(Z)-7-[3-(benzenesulfonamido)-2-bicyclo[2.2.1]heptanyl]hept-5-enoic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: (Z)-7-[3-(benzenesulfonamido)-2-bicyclo[2.2.1]heptanyl]hept-5-enoic acid
• 化学式: C₂₀H₂₇NO₄S
• 分子量: 377.505
• InChiKey: PWTCIBWRMQFJBC-BHQIHCQQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  26
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  91.8
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Use of a thromboxane A2 receptor antagonist for the manufacture of a medicament for the treatment of ulcerative gastrointestinal conditions
  申请人：E.R. SQUIBB & SONS, INC.

  公开号：EP0448274A2

  公开（公告）日：1991-09-25

  A method is provided for protecting against and/or treating ulcerative gastrointestinal conditions, including anti-inflammatory drug-induced gastrointestinal ulcers, using a thromboxane A₂ receptor antagonist. In addition, a combination is provided which includes a thromboxane A₂ receptor antagonist and an anti-inflammatory agent which combination may be used to treat inflammatory conditions, such as arthritis, while inhibiting formation of and/or treating gastrointestinal ulcers.

  本发明提供了一种使用血栓素 A₂受体拮抗剂防止和/或治疗胃肠道溃疡病的方法，包括抗炎药物诱发的胃肠道溃疡。此外，还提供了一种组合物，其中包括血栓素 A₂受体拮抗剂和一种消炎药，该组合物可用于治疗关节炎等炎症，同时抑制胃肠道溃疡的形成和/或治疗胃肠道溃疡。
• Sulfonylamino substituted bicyclyl hydroxamic acid derivatives
  申请人：SHIONOGI SEIYAKU KABUSHIKI KAISHA trading under the name of SHIONOGI & CO. LTD.

  公开号：EP0453960A1

  公开（公告）日：1991-10-30

  Sulfonylamino substituted bicyclyl hydroxamic acid derivatives of the formula: wherein R¹ and R² each is hydrogen or lower alkyl; R³ is hydrogen, lower alkyl, lower alkoxy, hydroxy or halogen; X is alkylene or alkenylene; Y is methylene or oxygen; and n is 0, 1, or 2 or the pharmaceutically acceptable salt thereof. These compounds have an advanced antagonistic activity to thromboxane A₂ (TXA₂)-receptor and are useful for the treatment of thrombosis, vasoconstriction, or bronchoconstriction, and the like disease which are induced by TXA₂.

  式中磺酰胺取代的双烯丙基羟肟酸衍生物： 其中 R¹ 和 R² 均为氢或低级烷基；R³ 为氢、低级烷基、低级烷氧基、羟基或卤素；X 为亚烷基或烯基；Y 为亚甲基或氧；n 为 0、1 或 2 或其药学上可接受的盐。这些化合物对血栓素 A₂（TXA₂）受体具有高级拮抗活性，可用于治疗由 TXA₂诱导的血栓形成、血管收缩或支气管收缩等疾病。
• Thromboxane inhibitors, compositions and methods of use
  申请人：——

  公开号：US20030050305A1

  公开（公告）日：2003-03-13

  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.

  本发明描述了治疗或预防男性和女性性功能障碍以及增强男性和女性性反应的方法，其方法是施用治疗有效量的至少一种血栓素抑制剂，以及可选的至少一种能捐献、转移或释放一氧化氮、提高内皮源性松弛因子的内源性水平、刺激一氧化氮的内源性合成或一氧化氮合酶底物的化合物和/或至少一种血管活性剂。男性或女性最好患有糖尿病。本发明还提供了新型组合物，其中包含至少一种血栓素抑制剂，以及至少一种能捐献、转移或释放一氧化氮、提高内皮源性松弛因子的内源性水平、刺激一氧化氮的内源性合成或作为一氧化氮合酶底物的化合物、以及至少一种治疗剂，如血管活性剂、非甾体抗炎化合物（NSAIDs）、选择性环氧化酶-2（COX-2）抑制剂、抗凝剂、血管紧张素转换酶（ACE）抑制剂、血管紧张素 II 受体拮抗剂、肾素抑制剂及其混合物。本发明还提供了治疗或预防缺血性心脏疾病、心肌梗塞、心绞痛、中风、偏头痛、脑出血、心脏病死亡、短暂性脑缺血发作、器官移植后并发症、冠状动脉搭桥术、血管成形术、动脉内膜切除术、动脉粥样硬化、肺栓塞、支气管哮喘、支气管炎、肺炎、各种器官的循环休克、肾衰竭、心肌梗塞、心绞痛、中风、偏头痛、脑出血、心肌梗塞、血管成形术、动脉内膜切除术、冠状动脉搭桥术、血管成形术、动脉内膜切除术、动脉粥样硬化、肺栓塞、支气管哮喘、支气管炎、肺炎的方法、各种器官的循环休克、肾炎、移植物排斥反应、癌症转移、妊娠高血压、子痫前期、子痫、血栓和血栓栓塞性疾病、宫内发育、胃肠功能紊乱、肾病和肾功能紊乱、尿酸水平升高引起的疾病和痛经，以及用于抑制血小板聚集或血小板粘附或松弛平滑肌。
• Novel combination of an ADP-receptor blocking antiplatelet drug and a thromboxane A2 receptor antagonist and a method for inhibiting thrombus formation employing such combination
  申请人：——

  公开号：US20030109543A1

  公开（公告）日：2003-06-12

  A method is provided for inhibiting platelet aggregation and thrombus formation by administering to a patient an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with a thromboxane A 2 receptor antagonist, such as ifetroban, and optionally a cholesterol lowering drug, such as an HMG CoA reductase inhibitor, for example, pravastatin.

  本发明提供了一种抑制血小板聚集和血栓形成的方法，通过向患者施用 ADP 受体阻断抗血小板药物（如氯吡格雷）与血栓素 A 2 受体拮抗剂，如依弗曲班，以及可选的降胆固醇药物，如 HMG CoA 还原酶抑制剂，如普伐他汀，从而抑制血小板聚集和血栓形成。
• ENDOGENOUS NITRIC OXIDE SYNTHESIS UNDER CONDITIONS OF LOW OXYGEN TENSION
  申请人：Nitromed, Inc.

  公开号：EP1242068A1

  公开（公告）日：2002-09-25