5-chloro-FTS

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: 5-chloro-FTS
• 英文别名: 5-chloro-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid
• 化学式: C₂₂H₂₉ClO₂S
• 分子量: 392.99
• InChiKey: BNENOULFKRUUQV-IJUJUXHTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.8
• 重原子数：
  26
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  62.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Non-malignant disease treatment with Ras antagonists
  申请人：Kloog Yoel

  公开号：US20050119237A1

  公开（公告）日：2005-06-02

  Disclosed is a method for inhibiting Ras-induced or mediated proliferation of cells associated with a non-malignant disease, disorder or pathological condition. The method entails administering to a patient a Ras antagonist in an amount effective to inhibit the proliferation. The invention is particularly applicable to diseases characterized by a proliferation of T-cells such as autoimmune disease, e.g., type 1 diabetes, lupus and multiple sclerosis, and pathological states such as graft rejection induced by the presentation of a foreign antigen such as a graft in response to a disease condition (e.g., kidney failure). Other non-malignant diseases characterized by proliferations of cells include cirrhosis of the liver and restenosis. Preferred Ras antagonists are S-trans-trans farnesylthiosalicylic acid (FTS) and structurally related compounds (or analogs) thereof.

  本发明公开了一种抑制与非恶性疾病、失调或病理状态相关的细胞Ras诱导或介导增殖的方法。该方法包括向患者施用有效量的Ras拮抗剂以抑制增殖。本发明特别适用于由T细胞增殖所特征的疾病，例如自身免疫疾病，例如1型糖尿病、狼疮和多发性硬化症，以及由疾病状态（例如肾衰竭）对外来抗原（例如移植物）的呈现引起的移植排斥等病理状态。其他由细胞增殖所特征的非恶性疾病包括肝硬化和再狭窄。首选的Ras拮抗剂是S-转-转-法尼基硫酸水杨酸（FTS）及其结构相关化合物（或类似物）。
• TREATMENT OF HEMATOLOGICAL MALIGNANCIES WITH FTS AND A BCR-ABL TYROSINE KINASE INHIBITOR
  申请人：Kloog Yoel

  公开号：US20090298843A1

  公开（公告）日：2009-12-03

  Disclosed are methods of treating a hematological malignancy by administering to a human in need thereof effective amounts of FTS (Farnesylthiosalicylic Acid), or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally in combination with a Bcr-Abl tyrosine kinase inhibitor. Also disclosed are pharmaceutical compositions comprising FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, a Bcr-Abl tyrosine kinase inhibitor, preferably Imatinib and a pharmaceutically acceptable carrier.

  本发明公开了治疗血液恶性肿瘤的方法，该方法通过向需要治疗的人体内给予有效量的FTS（芳基硫酰基水杨酸）或其各种类似物，或其药学上可接受的盐，可选择与Bcr-Abl酪氨酸激酶抑制剂联合使用。本发明还公开了包含FTS或其各种类似物或其药学上可接受的盐，Bcr-Abl酪氨酸激酶抑制剂，优选为伊马替尼和药学上可接受的载体的制药组合物。
• Use of FTS for treating malignant disorders
  申请人：Concordia Pharmaceuticals, Inc.

  公开号：EP2218451A1

  公开（公告）日：2010-08-18

  Disclosed are oral dosage forms containing a Ras antagonist including FTS and structural analogues thereof, and at least one pharmaceutically acceptable excipient other than a cyclodextrin, and methods of orally administering same to treat diseases and disorders responsive to the Ras antagonists

  公开了含有 Ras 拮抗剂（包括 FTS 及其结构类似物）和至少一种药学上可接受的赋形剂（环糊精除外）的口服剂型，以及口服该剂型以治疗对 Ras 拮抗剂有反应的疾病和失调的方法。
• NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS
  申请人：Thyreos Corporation

  公开号：EP1187605A1

  公开（公告）日：2002-03-20
• EP1187605A4
  申请人：——

  公开号：EP1187605A4

  公开（公告）日：2004-05-26