(5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-[4-(methylsulfonyl)-phenyl]-2,5-dihydro-2-furanone

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: (5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-[4-(methylsulfonyl)-phenyl]-2,5-dihydro-2-furanone
• 英文别名: (5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-(4-methylsulfonylphenyl)furan-2-one
• 化学式: C₂₀H₁₈F₂O₄S
• 分子量: 392.423
• InChiKey: CCTOCAZCUXUVKE-HXUWFJFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  68.8
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• 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。
• CYCLOOXYGENASE-2 INHIBITOR/HISTONE DEACETYLASE INHIBITOR COMBINATION
  申请人：Chen Ying-Nan Pan

  公开号：US20080227845A1

  公开（公告）日：2008-09-18

  The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.

  本发明涉及一种组合物，包括（a）环氧合酶-2抑制剂（“COX-2抑制剂”）和（b）组蛋白去乙酰化酶抑制剂（“HDAI”），用于同时、并行、分离或顺序使用，特别是用于治疗哺乳动物，特别是人类的癌前结肠病变或结肠癌或其他恶性肿瘤。本发明还涉及包含这种组合物的制药组合物，以及使用这种组合物治疗癌前结肠病变（例如息肉）和结肠癌以及其他恶性肿瘤的方法。本发明还涉及包含这种组合物的商业包装或产品。
• DIARYL-5-ALKYL-5-METHYL-2(5H)-FURANONES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS
  申请人：MERCK FROSST CANADA INC.

  公开号：EP1028951A1

  公开（公告）日：2000-08-23
• PHARMACEUTICAL COMPOSITION FOR USE FOR THE TREATMENT OF MALIGNANCIES COMPRISING IN COMBINATION A BISPHOSPHONATE, A COX-2 INHIBITOR AND A TAXOL
  申请人：Novartis AG

  公开号：EP1443942B1

  公开（公告）日：2008-01-02
• Silicon Containing Compounds Having Selective Cox-2 Inhibitory Activity and Methods of Making and Using the Same
  申请人：ENGLEBIENNE PATRICK

  公开号：US20090197833A1

  公开（公告）日：2009-08-06

  Silicon-containing compounds having selective COX-2 inhibitory activity, as well as compositions thereof are provided. The subject compounds find use in a variety of applications, including therapeutic applications. Also provided are kits containing the subject compounds and pharmaceutical preparations thereof.