3-isopropoxy-5,5-dimethyl-4-(4-(methylsulfonyl)phenyl)-2,5-dihydrofuran-2-ol | 190966-25-7

• 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: 3-isopropoxy-5,5-dimethyl-4-(4-(methylsulfonyl)phenyl)-2,5-dihydrofuran-2-ol
• 英文别名: 5,5-dimethyl-4-(4-methylsulfonylphenyl)-3-propan-2-yloxy-2H-furan-2-ol
• CAS: 190966-25-7
• 化学式: C₁₆H₂₂O₅S
• 分子量: 326.414
• InChiKey: ZUCJKEXQVGBQCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Combination therapy using COX-2 selective inhibitor and thromboxane inhibitor and compositions therefor
  申请人：——

  公开号：US20020016342A1

  公开（公告）日：2002-02-07

  The present invention provides a method for the treatment or prophylaxis of COX-2-mediated conditions in patients who are at risk of developing thromboembolic events which comprises administering to said patient a therapeutically or prophylactically effective amount of a COX-2 selective inhibitor and a cardiovascular protective amount of a thromboxane inhibitor, as well as compositions therefor.

  本发明提供了一种治疗或预防COX-2介导的病症的方法，适用于有发生血栓栓塞事件风险的患者，包括向该患者施用治疗或预防有效量的COX-2选择性抑制剂和心血管保护量的血栓素抑制剂，以及相应的组合物。
• Methods for treating or reducing the risk of pain and inflammatory disorders by administering inhibitors of activated thrombin activatable fibrinolysis inhibitor
  申请人：——

  公开号：US20030035795A1

  公开（公告）日：2003-02-20

  The invention includes methods for treating or reducing the risk of inflammation in a patient which comprises treating the patient with an inhibitor of activated thrombin activatable fibrinolysis inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. The invention includes methods for treating or reducing the risk of pain in a patient which comprises treating the patient with an inhibitor of activated thrombin activatable fibrinolysis inhibitor. In one class of these methods, the inhibitor of activated thrombin activatable fibrinolysis inhibitor is selected from the group consisting of 2-(6-amino-pyridin-3-ylmethyl)-3-butyl-succinic acid, 2-(6-amino-pyridin-3-ylmethyl)-3-phenethyl-succinic acid, 2-(6-amino-pyridin-3-ylmethyl)-3-methyl-succinic acid, 2-(6-amino-5-methyl-pyridin-3-ylmethyl)-3-[(1-benzyloxycarbonylamino-2-methyl-propyl)hydroxy-phosphinoyl]-propionic acid, 2-(6-amino-pyridin-3-ylmethyl)-3-[hydroxy-(3-phenyl-propyl)-phosphinoyl]-propionic acid, 2-(amino-pyridin-3-ylmethyl)-N-hydroxy-succinamic acid, 3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-propionic acid, 2-(2-amino-pyridin-4-ylmethyl)-3-mercapto-propionic acid, 2-(6-amino-pyridin-3-ylmethyl)-2-mercaptomethyl-butyric acid, 3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid, 3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid, 3-(6-amino-4-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid, and 3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-butyric acid or a pharmaceutically acceptable salt thereof. The invention is also a method for treating or reducing the risk of inflammation in a patient, or treating or reducing the risk of pain, which comprises treating the patient with a composition comprising an inhibitor of activated thrombin activatable fibrinolysis inhibitor and an NSAID, e.g., a COX-2 inhibitor. Such diseases include but are not limited to nephritis, systemic lupus, erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis.

  该发明涉及治疗或减少患者炎症风险的方法，包括使用活化凝血酶活化的纤溶抑制剂治疗患者。这些疾病包括但不限于肾炎、系统性红斑狼疮、类风湿关节炎、肾小球肾炎和结节病。该发明还涉及治疗或减少患者疼痛风险的方法，包括使用活化凝血酶活化的纤溶抑制剂治疗患者。在这些方法的一类中，活化凝血酶活化的纤溶抑制剂选择自2-(6-氨基吡啶-3-基甲基)-3-丁基琥珀酸、2-(6-氨基吡啶-3-基甲基)-3-苯乙基琥珀酸、2-(6-氨基吡啶-3-基甲基)-3-甲基琥珀酸、2-(6-氨基-5-甲基吡啶-3-基甲基)-3-[(1-苄氧羰基氨基-2-甲基-丙基)羟基磷酰基]-丙酸、2-(6-氨基吡啶-3-基甲基)-3-[羟基-(3-苯基-丙基)-磷酰基]-丙酸、2-(氨基吡啶-3-基甲基)-N-羟基琥酰胺酸、3-(6-氨基吡啶-3-基)-2-巯基甲基丙酸、2-(2-氨基吡啶-4-基甲基)-3-巯基丙酸、2-(6-氨基吡啶-3-基甲基)-2-巯基甲基丁酸、3-(6-氨基-5-甲基吡啶-3-基)-2-巯基甲基-2-甲基丙酸、3-(6-氨基-5-甲基吡啶-3-基)-2-巯基甲基丙酸、3-(6-氨基-4-甲基吡啶-3-基)-2-巯基甲基丙酸和3-(6-氨基吡啶-3-基)-2-巯基甲基丁酸或其药学上可接受的盐。该发明还是一种治疗或减少患者炎症风险，或治疗或减少疼痛风险的方法，包括使用含有活化凝血酶活化的纤溶抑制剂和NSAID（例如COX-2抑制剂）的组合物治疗患者。这些疾病包括但不限于肾炎、系统性红斑狼疮、类风湿关节炎、肾小球肾炎和结节病。
• Use of a COX-2 inhibitor and a NK-1 receptor antagonist for treating inflammation
  申请人：——

