N-[3,5-dichloro-4-(3-cyclobutylmethanesulfonyl-4-hydroxy-phenoxy)-phenyl]-oxamic acid ethyl ester | 290352-02-2

• 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: N-[3,5-dichloro-4-(3-cyclobutylmethanesulfonyl-4-hydroxy-phenoxy)-phenyl]-oxamic acid ethyl ester
• 英文别名: Ethyl 2-[[3,5-dichloro-4-[3-[(cyclobutylmethyl)sulfonyl]-4-hydroxyphenoxy]phenyl]amino]-2-oxoacetate；ethyl 2-[3,5-dichloro-4-[3-(cyclobutylmethylsulfonyl)-4-hydroxyphenoxy]anilino]-2-oxoacetate
• CAS: 290352-02-2
• 化学式: C₂₁H₂₁Cl₂NO₇S
• 分子量: 502.372
• InChiKey: UYRPOZMJJYOMQF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  127
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Thyromimetic organic compounds
  申请人：——

  公开号：US20020045751A1

  公开（公告）日：2002-04-18

  Compounds of the present invention of the formula 1 are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals. The compounds of the invention can therefore be used for the prevention and/or treatment of occlusive cardiovascular conditions in which hyperlipidemia and hyperlipoproteinemia are implicated, such as atherosclerosis and coronary heart disease in mammals.

  本发明的化合物具有以下公式的甲型甲状腺模拟剂，可用于预防和/或治疗与甲状腺激素失衡相关的疾病，如甲状腺功能减退和亢进、肥胖、骨质疏松症和抑郁症。本发明的化合物特别是降脂剂，可增强胆固醇从循环中的清除，特别是以低密度脂蛋白（LDL）形式的胆固醇的清除。这些化合物可用于减少哺乳动物的总胆固醇血浆水平，特别是减少LDL胆固醇水平。此外，这些化合物还可以降低哺乳动物体内独立的心血管风险因子脂蛋白（a）[Lp(a)]水平。因此，本发明的化合物可用于预防和/或治疗与高脂血症和高脂蛋白血症有关的闭塞性心血管疾病，如动脉粥样硬化和冠心病等。
• Oxamic acids and derivatives as thyroid receptor ligands
  申请人：——

  公开号：US20030114521A1

  公开（公告）日：2003-06-19

  The present invention provides novel compounds of the Formula 1 and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R 1 —R 8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

  本发明提供了式1的新化合物及其前药、几何和光学异构体以及这些化合物、前药和异构体的药学上可接受的盐，其中R1-R8和W如本文所述。还提供了含有这些化合物、前药、异构体或其药学上可接受的盐的药物组合物，以及用于治疗肥胖症、高脂血症、青光眼、心律失常、皮肤疾病、甲状腺疾病、甲状腺功能减退症以及相关的疾病和疾病，如糖尿病、动脉硬化、高血压、冠心病、高胆固醇血症、抑郁症和骨质疏松症的方法、药物组合物和工具包。
• OXAMIC ACIDS AND DERIVATIVES AS THYROID RECEPTOR LIGANDS
  申请人：Pfizer Products Inc.

  公开号：EP1157001A1

  公开（公告）日：2001-11-28
• US6326398B1
  申请人：——

  公开号：US6326398B1

  公开（公告）日：2001-12-04
• US6545018B2
  申请人：——

  公开号：US6545018B2

  公开（公告）日：2003-04-08