CAS: 143201-11-0; Sodium (3R,5S,E)-7-(4-(4-Fluorophenyl)-2,6-Diisopropyl-5-(Methoxymethyl)Pyridin-3-yl)-3,5-Dihydroxyhept-6-Enoate

该化合物是合成化合物,主要被归类为一种凝固剂,这是一种用于降低血液胆固醇水平的药物,其作用是抑制酶HMG-CoA再生酶,它在胆固醇的生物合成中起着关键作用.里瓦斯塔廷的特征是它能够减少低密度的脂质(LDL)胆固醇和三甘油,同时可能增加高密度的脂质(HDL)胆固醇,该化合物一般是口服的,以其有利的药性皮肤素特征为名,包括良好的吸收和新陈代谢.里瓦斯塔廷还可能表现出抗炎和抗氧化性特性,有助于除胆固醇管理外的心血管健康.它与其他statin一样,它可能具有副作用,包括肌肉疼痛和肝酶改变,在治疗期间必须进行监测.

结构式图片

合成工艺路线路线简述

    📜3-{2-[4-(4-Fluorophenyl)-5-(Methoxymethyl)-2,6-Di(Propan-2-yl)Pyridin-3-Yl]Ethenyl}-5-Hydroxycyclohexan-1-One 反应生成西立伐他汀钠
    参考文献:J. Labelled Compd. Rad. 1999,42,101-108
    标题:J. Labelled Compd. Rad. 1999,42,101-108

    海关参考信息

    专利信息


    专利号:US-8293290-B2
    优先权日:2003-04-08
    标题:Annatto extract compositions, including geranyl geraniols and methods of use
    发明人:TAN BARRIE
    权利人:TAN BARRIE; AMERICAN RIVER NUTRITION INC
    摘要:Annatto extract composition (AEC), including cis and trans geranyl geraniols (GG) and tocopherol-free C-5 unsubstituted tocotrienols (T3), increases the de novo synthesis of intermediate isoprenoid and distal protein products, including endogenous coenzyme Q10 (CoQ10), dolichols (DL) and all subsequent GG-prenylated and DL-glycosylated proteins, including GG-porphyrinated hemes. This intermediate and distal product replenishment by AEC reverses maladies of myotoxicity (of both drug and non-drug origins), including maladies that affect the muscle, kidney, eye, GI tract and skin, nerve, blood, and CoQ10-related syndromes of energetics and LDL protection. AEC anabolically increases the endogenous de novo CoQ10 synthesis via GG elongation/prenylation of side-chain and conversely CoQ10 catabolically increases the endogenous de novo GG synthesis via beta-oxidation of CoQ10. Also, such AEC decreases de novo synthesis and increases disposal of triglycerides (TG) in humans via PPAR activation and SREBP deactivation. Such drop in TG by AEC reverses maladies of insulin resistance (IR) and metabolic syndrome (MS), prediabetes, diabetes and diabetes-related cardiovascular diseases (CVD). GG activates PPAR and down regulates SREBP transcription factors. This AEC, containing GG, inhibits cancer growth whether or not GG involvement in protein prenylation is required.

    专利号:US-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

    专利号:US-7708989-B2
    优先权日:1999-10-29
    标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
    发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
    权利人:NITROMED INC
    摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

    专利号:WO-2017046598-A1
    优先权日:2015-09-16
    标题:Treatment of acute inflammatory disorders
    发明人:CRISANTI ANDREA; CANAVESE MIRIAM
    权利人:CRISANTI ANDREA; IMP INNOVATIONS LTD
    摘要:The present invention relates to a VEGF receptor agonist for use in the treatment of an acute inflammatory disorder associated with the overproduction of pro-inflammatory cytokine, administered with an agent that induces the synthesis of Nrf2. The invention also relates to pharmaceutical combinations comprising a VEGF receptor agonist and an agent that induces the synthesis of Nrf2, and kits comprising these agents. The described uses, combinations and methods may prevent or reduce the dis-regulated activation of an inflammatory response and reduce endothelial damage.

    专利号:US-7384976-B2
    优先权日:2001-05-02
    标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC
    摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

    专利号:US-7235237-B2
    优先权日:1999-10-29
    标 题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
    发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
    权利人:NITROMED INC
    摘要:The present invention provides methods of treating or preventing vascular diseases caused by nitric oxide (NO) insufficiency. The methods encompass administering a composition comprising an antioxidant, a compound to treat cardiovascular diseases, a nitrosated compound, a compound that donates, transfers or relases NO, or is a NO synthase substrate, or endogenously stimulates NO synthesis, or stimulates levels of endothelium derived relaxing factor. In the said composition, a hydralazine compound may be an antioxidant, isosorbide mono-or dinitrate may be the compound to donate, transfer, release, or stimulate endogenous NO synthesis. The isorsorbide may also elevate endogenous levels of endotherlium-derived relaxing factor, or be a NO synthase substrate and angiotensin enzyme inhibitor may be nitrosated compound. Disclosed in the invention is also a method to treat, or prevent Renaud's syndrome by administering a therapeutically effective amount of an antioxidant, a NO donor, a nitrosated compound and novel sustained-release formulations (e.g. a transdermal patch).

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Mezquita B, Mezquita P, Pau M, Gasa L, Navarro L, Samitier M, Pons M, Mezquita C. All-trans-retinoic acid activates the pro-invasive Src-YAP-Interleukin 6 axis in triple-negative MDA-MB-231 breast cancer cells while cerivastatin reverses this action. Sci Rep. 2018 May 4;8(1):7047. doi: 10.1038/s41598-018-25526-1.
    2: Yao Y, Toshimoto K, Kim SJ, Yoshikado T, Sugiyama Y. Quantitative Analysis of Complex Drug-Drug Interactions between Cerivastatin and Metabolism/Transport Inhibitors Using Physiologically Based Pharmacokinetic Modeling. Drug Metab Dispos. 2018 Jul;46(7):924-933. doi: 10.1124/dmd.117.079210. Epub 2018 Apr 30. doi: 10.1124/jpet.118.247643. Epub 2018 Apr 25.
    4: Gaukler SM, Ruff JS, Galland T, Underwood TK, Kandaris KA, Liu NM, Morrison LC, Veranth JM, Potts WK. Quantification of cerivastatin toxicity supports organismal performance assays as an effective tool during pharmaceutical safety assessment. Evol Appl. 2016 Apr 15;9(5):685-96. doi: 10.1111/eva.12365. eCollection 2016 Jun.

    合成参考文献


    参考文献:10.1007/s00417-009-1282-4
    摘要:Hata Y, Miura M, Asato R, Kita T, Oba K, Kawahara S, Arita R, Kohno R, Nakao S, Ishibashi T. Antiangiogenic mechanisms of simvastatin in retinal endothelial cells. Graefe's Archive for Clinical and Experimental Ophthalmology. 2010 Feb 13;248(5):667–73. doi: 10.1007/s00417-009-1282-4.
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