  公开号：US20040097573A1

  公开（公告）日：2004-05-20

  The present invention provides the use of a COX-2 inhibitior and an NK-1 receptor antagonist for the treatment or prevention of inflammatory disorders.

  本发明提供了利用COX-2抑制剂和NK-1受体拮抗剂用于治疗或预防炎症性疾病的方法。
• Combination therapy for treating neurodegenerative disease
  申请人：——

  公开号：US20020115689A1

  公开（公告）日：2002-08-22

  The instant invention provides a novel drug combination comprised of an HMG-CoA reductase inhibitor and a selective COX-2 inhibitor, which is useful for treating, preventing, delaying the onset of and/or reducing the risk of developing Alzheimer's disease. One object of the instant invention is to administer the above-described combination therapy to people who do not yet show clinical signs of Alzheimer's disease, but who are at risk of developing Alzheimer's disease. These individuals may already show signs of mild cognitive impairment. Toward this end, the instant invention provides methods for preventing or reducing the risk of developing Alzheimer's by administering the above-described combination therapy to said at risk persons. Such treatment may halt or reduce the rate of further cognitive decline or, in fact, reverse cognitive decline. The present invention also provides for a method of preventing cognitive impairment or dementia, reducing the risk of cognitive decline or impairment or reducing cognitive decline or impairment resulting from stroke, stroke, cerebral ischemia or de-myelinating disorders.

  本发明提供了一种新颖的药物组合，包括HMG-CoA还原酶抑制剂和选择性COX-2抑制剂，用于治疗、预防、延缓阿尔茨海默病的发作和/或减少发展阿尔茨海默病的风险。本发明的一个目的是将上述所述的组合疗法用于尚未表现出阿尔茨海默病临床症状，但处于患阿尔茨海默病风险的人群。这些个体可能已经表现出轻度认知障碍的迹象。为此，本发明提供了通过向上述风险人群施用上述组合疗法来预防或减少发展阿尔茨海默病的方法。这种治疗可能会阻止或减少进一步的认知下降速度，或者实际上逆转认知下降。本发明还提供了一种预防认知障碍或痴呆、减少认知下降或障碍风险或减少由中风、脑卒中、脑缺血或脱髓鞘性疾病导致的认知下降或障碍的方法。
• Method for treating inflammatory diseases by administering a thrombin inhibitor
  申请人：——

  公开号：US20010031757A1

  公开（公告）日：2001-10-18

  The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylene-carboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof. The invention is also a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor and an NSAID, e.g., a COX-2 inhibitor. Such diseases include but are not limited to nephritis, systemic lupus, erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylene-carboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl] -N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof and the COX-2 inhibitor is 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone or a pharmaceutically acceptable salt thereof.

  本发明是一种治疗患者炎症性疾病的方法，包括用一种包含凝血酶抑制剂的组合物治疗患者。这类疾病包括但不限于肾炎、系统性红斑狼疮、类风湿性关节炎、肾小球肾炎和囊肿病。在该方法的一类中，凝血酶抑制剂选自 3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基-羧酰胺甲基吡啶基)-2-吡嗪酮、N′-[&lsqb；1-(氨基亚氨基甲基)-4-哌啶基]甲基]-N-(3,3-二苯基丙酰基)-L-脯氨酸酰胺，以及3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基羧酰胺甲基吡啶基)-2-吡啶酮或其药学上可接受的盐。 本发明也是一种治疗患者炎症性疾病的方法，该方法包括用包含凝血酶抑制剂和非甾体抗炎药（如 COX-2 抑制剂）的组合物治疗患者。这类疾病包括但不限于肾炎、系统性红斑狼疮、类风湿性关节炎、肾小球肾炎和囊肿病。在该方法的一类中，凝血酶抑制剂选自 3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基-羧酰胺甲基吡啶基)-2-吡嗪酮、N′-[[1-(氨基亚氨基甲基)-4-哌啶基]甲基&rsqb；-N-(3,3-二苯基丙酰基)-L-脯氨酸酰胺和 3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基羧酰胺甲基吡啶基)-2-吡啶酮或其药学上可接受的盐，COX-2 抑制剂是 3-苯基-4-(4-(甲基磺酰基)苯基)-2-(5H)-呋喃酮或其药学上可接受的盐。