Amelparib dihydrochloride | 1227156-71-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: Amelparib dihydrochloride
• 英文别名: 10-ethoxy-8-(morpholin-4-ylmethyl)-2,3,4,6-tetrahydro-1H-benzo[h][1,6]naphthyridin-5-one;dihydrochloride
• CAS: 1227156-71-9
• 化学式: C19H27Cl2N3O3
• 分子量: 416.3
• InChiKey: GJWOWHCCGXTLDV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.96
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  62.8
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Kim Myung-Hwa

  公开号：US20110218193A1

  公开（公告）日：2011-09-08

  The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.

  本发明涉及一种新型三环衍生物，具有高效的抑制聚(ADP-核糖)聚合酶（PARP）或其药用可接受盐的活性，以及其制备方法和含有该衍生物的药物组合物。本发明的三环衍生物通过抑制聚(ADP-核糖)聚合酶的活性，对于预防或治疗由过度PARP活性引起的疾病特别有效，包括神经病痛、神经退行性疾病、心血管疾病、糖尿病肾病、炎症性疾病、骨质疏松症和癌症。
• CRYSTALLINE FORMS OF TRICYCLIC COMPOUND ACID SALT OR HYDRATE THEREOF, AND METHOD FOR MAKING THEREOF
  申请人：Jeil Pharmaceutical Co., Ltd.

  公开号：US20140350007A1

  公开（公告）日：2014-11-27

  The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.

  本发明涉及一种新型三环衍生物的结晶酸盐或其水合物及其生产方法。根据本发明的结晶酸盐或其水合物对湿度稳定且对吸湿性稳定，制药过程中的质量控制良好。此外，根据本发明的结晶酸盐或其水合物可用于预防或治疗由PARP过度活化引起的神经病症状，如神经痛、癫痫、中风、阿尔茨海默病、帕金森病、肌萎缩侧索硬化症（ALS）、亨廷顿病、精神分裂症、慢性和急性疼痛、缺血性脑损伤、缺氧后神经元丧失、创伤和神经损伤等医疗状况中的药物组合物。
• US8815891B2
  申请人：——

  公开号：US8815891B2

  公开（公告）日：2014-08-26
• US9522911B2
  申请人：——

  公开号：US9522911B2

  公开（公告）日：2016-12-20
• [EN] PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ISCHEMIC ACUTE KIDNEY INJURY, CONTAINING TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF<br/>[FR] COMPOSITION PHARMACEUTIQUE DE PRÉVENTION OU DE TRAITEMENT D'UNE LÉSION RÉNALE AIGUË ISCHÉMIQUE, COMPRENANT UN DÉRIVÉ TRICYCLIQUE OU UN SEL PHARMACEUTIQUEMENT ACCEPTABLE DE CE DERNIER<br/>[KO] 트리시클릭 유도체 또는 이의 약학적으로 허용 가능한 염을 포함하는 허혈성 급성 신 손상 예방 또는 치료용 약학적 조성물
  申请人：SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

  公开号：WO2018101762A1

  公开（公告）日：2018-06-07

  본 발명은 트리시클릭 유도체 또는 이의 약학적으로 허용 가능한 염을 포함하는 허혈성 급성 신 손상, 이식신 기능 지연 (delayed graft function, DGF)의 예방 또는 치료용 약학적 조성물 또는 이의 치료 방법에 관한 것이다. 본 발명의 트리시클릭 유도체, 바람직하게는 10-에톡시-8-(모르폴리노메틸)-1,2,3,4-테트라히드로벤조[h][1,6]나프티리딘-5(6H)-온 디히드로클로라이드 또는 이의 약학적으로 허용 가능한 염은 PARP의 저해제로 PARP를 특이적으로 저해함으로써, 재관류 손상에 의해 손상된 신세관 세포 자체가 면역학적 염증 반응을 촉진하여 신 손상을 진행시키는 것을 직접적인 면역억제작용 (immunosuppression) 없이 원천적으로 억제할 수 있으며, 경구 투여 흡수율이 좋을 뿐만 아니라, 주로 간으로 대사되어 신기능이 저하된 상태에서도 투여 가능하므로, 임상에서 더욱 유용하게 사용될 수 있다.