FG 1730 | 289638-54-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: FG 1730
• 英文别名: 3-{{4-[3-(4-chloro-phenyl)-ureido]-benzenesulfonyl}-[2-(4-methoxy-phenyl)-ethyl]-amino}-N-hydroxy-propionamide；N-Hydroxy-3-[(4-methoxyphenethyl)-(4-(3-(4-chlorophenyl)ureido)benzenesulfonyl)-amino]-propionamide；3-[[4-[(4-chlorophenyl)carbamoylamino]phenyl]sulfonyl-[2-(4-methoxyphenyl)ethyl]amino]-N-hydroxypropanamide
• CAS: 289638-54-6
• 化学式: C₂₅H₂₇ClN₄O₆S
• 分子量: 547.032
• InChiKey: URNDLUZKMFHORX-UHFFFAOYSA-N

物化性质

• 密度：
  1.420±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  37
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  145
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-(氯磺酰)异氰酸苯酯 在 羟胺 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 FG 1730
  参考文献：
  名称：

  Design and synthesis of procollagen C-proteinase inhibitors

  摘要：

  Non-peptidic inhibitors of procollagen C-proteinase (PCP) were designed from substrate leads. Compounds were optimized for potency and selectivity, with N-substituted aryl sulfonamide hydroxamates having the best combination of these properties. Compounds 89 and 60 have IC50 values of 10 and 80 nM, respectively, against PCP; excellent selectivity over MMP's 1, 2, and 9; and activity in cell-based collagen deposition assays. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.10.067

文献信息

• N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of C-proteinase and for treating or preventing disorders related to unregulated collagen production
  申请人：——

  公开号：US20030191309A1

  公开（公告）日：2003-10-09

  The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.

  本发明涉及一种新型有机分子类，能够抑制C-蛋白酶，并且利用它们来调节、调节和/或抑制异常胶原形成，作为治疗纤维化疾病的治疗方法。
• Stabilization of hypoxia inducible factor (HIF) alpha
  申请人：FIBROGEN, INC.

  公开号：EP2295059A2

  公开（公告）日：2011-03-16

  The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.

  本发明涉及稳定缺氧诱导因子（HIF）α亚基的方法。本发明进一步涉及预防、预处理或治疗与 HIF 相关的病症（包括缺血和缺氧病症）的方法。本发明还提供了用于这些方法的化合物。
• Medicaments for increasing endogenous erythropoietine (EPO)
  申请人：FIBROGEN, INC.

  公开号：EP2289531A2

  公开（公告）日：2011-03-02

  The present invention relates to compounds for use in methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Compounds for use in methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included.

  本发明涉及用于通过在体外和体内增加内源性促红细胞生成素来治疗促红细胞生成素相关疾病的方法的化合物。本发明还包括用于治疗、预处理或预调节或预防促红细胞生成素相关疾病的化合物。
• Medicaments for increasing endogenous Erythropoietin (EPO)
  申请人：Fibrogen, Inc.

  公开号：EP2298301A2

  公开（公告）日：2011-03-23

  The present invention relates to compounds for use in methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Compounds for use in methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included.

  本发明涉及用于通过在体外和体内增加内源性促红细胞生成素来治疗促红细胞生成素相关疾病的方法的化合物。本发明还包括用于治疗、预处理或预调节或预防促红细胞生成素相关疾病的化合物。
• Use of HIF Alpha stabilizers for enhancing erythropoiesis
  申请人：Fibrogen, Inc.

  公开号：EP2322153A1

  公开（公告）日：2011-05-18

  The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

  本发明涉及调节或增强红细胞生成和铁代谢以及治疗或预防慢性病缺铁和贫血的方法和化合物。