2-[[3-[[(3-Fluorophenyl)-(3-methylphenyl)carbamoyl]oxymethyl]cyclohexyl]methoxy]acetic 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: 2-[[3-[[(3-Fluorophenyl)-(3-methylphenyl)carbamoyl]oxymethyl]cyclohexyl]methoxy]acetic acid
• 英文别名: 2-[[3-[[(3-fluorophenyl)-(3-methylphenyl)carbamoyl]oxymethyl]cyclohexyl]methoxy]acetic acid
• 化学式: C₂₄H₂₈FNO₅
• 分子量: 429.5
• InChiKey: OZDRAVOEJMFIRN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  31
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Modulators of the prostacyclin (PG12) receptor useful for the treatment of disorders related thereto
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2857015A1

  公开（公告）日：2015-04-08

  The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

  本发明涉及可调节 PGI2 受体活性的式 (XIIIa) 酰胺衍生物及其药物组合物。 本发明的化合物及其药物组合物用于治疗以下疾病的方法：肺动脉高压 (PAH)；特发性 PAH；家族性 PAH；与胶原血管疾病、先天性心脏病、门静脉高压、HIV 感染、摄入药物或毒素、遗传性出血性毛细血管扩张症、脾切除术、肺静脉闭塞性疾病 (PVOD) 或肺毛细血管血管瘤病 (PCH) 相关的 PAH；严重累及静脉或毛细血管的 PAH；血小板聚集；冠状动脉疾病；心肌梗塞；短暂性脑缺血发作；心绞痛；中风；缺血再灌注损伤；再狭窄；心房颤动；血管成形术或冠状动脉搭桥术患者或心房颤动患者血栓形成；动脉粥样硬化；动脉粥样硬化性血栓形成；哮喘或其症状；糖尿病相关疾病，如糖尿病周围神经病变、糖尿病肾病或糖尿病视网膜病变；青光眼或其他眼内压异常的眼部疾病；高血压；炎症；银屑病；银屑病关节炎；类风湿性关节炎、克罗恩病、移植排斥反应、多发性硬化症、系统性红斑狼疮 (SLE)、溃疡性结肠炎、缺血再灌注损伤、血管再狭窄、动脉粥样硬化、痤疮、1 型糖尿病、2 型糖尿病、败血症和慢性阻塞性肺病 (COPD)。
• MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2280696B1

  公开（公告）日：2014-09-17