CAS: 112966-96-8; Domitroban

该化合物是一种属于非类类类非类类类抗炎药物的化学化合物,主要被承认为具有选择性的色波纳A2受体抗体敌异体作用,这意味着它抑制了Tromboxane A2的动作,一种涉及小板块聚合和血管收缩的复合体.这一特征使得Domitroban有可能有助于管理与心血管健康有关的条件,因为它可能有助于减少形成色波的风险.该化合物的特点主要是其中度溶解于有机溶剂和水溶解度有限,从而影响其生物利用率和药用.此外,Domitroban已经研究其抗炎特性,有助于其治疗潜力.与许多药品一样,了解其行动机制,功效和安全概况对于其在临床环境中的应用至关重要.继续进一步研究其生物效应和潜在治疗用途.

结构式图片

MSDS等安全信息

    上下游产品

    (1R,2S,3S,4S)-(3-Phenylsulfonylaminobicyclo<2.2.1>Hept-2-yl)Acetaldehyde 128299-81-0
    (1S,2S,3S,4R)-3-Carboxy-2-((Phenylsulfonyl)Amino)Bicyclo<2.2.1>Heptane 132747-46-7

    合成工艺路线路线简述

      📜4-羧丁基三苯基溴化膦置于氢氧化钾,Dimsylsodium,三乙胺体系中,用 甲醇,乙醚,二氯甲烷,二甲基亚砜 用作溶剂,化学反应生成多米曲班
      参考文献:新型血栓烷受体拮抗剂(+/-)-(5Z)-7-[3-内-[(苯磺酰基)氨基]双环[2.2.1]庚-2-外-的各种衍生物的合成及体外活性yl]庚烯酸.
      标题:新型血栓烷受体拮抗剂(+/-)-(5Z)-7-[3-内-[(苯磺酰基)氨基]双环[2.2.1]庚-2-外-的各种衍生物的合成及体外活性yl]庚烯酸.
      摘要:通过其甲基合成了(+/-)-(5Z)-7-(3-Endo-Aminobicyclo [2.2.1] Hept-2-Exo-Yl)庚烯酸(vi)的几种磺酰基衍生物(13A-T)酯10.用11A-T磺化10,然后皂化,得到13A-T.用大鼠洗涤的血小板(wp)和兔富含血小板的血浆(prp)测量相应的钠盐14A-T对血小板聚集的抑制浓度(ic50).还测量了某些衍生物对大鼠主动脉收缩的ic50值.对于带有芳基磺酰基残基的衍生物,大鼠wp的ic50值从2.9 Nm依次增加到14N,14C,14D和14B,具体取决于中间亚甲基的数量.甲基衍生物14E表现出比正己基衍生物14F更高的ic 50值.用对甲基,对氟-,或14A中的对氯基保留或略微降低其ic50值,而pn-戊基或对氧羰基则显着提高其ic50值.代表性的14A抑制(15S)-15-羟基-11,9-(环氧甲氧基)prosta-5(z),13(e
      Doi:10.1021/jm00117A028

      海关参考信息

      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:JP-2004500344-A
      优先权日:1999-10-29
      标 题 :Synthesis of endogenous nitric oxide under low oxygen partial pressure

      专利号:EP-1242068-A1
      优先权日:1999-10-29
      标 题:Endogenous nitric oxide synthesis under conditions of low oxygen tension

      专利号:AU-1342901-A
      优先权日:1999-10-29
      标 题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension

      专利号:WO-0132167-A1
      优先权日:1999-10-26
      标题:Endogenous nitric oxide synthesis under conditions of low oxygen tension

      专利号:CA-2386938-A1
      优先权日:1999-10-29
      标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension

      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: Ushikubi F, Nakajima M, Yamamoto M, Ohtsu K, Kimura Y, Okuma M, Uchino H, Fujiwara M, Narumiya S. [3H]S-145 and [125I]I-S-145-OH: new radioligands for platelet thromboxane A2 receptor with low nonspecific binding and high binding affinity for various receptor preparations. Eicosanoids. 1989;2(1):21-7.
      8: Otani K, Shima N, Doteuchi M. [Pharmacological actions of S-145, a novel thromboxane A2 antagonist, in various smooth muscles]. Nihon Yakurigaku Zasshi. 1989 Nov;94(5):319-28. Japanese.
      10: Yamaguchi Y, Baba T, Touchi A, Matsubara T. In vitro studies to elucidate the metabolic pathway of (+)-S-145, a thromboxane A2 receptor antagonist, in rats. Evidence for two independent pathways in peroxisomal beta-oxidation. Drug Metab Dispos. 1995 Nov;23(11):1195-201. Japanese. Japanese.

      合成参考文献


      摘要:S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560
      📝 需求与反馈
      尽可能描述清楚需求与问题信息
      ×

      通知