CAS: 129-51-1; Ergonovine Maleate

该化合物是一种主要用于产科的药物化合物,主要用于管理产后出血和诱发子宫萎缩,是一种半合成的甘醇衍生物,具体地来自真菌三氯硝基苯,具体地来自真菌三氯硝基苯,该物质在水中是白色的脱白晶粉,可溶于水,适合注射.其行动机制包括刺激甲型肾上腺受体,导致血管受限和子宫结膜增加.乙型甘草甲酸通常通过肌肉内或静脉注射途径施用,其影响可能很快,由于可能造成的副作用,如高血压和恶心,需要仔细监测.该化合物被归类为处方药,在某些条件下,包括高血压和心血管疾病中,具有抗药性.与所有药物一样,必须在医疗监督下使用甲状腺来降低风险,确保适当的治疗结果.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    📜N,N'-羰基二咪唑,顺丁烯二酸,麦角酸 反应生成马来酸麦角新碱
    参考文献:Borucky,Jan;Andrysek,Stanislav
    标题:Borucky,Jan;Andrysek,Stanislav

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    专利信息


    专利号:US-2003050305-A1
    优先权日:2000-05-22
    标题:Thromboxane inhibitors, compositions and methods of use
    发明人:TEJADA INIGO SAENZ DE
    摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

    专利号:US-6469065-B1
    优先权日:1996-02-02
    标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
    发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, 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 are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, 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 benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

    专利号:US-6436997-B1
    优先权日:1998-06-01
    标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension
    发明人:DE TEJADA INIGO SAENZ
    权利人:NITROMED INC
    摘要:The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides methods of promoting vasorelaxation and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, at least one vasoactive agent and/or thromboxane A2 receptor antagonist. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions resulting from an abnormally high level of arginase activity, such as, heart disease, systemic hypertension, pulmonary hypertension, sexual dysfunction, autoimmune disease, chronic renal failure and cerebral vasospasm. The present invention also provides methods for treating clinical conditions associated with a deficient nitric oxide pathway by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists.

    专利号:US-6693122-B2
    优先权日:1999-05-12
    标题:Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
    发明人:GARVEY DAVID S; SAENZ DE TEJADA INIGO
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, 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 vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, 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 vasoactive agent. 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 cardiovascular disorders, cerebrovascular disorders, hypertension, asthma, baldness, urinary incontinence, epilepsy, sleep disorders, gastrointestinal disorders, migraines, irritable bowel syndrome and sensitive skin.

    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-7238814-B2
    优先权日:2000-05-09
    标题:Compositions of S-nitrosothiols and methods of use
    发明人:MAREK PRZEMYSLAW A; TROCHA ANDZREJ M; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K
    权利人:NITROMED INC
    摘要:The invention describes compositions and kits comprising 4-aza-4-(2-methyl-2-sulfanylpropyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-aza-4-(2-methyl-2-(nitrosothio)propyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-{1-methyl-1-((2,4,6-trimethoxyphenyl)methylthio)ethyl}-1,3-oxazolidin-2-one; 2-aAmino-3-methyl-3-((2,4,6-trimethoxyphenyl)methylthio)butan-1-ol; 4-(1-methyl-1-(nitrosothio)ethyl)-1,3-oxazolidin-2-one; or pharmaceutically acceptable salts thereof. The compositions of the invention can further comprise at least one penetration enhancer, 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 vasoactive agent.

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    主要参考文献


    1: Heupler FA Jr, Proudfit WL, Razavi M, Shirey EK, Greenstreet R, Sheldon WC. Ergonovine maleate provocative test for coronary arterial spasm. Am J Cardiol. 1978 Apr;41(4):631-40. doi: 10.1016/0002-9149(78)90810-x. 25(1):1-2. doi: 10.1080/01443610400023429. 1(5695):563-4. doi: 10.1136/bmj.1.5695.563-c.
    4: Ergometrien of oksitosien? [Ergonovine or oxytocin?]. S Afr Med J. 1979 May 19;55(21):818. Afrikaans. 103(6):E30. doi: 10.1161/01.cir.103.6.e30. 59(1):82-9. doi: 10.1161/01.cir.59.1.82. 13(10):703-10. doi: 10.1002/clc.4960131006. 69(1):57-65. doi: 10.1016/j.jjcc.2016.09.012. Epub 2016 Nov 15. 27(1):43-6. doi: 10.1212/wnl.27.1.43. 6(3):217-23. doi: 10.1002/ccd.1810060302. 20(1):107-11. doi: 10.1016/0735-1097(92)90145-d. Erratum in: J Am Coll Cardiol 1993 Mar 1;21(3):848. 40(4):487-91. doi: 10.1016/0002-9149(77)90060-1. 29(6):366-7. doi: 10.1111/j.1526-4610.1989.hed2906366.x. 68(1):1-6. doi: 10.1016/j.jjcc.2016.03.005. Epub 2016 May 24. 17(3):269-77. doi: 10.1177/1933719109351934. Epub 2010 Feb 2. 11(1-2):147-9. doi: 10.1080/02791072.1979.10472099. 97(9):1322-5. doi: 10.1016/j.amjcard.2005.11.073. Epub 2006 Mar 20. 58(5):879-83. 47(9):798-803. French. doi: 10.1016/j.lpm.2018.08.004. Epub 2018 Sep 21. 19(2):243-56.

    合成参考文献


    摘要:JAMA, Journal of the American Medical Association., 250(729), 1983
    摘要:Toxicology and Applied Pharmacology., 23(537), 1972 []
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