4-hydroxy-3-(3'-hydroxymethylbiphenyl-4-yl)-5-phenyl-6,7-dihydro-thieno[2,3-b]pyridin-6-one | 1194091-49-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: 4-hydroxy-3-(3'-hydroxymethylbiphenyl-4-yl)-5-phenyl-6,7-dihydro-thieno[2,3-b]pyridin-6-one
• 英文别名: 4-hydroxy-3-[4-[3-(hydroxymethyl)phenyl]phenyl]-5-phenyl-7H-thieno[2,3-b]pyridin-6-one
• CAS: 1194091-49-0
• 化学式: C₂₆H₁₉NO₃S
• 分子量: 425.508
• InChiKey: GOSMRIZUTRINQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  97.8
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] MODULATEURS DU RÉCEPTEUR DE LA PROSTACYCLINE (PGI2) UTILES POUR LE TRAITEMENT DE TROUBLES LIÉS À CELUI-CI
  申请人：ARENA PHARM INC

  公开号：WO2009117095A1

  公开（公告）日：2009-09-24

  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).

  本发明涉及式（XIIIa）的酰胺衍生物及其药物组合物，其调节PGI2受体的活性。本发明的化合物和药物组合物适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、门脉高压、HIV感染、药物或毒素摄入、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；具有明显静脉或毛细血管受累的PAH；血小板聚集；冠状动脉疾病；心肌梗死；短暂性缺血发作；心绞痛；中风；缺血再灌注损伤；再狭窄；心房颤动；血栓形成在介入治疗或冠状动脉旁路手术个体中或患有心房颤动的个体中；动脉粥样硬化；动脉血栓形成；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；青光眼或眼内压异常的其他眼部疾病；高血压；炎症；牛皮癣；银屑病性关节炎；类风湿性关节炎；克罗恩病；移植排斥反应；多发性硬化；系统性红斑狼疮（SLE）；溃疡性结肠炎；缺血再灌注损伤；再狭窄；动脉粥样硬化；痤疮；1型糖尿病；2型糖尿病；败血症；慢性阻塞性肺疾病（COPD）。
• [EN] THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS<br/>[FR] DÉRIVÉS DE THIÉNOPYRIDONE COMME ACTIVATEURS DE LA PROTÉINE KINASE ACTIVÉE PAR L'AMP (AMPK)
  申请人：MERCK PATENT GMBH

  公开号：WO2009135580A1

  公开（公告）日：2009-11-12

  The present invention relates to compounds of formula (I) wherein R1, R2 and B1, B2 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).

  本发明涉及公式（I）中的化合物，其中R1、R2和B1、B2如权利要求1所定义，包括其药物组成物，并用于治疗和/或预防由AMP激动剂调节的疾病和紊乱。该发明还涉及中间体和公式（I）化合物的制备方法。
• MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2280696A1

  公开（公告）日：2011-02-09
• THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS
  申请人：Merck Patent GmbH

  公开号：EP2280952A1

  公开（公告）日：2011-02-09
• THIENOPYRIDONE DERIVATIVES AS AMP- ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS
  申请人：Cravo Daniel

  公开号：US20110060001A1

  公开（公告）日：2011-03-10

  The present invention relates to compounds of formula (I) wherein R 1 , R 2 and B 1 , B 2 are as defined in claim 1 , including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).