CAS: 129-06-6; Warfarin-Sodium

该化合物是一种抗冷凝剂,主要用于防止各种医疗条件下的血凝块,如酸性纤维化和深血管血栓,是一种合成的科马林衍生物,其功能是抑制维生素K 聚氧氧化还原酶,这是合成维生素K依赖凝聚因子所必不可少的.该化合物的特征是由R和Santomos构成的种族混合物,每种药物都具有不同的药理特性.Warfarin 钠通常通过口服方式施用,以其狭窄的治疗指数而著称,需要仔细监测血液凝聚水平,通常由国际统一比率测量.该物质在水中溶解,其分子重量相对较低.其致癌性涉及吸收,主要在肝脏中的代谢和通过尿液排泄.由于它具有强大的影响,而且有可能与各种药物和饮食因素发生相互作用,病人的治疗需要全面了解其药理动力学和药理学.

结构式图片

欧盟法规

ECHA物质C&L通报欧盟生物杀灭剂法规欧盟《生物杀灭剂法规》REACH预注册

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CAS号81-81-2 杀鼠灵 | CAS号24579-14-4 4-羟基华法林

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    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-6869973-B2
    优先权日:2000-06-22
    标题:Nitrosated and nitrosylated taxanes, compositions and methods of use
    发明人:GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; RICHARDSON STEWART K; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, 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 present invention also provides novel compositions comprising at least one taxane 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 compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.

    专利号:US-2003203915-A1
    优先权日:2002-04-05
    标题 :Nitric oxide donors, compositions and methods of use related applications
    发明人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
    权利人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
    摘要:The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.
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    主要参考文献


    1: Atoui M, Gunda S, Lakkireddy D. Left atrial appendage closure is preferred to chronic warfarin therapy: the pro perspective. Card Electrophysiol Clin. 2015 Sep;7(3):403-13. doi: 10.1016/j.ccep.2015.05.019. Epub 2015 Jul 10. Review. doi: 10.1016/j.mgene.2015.05.003. eCollection 2015 Sep. Review.
    3: Entezari-Maleki T, Dousti S, Hamishehkar H, Gholami K. A systematic review on comparing 2 common models for management of warfarin therapy; pharmacist-led service versus usual medical care. J Clin Pharmacol. 2015 Jun 22. doi: 10.1002/jcph.576. [Epub ahead of print] Review. doi: 10.1016/j.ijcard.2015.06.006. Epub 2015 Jun 15. Review. doi: 10.1542/peds.2014-2578. Review. doi: 10.3978/j.issn.2072-1439.2015.01.23. Review.
    7: Watanabe H, Itoh H, Tsuchiya Y, Miyagi N, Sugiyama T, Nakai Y, Shinozaki Y, Noguchi T, Jinbu Y, Kusama M. [Reinforcement of warfarin action in a patient administered S-1]. Gan To Kagaku Ryoho. 2015 Jan;42(1):131-3. Review. Japanese. doi: 10.1146/annurev-med-051113-024633. Review. doi: 10.1161/CIRCULATIONAHA.114.010426. Review. doi: 10.1517/14740338.2015.973847. Epub 2014 Oct 24. Review. doi: 10.1016/j.tcm.2014.09.001. Epub 2014 Sep 6. Review.

    合成参考文献


    摘要:American Journal of Diseases of Children., 147(609), 1993
    摘要:Therapie., 18(921), 1963 []
    摘要:U.S. Environmental Protection Agency. 1998. Extremely Hazardous Substances (EHS) Chemical Profiles and Emergency First Aid Guides. Washington, D.C.: U.S. Government Printing Office.
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