CAS: 60719-84-8; 5-Amino-[3,4'-Bipyridin]-6(1H)-One

该化合物是主要用作心血管剂的药物化合物,属于磷柴油酶抑制剂类别,具体针对III类磷柴油酶.这一机制可提高心肌内折合性,促进血管血管变异,有利于治疗心脏衰竭和某些类型的冲击.Amrinone的特点是其能够提高细胞内循环AMP水平,从而在不大幅提高心脏率的情况下改善心脏产量.该化合物通常通过静脉注射进行,以相对短的半衰期为名,需要谨慎监测剂量和病人的反应.常见副作用可能包括低血压,心律不齐和胃肠扰动.由于其药理学特征,氨经常被用于急性环境,特别是那些对常规疗法没有做出充分反应的病人.但是,由于出现了能够提供更安全性和效能特征的新剂,其使用率已经下降.

结构式图片

相似化合物

75898-90-7 62749-34-2 62749-26-2

欧盟法规

ECHA物质C&L通报REACH预注册

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CAS号62749-46-6 2-oxo-5-pyridin... | CAS号62749-33-1 5-nitro-1H-[3,4... | CAS号893440-43-2 (5-iodo-2-metho... | CAS号893440-45-4 (2-甲氧基-5-(4,4,5...

合成工艺路线路线简述

    3-<<(Benzyloxy)Carbonyl>Amino>-5-Iodopyrid-2-One置于palladium Dihydroxide Bis-Triphenylphosphine-Palladium(II) Chloride,三甲基氯硅烷,氢气,Silver Carbonate,Sodium Iodide体系中,用 1,4-二氧六环,甲醇,氯仿,乙腈 作为反应溶剂,化学反应 49.5H,反应生成 氨力农
    参考文献:Durrant,Steven J.; Pinder,Joanne L.; Charrier,Jean-Damien,Heterocycles,2006,Vol. 70,P. 509-517
    标题:Durrant,Steven J.; Pinder,Joanne L.; Charrier,Jean-Damien,Heterocycles,2006,Vol. 70,P. 509-517

    海关参考信息

    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-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-6930113-B2
    优先权日:1996-11-01
    标题 :Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
    发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ; EARL RICHARD A; KHANAPURE SUBHASH P
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

    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.

    专利号:US-2008090885-A1
    优先权日:2006-10-12
    标题:Preparation of losartan 5-carboxylic acid and use thereof
    发明人:CHEN LIQIN; LI JIAN; SHEN YINGZHONG
    权利人:CHEN LIQIN; LI JIAN; SHEN YINGZHONG
    摘要:A method for synthesis of losartan 5-carboxylic acid (EXP-3174).

    专利号:US-12295961-B2
    优先权日:2009-12-31
    标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
    发明人:DHINGRA OM
    权利人:MARIUS PHARMACEUTICALS INC
    摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
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    主要参考文献


    1: Shepherd G. Treatment of poisoning caused by beta-adrenergic and calcium- channel blockers. Am J Health Syst Pharm. 2006 Oct 1;63(19):1828-35. doi: 10.2146/ajhp060041. Erratum in: Am J Health Syst Pharm. 2008 Sep 1;65(17):1592. 3(6 Suppl 2):10-4. doi: 10.1016/0888-6296(89)90054-9. 29(3):394-401. doi: 10.1038/clpt.1981.54. 121(6 Pt 2):1939-44. doi: 10.1016/0002-8703(91)90828-6. 27(2):231-2. doi: 10.1097/00003246-199902000-00002. 48(9):573-80. Spanish. 18(1 Pt 2):S56-60. 53(6):661-7. doi: 10.1038/clpt.1993.87.
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    合成参考文献


    参考文献:10.1159/000089954
    摘要:Toyoshima K, Momma K, Imamura S, Nakanishi T. In vivo dilatation of the fetal and postnatal ductus arteriosus by inhibition of phosphodiesterase 3 in rats. Biol Neonate. 2006;89(4):251–6. doi: 10.1159/000089954.
    参考文献:10.1186/cc10307
    摘要:Hasslacher J, Bijuklic K, Bertocchi C, Kountchev J, Bellmann R, Dunzendorfer S, Joannidis M. Levosimendan inhibits release of reactive oxygen species in polymorphonuclear leukocytes in vitro and in patients with acute heart failure and septic shock: a prospective observational study. Crit Care. 2011 Jul 12;15(4):R166.
    参考文献:10.1007/s11936-011-0142-9
    摘要:Bronicki RA. Perioperative Management of Pulmonary Hypertension in Children with Critical Heart Disease. Current Treatment Options in Cardiovascular Medicine. 2011 Jul 19;13(5):402. doi: 10.1007/s11936-011-0142-9.
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