(E)-6-[3-[1-[(4-iodophenyl)sulfonylamino]-2-methylpropan-2-yl]phenyl]-6-pyridin-3-ylhex-5-enoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (E)-6-[3-[1-[(4-iodophenyl)sulfonylamino]-2-methylpropan-2-yl]phenyl]-6-pyridin-3-ylhex-5-enoic acid
• 化学式: C₂₇H₂₉IN₂O₄S
• 分子量: 604.5
• InChiKey: JILQVWNDRFJPRF-KIBLKLHPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  35
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• 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。
• METHODS FOR THE TREATMENT AND DIAGNOSIS OF BONE MINERAL DENSITY RELATED DISEASES
  申请人：INSERM - Institut National de la Santé et de la Recherche Médicale

  公开号：EP2227560B1

  公开（公告）日：2017-10-18
• Methods for the Treatment and Diagnosis of Bone Mineral Density Related Diseases
  申请人：Cormier-Daire Valerie

  公开号：US20100284991A1

  公开（公告）日：2010-11-11

  The present invention relates to methods of the treatment and diagnosis of bone mineral density related disorders. More particularly, the present invention relates to a method of diagnosing or predicting a bone mineral density related disease, or a risk of a bone mineral density related disease, in a subject, which method comprises detecting a mutation in the TBXAS1 gene, wherein the presence of said mutation is indicative of a bone mineral density related disease or of a risk of a bone mineral density related disease. The invention also relates to a compound selected in the group consisting of a thromboxane synthase (TXAS) encoding polynucleotide, a TXAS, thromboxane A2 or an analog thereof for treating or preventing a disease associated with an increased bone mineral density (e.g., Ghosal hematodiaphyseal dysplasia syndrome). The invention also relates to a compound selected from the group consisting of an inhibitor of TBXAS1 gene expression or a thromboxane inhibitor for treating or preventing a disease associated with a decreased bone mineral density (e.g., osteoporosis).
• US9834820B2
  申请人：——

  公开号：US9834820B2

  公开（公告）日：2017-12-05