ethyl 5-[2-(4-chlorophenyl)-4-thiazolyl]-2-thienylcarboxylate | 254911-15-4

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: ethyl 5-[2-(4-chlorophenyl)-4-thiazolyl]-2-thienylcarboxylate
• 英文别名: Ethyl 5-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]thiophene-2-carboxylate
• CAS: 254911-15-4
• 化学式: C₁₆H₁₂ClNO₂S₂
• 分子量: 349.862
• InChiKey: IIEADTHWGNBGNS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  95.7
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• RETINOID-ASSOCIATED RECEPTOR REGULATORS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1092711A1

  公开（公告）日：2001-04-18

  A pharmaceutical composition of the invention which is a retinoid-related receptor function regulating agent comprising a 1,3-azole derivative represented by formula (I): wherein R1 is an aromatic hydrocarbon group or an aromatic heterocyclic group, each of which may be substituted; R2 is hydrogen or an optionally substituted hydrocarbon group; X is O, S or a group represented by the formula: -NR4- wherein R4 is hydrogen or an optionally substituted alkyl group; A is an aromatic hydrocarbon group or an aromatic heterocyclic group, each of which may be substituted; R3 is a group represented by the formula: -OR5 wherein R5 is hydrogen or an optionally substituted hydrocarbon group, or -NR6R7 wherein R6 and R7 are same or different and each is hydrogen or an optionally substituted hydrocarbon group, or R6 and R7 may be taken together with an adjacent nitrogen atom to form a ring, provided that compounds represented by the formulae: are excluded, or its salt, is low in toxicity, and can be employed, for instance, as an agent for preventing or treating diabetes (e.g., insulin-dependent diabetes, non-insulin-dependent diabetes, gestational diabetes), an agent for preventing or treating hyperlipidemia (e.g., hypertriglyceridemia, hypercholesterolemia, hypo-HDL-cholesterolemia), an insulin sensitivity enhancing agent, an insulin resistance improving agent, an agent for preventing or treating impaired glucose tolerance (IGT), and an agent for preventing transition from impaired glucose tolerance to diabetes. Further, a pharmaceutical composition of the invention can be used, for instance, as an agent for preventing or treating diabetic complications (e.g., neuropathy, nephropathy, retinopathy, cataract, macroangiopathy, osteopenia), obesity, osteoporosis, cachexia (e.g., carcinomatous cachexia, tuberculous cachexia, diabetic cachexia, hemopathic cachexia, endocrinopathic cachexia, infectious cachexia or cachexia induced by acquired immunodeficiency syndrome), fatty liver, hypertension, polycystic ovary syndrome, renal diseases (e.g., diabetic nephropathy, glomerular nephritis, glomerulosclerosis, nephrotic syndrome, hypertensive nephrosclerosis, terminal renal disorder), muscular dystrophy, myocardiac infarction, angina pectoris, cerebral infarction, insulin resistant syndrome, syndrome X, hyperinsulinemia-induced sensory disorder, tumor (e.g., leukemia, breast cancer, prostate cancer, skin cancer), arteriosclerosis (e.g., atherosclerosis) and as a pharmaceutical for controlling appetite or food intake.

  本发明的一种药物组合物是一种视黄酸相关受体功能调节剂，由式（I）代表的 1，3-唑衍生物组成： 其中 R1 是芳香烃基团或芳香杂环基团，每个基团均可被取代； R2 是氢或任选取代的烃基团； X 是 O、S 或由式表示的基团：-其中 R4 是氢或任选取代的烷基；A 是芳香烃基团或芳香杂环基团，其中每个基团均可被取代；R3 是由式表示的基团：-OR5，其中 R5 为氢或任选取代的烃基，或-NR6R7，其中 R6 和 R7 相同或不同，且各自为氢或任选取代的烃基，或 R6 和 R7 可与相邻的氮原子一起形成环，条件是由式表示的化合物： 或其盐的毒性低，可用作预防或治疗糖尿病（如胰岛素依赖型糖尿病、非胰岛素依赖型糖尿病、妊娠糖尿病）的制剂、预防或治疗高脂血症（如高甘油三酯血症、高胆固醇血症、高胆固醇血症）的制剂等、高甘油三酯血症、高胆固醇血症、低 HDL-胆固醇血症）的制剂，提高胰岛素敏感性的制剂，改善胰岛素抵抗的制剂，预防或治疗糖耐量受损（IGT）的制剂，以及预防从糖耐量受损转变为糖尿病的制剂。 此外，本发明的药物组合物还可用作预防或治疗糖尿病并发症（如神经病变、肾病变、视网膜病变、白内障、大血管病变、骨质疏松）、肥胖症、骨质疏松症、恶病质（如癌性恶病质、结核性恶病质）等的药物、癌症性恶病质、结核性恶病质、糖尿病性恶病质、血液病性恶病质、内分泌病性恶病质、感染性恶病质或获得性免疫缺陷综合征诱发的恶病质）、脂肪肝、高血压、多囊卵巢综合征、肾病（如糖尿病肾病、肾小球肾炎、肾小球硬化症、肾病综合征、高血压肾硬化症、终末期肾功能紊乱）、肌肉萎缩症、心肌梗塞、心绞痛、脑梗塞、胰岛素抵抗综合征、X 综合征、高胰岛素血症诱发的感觉障碍、肿瘤（如白血病、乳腺癌、前列腺癌）、白血病、乳腺癌、前列腺癌、皮肤癌）、动脉硬化（如动脉粥样硬化）以及控制食欲或食物摄入量的药物。
• US6545009B1
  申请人：——

  公开号：US6545009B1

  公开（公告）日：2003-04-08