4-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-benzenesulfonic acid sodium salt | 532958-72-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-benzenesulfonic acid sodium salt
• 英文别名: 4-(5-Methyl-2-phenyloxazol-4-ylmethoxy)-benzenesulfonic acid sodium salt；sodium;4-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]benzenesulfonate
• CAS: 532958-72-8
• 化学式: C₁₇H₁₄NO₅S*Na
• 分子量: 367.358
• InChiKey: HUTKNQABCYMBQT-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  0.14
• 重原子数：
  25
• 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：
  101
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-benzenesulfonic acid sodium salt 在 氯化亚砜 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 3.33h， 生成 4-(5-甲基-2-苯基-噁唑-4-基甲氧基)-苯磺酰氯
  参考文献：
  名称：

  [EN] ORGANIC COMPOUNDS
  [FR] COMPOSES ORGANIQUES

  摘要：

  (I)式化合物提供与过氧化物酶体增殖物激活受体（PPARs）结合的药理剂。因此，本发明的化合物对于治疗哺乳动物中由PPAR受体活性介导的疾病是有用的。这些疾病包括脂质代谢异常、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病（IBDs）、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用，用于治疗和预防与糖耐量受损、高血糖和胰岛素抵抗有关的疾病，如1型和2型糖尿病以及X综合征。

  公开号：

  WO2005026134A1
• 作为产物：
  描述：

  disodiumphenolsulfonate 、 4-(氯甲基)-5-甲基-2-苯基-1,3-恶唑 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 18.0h， 生成 4-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-benzenesulfonic acid sodium salt
  参考文献：
  名称：

  [EN] ORGANIC COMPOUNDS
  [FR] COMPOSES ORGANIQUES

  摘要：

  (I)式化合物提供与过氧化物酶体增殖物激活受体（PPARs）结合的药理剂。因此，本发明的化合物对于治疗哺乳动物中由PPAR受体活性介导的疾病是有用的。这些疾病包括脂质代谢异常、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病（IBDs）、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用，用于治疗和预防与糖耐量受损、高血糖和胰岛素抵抗有关的疾病，如1型和2型糖尿病以及X综合征。

  公开号：

  WO2005026134A1

文献信息

• [EN] HETEROCYCLIC COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSES HETEROCYCLIQUES ET PROCEDES D'UTILISATION
  申请人：NOVARTIS AG

  公开号：WO2003043985A1

  公开（公告）日：2003-05-30

  Compounds of the formula (I) provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARa and PPARy receptors.

  式(I)的化合物是有效的过氧化物酶体增殖物激活受体（PPARs）激动剂，具有药理学作用。因此，本发明的化合物可用于治疗哺乳动物中由PPAR受体活性介导的疾病。这些疾病包括血脂异常、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病、溃疡性结肠炎和克罗恩病等。本发明的化合物特别适用于哺乳动物中作为降糖药物，用于治疗和预防因糖耐量受损、高血糖和胰岛素抵抗引起的疾病，如1型和2型糖尿病以及X综合征。本发明的化合物中，PPARa和PPARy受体的双重激动剂是首选的。
• Heterocyclic compounds and methods of use
  申请人：——

  公开号：US20040248936A1

  公开（公告）日：2004-12-09

  Compounds of the formula 1 provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPAR&agr; and PPAR&ggr; receptors.

  式1的化合物提供了具有强效 Peroxisome Proliferator-Activated Receptors（PPARs）激动剂作用的药理剂。因此，本发明的化合物对哺乳动物体内由 PPAR 受体活性介导的疾病的治疗具有用处。这些疾病包括：血脂异常、高脂血症、高胆固醇血症、动脉硬化、高三酰甘油血症、心力衰竭、心肌梗塞、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物体内特别有用，作为降血糖剂，用于治疗和预防与糖耐量受损、高血糖和胰岛素抵抗有关的疾病，如1型和2型糖尿病以及X综合征。本发明的优选化合物是 PPAR&agr; 和 PPAR&ggr; 双重激动剂。
• HETEROCYCLIC COMPOUNDS AND METHODS OF USE
  申请人：Bach Thomas Andrew

  公开号：US20070135502A1

  公开（公告）日：2007-06-14

  Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.

  该公式化合物提供了对过氧化物酶体增殖物激活受体（PPARs）具有强效激动剂作用的药理制剂。因此，本发明的化合物对于治疗哺乳动物PPAR受体活性介导的疾病是有用的。这些疾病包括：血脂异常、高血脂、高胆固醇血症、动脉粥样硬化、高三酰甘油血症、心力衰竭、心肌梗塞、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸道疾病、眼科疾病、炎症性肠病、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用，用于治疗和预防出现受损的葡萄糖耐受性、高血糖和胰岛素抵抗的疾病，例如1型和2型糖尿病和X综合症。本发明的化合物中，对于同时激活PPARα和PPARγ受体的双重激动剂，更为优选。
• Organic compounds
  申请人：Damon Edson Robert

  公开号：US20070004704A1

  公开（公告）日：2007-01-04

  Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

  本发明的化合物具有以下公式，可提供与过氧化物酶体增殖物激活受体（PPARs）结合的药理剂。因此，本发明的化合物对于治疗哺乳动物中由PPAR受体活性介导的疾病是有用的。这些疾病包括失调脂质代谢、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖症、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼部疾病、炎症性肠病（IBD）、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖药物特别有用，用于治疗和预防因受损葡萄糖耐受性、高血糖和胰岛素抵抗而引起的疾病，例如1型和2型糖尿病以及X综合症。
• Organic Compounds
  申请人：Damon Robert Edson

  公开号：US20100152255A1

  公开（公告）日：2010-06-17

  Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

  公式化合物提供了与过氧化物酶体增殖物激活受体（PPARs）结合的药理剂。因此，本发明的化合物对于治疗哺乳动物中PPAR受体活性介导的疾病是有用的。这些疾病包括失调脂质代谢症、高脂血症、高胆固醇血症、动脉硬化、高三酰甘油血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖症、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病（IBDs）、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用，用于治疗和预防因糖耐量受损、高血糖和胰岛素抵抗而引起的疾病，例如1型和2型糖尿病和X综合症。