CAS: 32828-81-2; 4-Methoxy-N1,N3-Bis(Pyridin-3-Ylmethyl)Isophthalamide

该化合物是一种双作用的抗板剂,它既可以作为tromboxane A2合成酶抑制剂,又可以作为tromboxane A2受体抗体抗体. 这种双机制有效地减少了板块聚集,使其在管理血栓性疾病方面有用.它同时堵塞tromboxane A2的生产和受体结合的能力增强了它的抗血栓性功效,同时有可能最大限度地减少与单管抑制相关的副作用. 皮卡坦米德因其有利的药用动力特征而特别引人注目,包括可以预测的生物利用率和平衡的行动持续时间. 它的化学稳定性和特性使它成为心血管治疗临床和研究应用的可靠选择.

结构式图片

合成工艺路线路线简述

  • 合成目标产物 Picotamide 主要起始原料 3-(Aminomethyl)Pyridine And 4-Methoxyisophthaloyl Dichloride
  • (文献来源)合成步骤主要原料 3-(Aminomethyl)Pyridine 和 4-Methoxyisophthaloyl Dichloride
📜4-羟基间苯二甲酸二甲酯置于氯化亚砜,水,四丁基碘化铵,铁粉,Potassium Carbonate,Sodium Hydroxide体系中,用 N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 12.5H,反应生成 匹考他胺
参考文献:吡考他胺的制备方法
标题:吡考他胺的制备方法
摘要:本发明提供一种制备吡考他胺的方法,所述方法包括:以4‑羟基间苯二甲酸二甲酯为原料,经甲醚化反应得到4‑甲氧基间苯二甲酸二甲酯;再经水解反应得到4‑甲氧基间苯二甲酸;最后酰胺化反应得到吡考他胺.和传统方法相比,本发明的制备方法具有合成步骤短,操作简便,反应快,收率高等优点.另外,本发明所需的原料是从工业生产产生的废渣中提取的,提取方法简单,提高了资源利用率,减少了环境污染,降低了生产成本,适合大规模工业生产.

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-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-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-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:AU-2007308022-A2
优先权日:2006-10-05
标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:AU-2007308022-A1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Celestini A, Violi F. A review of picotamide in the reduction of cardiovascular events in diabetic patients. Vasc Health Risk Manag. 2007;3(1):93-8.
2: Hennenberg M, Tamalunas A, Wang Y, Keller P, Schott M, Strittmatter F, Herlemann A, Yu Q, Rutz B, Ciotkowska A, Stief CG, Gratzke C. Inhibition of agonist-induced smooth muscle contraction by picotamide in the male human lower urinary tract outflow region. Eur J Pharmacol. 2017 May 15;803:39-47. doi: 10.1016/j.ejphar.2017.03.022. Epub 2017 Mar 14. 305(10):F1383-90. doi: 10.1152/ajprenal.00380.2013. Epub 2013 Sep 18. 25 Suppl
3:S267-9. doi: 10.1007/s10072-004-0304-6. Drug Evaluation in Atherosclerotic Vascular Disease in Diabetics (DAVID) Study Group. Picotamide, a combined inhibitor of thromboxane A2 synthase and receptor, reduces 2-year mortality in diabetics with peripheral arterial disease: the DAVID study. Eur Heart J. 2004 Oct;25(20):1845-52. doi: 10.1016/j.ehj.2004.07.013. 24(3):311-5. doi: 10.1177/030006059602400312. 87(5):1563-9. doi: 10.1161/01.cir.87.5.1563. 85(3):207-15. doi: 10.1016/s0049-3848(97)00005-4. 33(6):599-602. doi: 10.1007/BF00542494. 355(1):77-83. doi: 10.1016/s0014-2999(98)00467-1. 42(1):178-82. doi: 10.2337/diab.42.1.178. 21(8):78. doi: 10.1007/s11886-019-1168-y. 64(1):80-6. 78(5):1385-91. 133(4):233-7. Italian. 10(3):315-20. doi: 10.1111/j.0953-0673.1996.00315.x. 62(6):717-24. doi: 10.1016/0049-3848(91)90375-7. 10(2):91-8. 2(4):292-5. doi: 10.1177/1358863X9700200403.

合成参考文献


参考文献:10.1155/2011/250518
摘要:Tufano A, Cimino E, Di Minno MND, Ieranò P, Marrone E, Strazzullo A, Di Minno G, Cerbone AM. Diabetes Mellitus and Cardiovascular Prevention: The Role and the Limitations of Currently Available Antiplatelet Drugs. International Journal of Vascular Medicine. 2011;2011():1–5. doi: 10.1155/2011/250518.
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