Lpt-99 | 1263477-83-3

• 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: Lpt-99
• 英文别名: 2-[4-[2-(2,4-dichlorophenyl)ethyl]-3,6-dioxo-1-(2-thiophen-2-ylethyl)piperazin-2-yl]-N-[2-(5-methoxy-1H-indol-3-yl)ethyl]acetamide
• CAS: 1263477-83-3
• 化学式: C₃₁H₃₂Cl₂N₄O₄S
• 分子量: 627.6
• InChiKey: XLXXBYJYWULGGD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  42
• 可旋转键数：
  12
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  123
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• APAF-1 INHIBITOR COMPOUNDS
  申请人：Messeguer Pyepoch Ángel

  公开号：US20120122868A1

  公开（公告）日：2012-05-17

  Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.

  公式（I）的2,5-哌嗪二酮衍生物是凋亡肽酶激活因子1（Apaf-1）抑制剂，因此它们可用作预防和/或治疗与凋亡增加相关的病理和/或生理状况的活性药用成分。
• Apoptosis inhibitor formulations for prevention of hearing loss
  申请人：Spiral Therapeutics, Inc.

  公开号：US10561736B1

  公开（公告）日：2020-02-18

  A formulation for sustained release of an apoptosis inhibitor in the inner ear to protect from hearing loss, especially due to exposure to chemotherapy with drugs such as cisplatin. The formulation can be injected through a small gauge needle into the inner ear, where it gels to form a sustained release depot for controlled delivery of drug over a few days. In the preferred embodiment, the formulation includes a thermoresponsive sol-gel polymer such as POLOXAMER 407 and an apoptosis inhibitory agent, preferably an inhibitor of apoptotic protease activating factor-1 (APAF-1), in an effective amount to prevent hearing loss, for example, due to the administration of platinum-based chemotherapeutic agents. As demonstrated by the examples, the hydrogel provides sustained release of an apoptosis inhibitory agent, LPT99, an anti-apoptosis agent that inhibits apoptotic protease activating factor-1 (APAF-1), as well as safety and efficacy in in vitro and in vivo models.

  一种可在内耳中持续释放细胞凋亡抑制剂的制剂，可防止听力损失，尤其是因接触顺铂等化疗药物而导致的听力损失。该制剂可通过小号针头注入内耳，在内耳中凝胶化形成缓释库，在数天内控制药物的输送。在优选的实施方案中，制剂包括一种热致伸缩性溶胶凝胶聚合物（如 POLOXAMER 407）和一种凋亡抑制剂，最好是一种凋亡蛋白酶激活因子-1（APAF-1）抑制剂，其有效用量可防止因施用铂类化疗药物等引起的听力损失。如实例所示，水凝胶可持续释放凋亡抑制剂 LPT99（一种抑制凋亡蛋白酶活化因子-1（APAF-1）的抗凋亡剂），并在体外和体内模型中具有安全性和有效性。
• SELF-GELLING SOLUTIONS FOR ADMINISTRATION OF THERAPEUTICS TO THE INNER EAR
  申请人：Spiral Therapeutics, Inc.

  公开号：US20200214976A1

  公开（公告）日：2020-07-09

  A solution for sustained release of therapeutic, prophylactic and/or diagnostic agent in the inner ear has been developed. The formulation can be injected through a small gauge needle into the inner ear, where it gels to form a sustained release depot for controlled delivery of drug over a few days. In the preferred embodiment, the formulation includes a thermoresponsive sol-gel polymer such as POLOXAMER 407 which forms a stable hydrogel after trans-tympanic injection. As demonstrated by the examples, the hydrogel provides sustained release of an apoptosis inhibitory agent, LPT99, an anti-apoptosis agent that inhibits apoptotic protease activating factor 1 (APAF-1), as well as safety and efficacy in in vitro and in vivo models.
• APOPTOSIS INHIBITOR FORMULATIONS FOR PREVENTION OF HEARING LOSS
  申请人：Spiral Therapeutics, Inc.

  公开号：US20200215194A1

  公开（公告）日：2020-07-09

  A formulation for sustained release of an apoptosis inhibitor in the inner ear to protect from hearing loss, especially due to exposure to chemotherapy with drugs such as cisplatin. The formulation can be injected through a small gauge needle into the inner ear, where it gels to form a sustained release depot for controlled delivery of drug over a few days. In the preferred embodiment, the formulation includes a thermoresponsive sol-gel polymer such as POLOXAMER 407 and an apoptosis inhibitory agent, preferably an inhibitor of apoptotic protease activating factor-1 (APAF-1), in an effective amount to prevent hearing loss, for example, due to the administration of platinum-based chemotherapeutic agents. As demonstrated by the examples, the hydrogel provides sustained release of an apoptosis inhibitory agent, LPT99, an anti-apoptosis agent that inhibits apoptotic protease activating factor-1 (APAF-1), as well as safety and efficacy in in vitro and in vivo models.
• US9040701B2
  申请人：——

  公开号：US9040701B2

  公开（公告）日：2015-05-26