H-DL-Pyr-DL-His-DL-Trp-DL-Ser-DL-Tyr-Gly-DL-Leu-DL-Arg-DL-Pro-Gly-NH2.Cl-

• 分子结构分类: 有机化合物 - 有机聚合物 - 多肽
• 英文名称: H-DL-Pyr-DL-His-DL-Trp-DL-Ser-DL-Tyr-Gly-DL-Leu-DL-Arg-DL-Pro-Gly-NH2.Cl-
• 英文别名: N-[1-[[1-[[1-[[1-[[2-[[1-[[1-[2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide;hydron;chloride
• 化学式: C55H76ClN17O13
• 分子量: 1218.7
• InChiKey: UPRWQSQENCASAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.97
• 重原子数：
  86
• 可旋转键数：
  31
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  475
• 氢给体数：
  17
• 氢受体数：
  15

文献信息

• LONG-ACTING PALMITIC ACID-CONJUGATED GnRH DERIVATIVE, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
  申请人：Novel Pharma Inc.

  公开号：EP3639856A1

  公开（公告）日：2020-04-22

  The present invention relates to a novel long-acting palmitic acid-conjugated gonadotrophin-releasing hormone (GnRH) derivative and a pharmaceutical composition containing the same. A GnRH derivative of the present invention is expected to greatly contribute, through excellent bioavailability and increased half-life in blood, to the reduction in drug dosing frequency and dosage and the like in the treatment of sex hormone-dependent diseases. Particularly, the GnRH derivative can overcome the disadvantages of existing GnRH sustained-release preparations, which have the side effects of residual feeling and pain at the injection site.

  本发明涉及一种新型长效棕榈酸共轭促性腺激素释放激素（GnRH）衍生物和含有该衍生物的药物组合物。本发明的 GnRH 衍生物具有极佳的生物利用度和更长的血液半衰期，有望在治疗性激素依赖性疾病时大大有助于减少用药次数和剂量等。特别是，本发明的 GnRH 衍生物可以克服现有 GnRH 缓释制剂存在的注射部位残留感和疼痛等副作用的缺点。
• Long-acting palmitic acid-conjugated GnRH derivative, and pharmaceutical composition containing same
  申请人：NOVEL PHARMA INC.

  公开号：US10994018B2

  公开（公告）日：2021-05-04

  The present invention relates to a novel long-acting palmitic acid-conjugated gonadotrophin-releasing hormone (GnRH) derivative and a pharmaceutical composition containing the same. A GnRH derivative of the present invention is expected to greatly contribute, through excellent bioavailability and increased half-life in blood, to the reduction in drug dosing frequency and dosage and the like in the treatment of sex hormone-dependent diseases. Particularly, the GnRH derivative can overcome the disadvantages of existing GnRH sustained-release preparations, which have the side effects of residual feeling and pain at the injection site.

  本发明涉及一种新型长效棕榈酸共轭促性腺激素释放激素（GnRH）衍生物和含有该衍生物的药物组合物。本发明的 GnRH 衍生物具有极佳的生物利用度和更长的血液半衰期，有望在治疗性激素依赖性疾病时大大有助于减少用药次数和剂量等。特别是，本发明的 GnRH 衍生物可以克服现有 GnRH 缓释制剂存在的注射部位残留感和疼痛等副作用的缺点。
• [EN] LONG-ACTING PALMITIC ACID-CONJUGATED GnRH DERIVATIVE, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME<br/>[FR] DÉRIVÉ DE GnRH CONJUGUÉ À DE L'ACIDE PALMITIQUE À ACTION PROLONGÉE ET COMPOSITION PHARMACEUTIQUE CONTENANT CELUI-CI<br/>[KO] 지속형 팔미트산 결합 GnRH 유도체 및 이를 포함하는 약제학적 조성물
  申请人：JP BIO G INC

  公开号：WO2019066199A1

  公开（公告）日：2019-04-04

  본 발명은 생식샘자극 호르몬 방출 호르몬(gonadotrophin-releasing hormone; GnRH)의 신규한 지속형 팔미트산 결합 GnRH 유도체 및 이를 포함하는 약제학적 조성물에 관한 것이다. 본 발명 GnRH 유도체의 우수한 생체 이용률 및 증가한 혈중 반감기를 통해 성 호르몬-의존성 질환 치료에 있어 의약의 투약 빈도수나 투약량 감소 등에 크게 기여할 것으로 기대된다. 특히, 기존의 주사 부위의 잔존감과 통증의 부작용을 가지고 있던 GnRH 서방형 제제들의 단점을 극복할 수 있을 것이다.