9-p-Methylsulfonamidobenzyl-6,8-difluoro-1,2,3,4-tetrahydro carbazol-1-yl-acetic acid | 121083-15-6

• 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: 9-p-Methylsulfonamidobenzyl-6,8-difluoro-1,2,3,4-tetrahydro carbazol-1-yl-acetic acid
• 英文别名: 2-[6,8-Difluoro-9-[[4-(methanesulfonamido)phenyl]methyl]-1,2,3,4-tetrahydrocarbazol-1-yl]acetic acid
• CAS: 121083-15-6
• 化学式: C₂₂H₂₂F₂N₂O₄S
• 分子量: 448.49
• InChiKey: PNDCNKXNVFWCJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  96.8
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Tetrahydrocarbazoles for the improvement of cyclosporin therapy
  申请人：MERCK FROSST CANADA INC.

  公开号：EP0307077A1

  公开（公告）日：1989-03-15

  Tetrahydrocarbazoles, especially Tetrahydrocarbazole-1-alkanoic acids are disclosed. The compounds are useful for improving cyclosporine therapy. In particular, the compounds are useful for limiting cyclosporine induced nephrotoxicity which comprises the adjunct administration in a mammal of an effective amount of cyclosporine and an effective amount of the tetrahydrocarbazole 1-alkanoic acids.

  四氢咔唑，尤其是四氢咔唑-1-烷酸被披露。这些化合物对改善环孢霉素疗法有用。具体来说，这些化合物对限制环孢霉素诱导的肾毒性有用，包括在哺乳动物中同时给予有效剂量的环孢霉素和四氢咔唑-1-烷酸。
• Tetrahydrocarbazole 1-alkanoic acids
  申请人：MERCK FROSST CANADA INC.

  公开号：EP0300676A2

  公开（公告）日：1989-01-25

  Tetrahydrocarbazole 1-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and as cytoprotective agents.

  公开了四氢咔唑 1-烷酸。这些化合物具有前列腺素和血栓素拮抗剂的作用，可用于治疗哮喘、腹泻、高血压、心绞痛、血小板聚集、脑痉挛、早产、自然流产和痛经，还可用作细胞保护剂。
• Tetrahydrocarbazole esters
  申请人：MERCK FROSST CANADA INC.

  公开号：EP0310179A2

  公开（公告）日：1989-04-05

  Tetrahydrocarbazole esters are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and nephrotoxicity casued by cyclosporin A and as cytoprotective agents.

  公开了四氢咔唑酯。这些化合物具有前列腺素和血栓素拮抗剂的作用，可用于治疗哮喘、腹泻、高血压、心绞痛、血小板聚集、脑痉挛、早产、自然流产、痛经、环孢素 A 引起的肾毒性以及细胞保护剂。
• Compositions for the treatment and prevention of arterial thrombosis and use of an inhibitor of factor Xa alone and/or in combination with an anti-platelet aggregation agent
  申请人：——

  公开号：US20040092477A1

  公开（公告）日：2004-05-13

  The invention relates to the use of direct or indirect selective inhibitors of factor Xa acting via antithrombin III, alone or in combination with one or more compounds with anti-platelet aggregation activity, for the preparation of medicines intended to prevent and to treat thromboembolic arterial diseases. The subject of the invention is also pharmaceutical compositions containing one or more direct or indirect selective inhibitors of factor Xa which act via antithrombin III in combination with one or more compounds with anti-platelet aggregation activity, and optionally one or more pharmaceutically acceptable vehicles.

  本发明涉及通过抗凝血酶 III 起作用的 Xa 因子的直接或间接选择性抑制剂单独或与一种或多种具有抗血小板聚集活性的化合物相结合，用于制备旨在预防和治疗血栓栓塞性动脉疾病的药物。 本发明的主题也是药物组合物，含有一种或多种通过抗凝血酶 III 起作用的 Xa 因子直接或间接选择性抑制剂，与一种或多种具有抗血小板聚集活性的化合物，以及一种或多种药学上可接受的载体。
• US4808608A
  申请人：——

  公开号：US4808608A

  公开（公告）日：1989-02-28