j.mce.2014.04.017. Epub 2014 May 9. doi: 10.3109/00498254.2013.873156. Epub 2014 Apr 16. doi: 10.1111/dom.12292. Epub 2014 Apr 16. doi: 10.1007/s40261-014-0184-3. doi: 10.5414/CP202038. doi: 10.3109/00498254.2013.865856. Epub 2013 Dec 4. doi: 10.1007/s12272-013-0171-x. Epub 2013 Jun 15. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor gemigliptin compared with sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Obes Metab. 2013 Jun;15(6):523-30. doi: 10.1111/dom.12060. Epub 2013 Jan 30. doi: 10.1111/dom.12042. Epub 2012 Dec 17. doi: 10.1016/j.clinthera.2012.04.001. Epub 2012 Apr 24.

    合成参考文献


    参考文献:10.1007/s40256-020-00423-z
    摘要:Liakos CI, Papadopoulos DP, Sanidas EA, Markou MI, Hatziagelaki EE, Grassos CA, Velliou ML, Barbetseas JD. Blood Pressure-Lowering Effect of Newer Antihyperglycemic Agents (SGLT-2 Inhibitors, GLP-1 Receptor Agonists, and DPP-4 Inhibitors). American Journal of Cardiovascular Drugs. 2020 Aug 11;21(2):123–37. doi: 10.1007/s40256-020-00423-z.
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