5-[3-[4-(氨基甲基)苯氧基]丙基]-2-[8-[2-(2-苯并噻唑基)亚肼基]-5,6,7,8-四氢-2-萘基]-4-噻唑羧酸

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 5-[3-[4-(氨基甲基)苯氧基]丙基]-2-[8-[2-(2-苯并噻唑基)亚肼基]-5,6,7,8-四氢-2-萘基]-4-噻唑羧酸
• 中文别名: WEHI539抑制剂
• 英文名称: 5-[3-[4-(Aminomethyl)phenoxy]propyl]-2-[(8e)-8-(1,3-Benzothiazol-2-Ylhydrazinylidene)-6,7-Dihydro-5h-Naphthalen-2-Yl]-1,3-Thiazole-4-Carboxylic Acid
• 英文别名: 5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[(8E)-8-(1,3-benzothiazol-2-ylhydrazinylidene)-6,7-dihydro-5H-naphthalen-2-yl]-1,3-thiazole-4-carboxylic acid
• 化学式: C₃₁H₂₉N₅O₃S₂
• 分子量: 583.7
• InChiKey: JKMWZKPAXZBYEH-JWHWKPFMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  41
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  179
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• [EN] NEW ANTICANCER DRUG COMBINATIONS<br/>[FR] NOUVELLES COMBINAISONS DE MÉDICAMENTS ANTICANCÉREUX
  申请人：FUNDACION PARA LA INVESTIG MEDICA APLICADA

  公开号：WO2019243236A1

  公开（公告）日：2019-12-26

  It relates to a combination comprising: A) a compound of formula (I), or a pharmaceutically or veterinary acceptable salt thereof, or any stereoisomer or mixtures of stereoisomers, either of the compound of formula (I) or of any of its pharmaceutically or veterinary acceptable salts, wherein L, X, R1, R2, R3, and R4 are as defined herein; and B) a drug selected from the group consisting of: i) an immune checkpoint inhibitor, ii) an inhibitor of an anti-apoptotic protein, and iii) a chemotherapeutic agent other than an inhibitor of an anti-apoptotic protein and an immune checkpoint inhibitor; and to pharmaceutical or veterinary compositions, and package or kit of parts comprising it. It also relates to the combination, the composition or a package or kit of parts for use in the treatment and/or prevention of cancer.

  它涉及到一种组合物，包括：A）式（I）的化合物，或其药学或兽医上可接受的盐，或者是式（I）的化合物或其药学或兽医上可接受的盐的任何立体异构体或立体异构体混合物，其中L，X，R1，R2，R3和R4如本文所定义；和B）从以下组中选择的药物：i）免疫检查点抑制剂，ii）抗凋亡蛋白的抑制剂，和iii）化疗药物，除了抗凋亡蛋白的抑制剂和免疫检查点抑制剂之外的化疗药物；以及用于治疗和/或预防癌症的药物或兽医组合物、包装或配件套件。它还涉及到该组合物、组合物或包装或配件套件，用于治疗和/或预防癌症。
• COMPOSITIONS FOR USE IN THE TREATMENT OF SENESCENCE-ASSIOCATED DISEASE AND DISORDERS
  申请人：Buck Institute for Research on Aging

  公开号：EP3669881A1

  公开（公告）日：2020-06-24

  Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

  本文提供了选择性杀死衰老细胞和通过施用衰老分解剂治疗衰老相关疾病和紊乱的方法。可通过使用本文所述衰老分解剂的方法治疗的衰老相关疾病和失调包括与动脉硬化相关或由动脉硬化引起的心血管疾病和失调，如动脉粥样硬化；特发性肺纤维化；慢性阻塞性肺病；骨关节炎；衰老相关眼科疾病和失调；以及衰老相关皮肤病和失调。
• Treatment of ophthalmic conditions by selectively removing senescent cells from the eye
  申请人：Buck Institute for Research on Aging

  公开号：US10010546B2

  公开（公告）日：2018-07-03

  Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

  本文提供了选择性杀死衰老细胞和通过施用衰老分解剂治疗衰老相关疾病和紊乱的方法。可通过使用本文所述衰老分解剂的方法治疗的衰老相关疾病和失调包括与动脉硬化相关或由动脉硬化引起的心血管疾病和失调，如动脉粥样硬化；特发性肺纤维化；慢性阻塞性肺病；骨关节炎；衰老相关眼科疾病和失调；以及衰老相关皮肤病和失调。
• Chemical entities that kill senescent cells for use in treating age-related disease
  申请人：Unity Biotechnology, Inc.

  公开号：US10195213B2

  公开（公告）日：2019-02-05

  Disclosed herein are compounds that are effective for treatment of various disease states associated with senescence. The disclosed compounds can be used to eliminate senescent cells for disease treatment. The dosing of the compounds includes both single administration and regimens of cycling dosages.

  本文公开的化合物可有效治疗与衰老有关的各种疾病状态。所公开的化合物可用于消除衰老细胞以治疗疾病。化合物的给药方式包括单次给药和循环给药。
• Anti-CDH6 antibody drug conjugates
  申请人：Bialucha Carl Uli

  公开号：US10238748B2

  公开（公告）日：2019-03-26

  The present invention relates to anti-CDH6 antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer.

  本发明涉及抗 CDH6 抗体、抗体片段、抗体药物共轭物及其治疗癌症的用途。