CAS: 37762-06-4; 5-(2-Propoxyphenyl)-1H-[1,2,3]Triazolo[4,5-D]Pyrimidin-7(4H)-One

该化合物是一种化学化合物,其作用是选择性抑制5型磷酸酯(PDE5),它是一种酶,打破了环氨酸单磷酸酯(cGMP),通过抑制这种酶,Zaprinest提高了CGMP的水平,导致血管变异和血液流动增加,特别是在肺部和系统循环中.这种特性使它对治疗肺高血压等条件感兴趣.Zaprinast的特征是其分子结构,包括一个火药环和一个硝基,有助于其生物活动.该化合物通常在研究环境中进行,研究其对血管滑动肌肉放松和其他生理过程的影响.此外,Zaprinast还因其潜在的...

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

    📜5,6-二氨基-2-(2-丙氧苯基)-4(1H)-嘧啶酮,Sodium Nitrite 以70%的收率获得
    参考文献:Broughton B. J.; Chaplen P.; Knowles P.; Lunt E.; Marshall S. M.; Pain D.+,J. Med. Chem.,1975,18,No 11,1117-1122
    标题:Broughton B. J.; Chaplen P.; Knowles P.; Lunt E.; Marshall S. M.; Pain D.+,J. Med. Chem.,1975,18,No 11,1117-1122

    海关参考信息

    专利信息


    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    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-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-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.

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    主要参考文献


    1: Kang X, Xie Z, Yang Y, Wu L, Xu H, Zhang S, Liang Y, Wu X. Hippocampal GPR35 is involved in the depression-like behaviors induced by inflammation and mediates the antidepressant effects of fluoxetine in mice. Brain Behav Immun. 2025 Feb 18;126:189-213. doi: 10.1016/j.bbi.2025.02.010. Epub ahead of print.
    149:114192. doi: 10.1016/j.intimp.2025.114192. Epub 2025 Feb 3. 166(3):596-613. doi: 10.1097/j.pain.0000000000003399. Epub 2024 Oct 3.
    4: Oka M, Akaki S, Ohno O, Terasaki M, Hamaoka-Tamura Y, Saito M, Kato S, Inoue A, Aoki J, Matsuno K, Furuta K, Tanaka S. Suppression of Mast Cell Activation by GPR35: GPR35 Is a Primary Target of Disodium Cromoglycate. J Pharmacol Exp Ther. 2024 Mar 15;389(1):76-86. doi: 10.1124/jpet.123.002024. 102(3):218-227. doi: 10.1139/cjpp-2023-0314. Epub 2023 Nov 17. 1867(12):130492. doi: 10.1016/j.bbagen.2023.130492. Epub 2023 Oct 21. 5-HIAA serotonin metabolite becomes a ligand. Arch Pharm Res. 2023 Jun;46(6):550-563. doi: 10.1007/s12272-023-01449-y. Epub 2023 May 25.

    合成参考文献


    参考文献:10.3389/fnsys.2011.00055
    摘要:West AR, Tseng KY. Nitric Oxide-Soluble Guanylyl Cyclase-Cyclic GMP Signaling in the Striatum: New Targets for the Treatment of Parkinson's Disease Front Syst Neurosci. 2011;5():55.
    参考文献:10.1007/s10822-011-9458-5
    摘要:Howard BL, Thompson PE, Manallack DT. Active site similarity between human and Plasmodium falciparum phosphodiesterases: considerations for antimalarial drug design. Journal of Computer-Aided Molecular Design. 2011 Jul 16;25(8):753. doi: 10.1007/s10822-011-9458-5.
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