5-[(3,5,5,8,8-五甲基-5,6,7,8-四氢-2-萘基)甲基]-N-(2,4,6-三甲氧基苯基)-2-糠酰胺 | 263847-55-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 5-[(3,5,5,8,8-五甲基-5,6,7,8-四氢-2-萘基)甲基]-N-(2,4,6-三甲氧基苯基)-2-糠酰胺
• 英文名称: 5-((3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide
• 英文别名: 5-[(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)methyl]-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide
• CAS: 263847-55-8
• 化学式: C₃₀H₃₇NO₅
• 分子量: 491.6
• InChiKey: IPEMCIBPDYCJLO-UHFFFAOYSA-N

物化性质

• 溶解度：
  溶于 DMSO<49.16mg/ml；在乙醇中 <24.58mg/ml

计算性质

• 辛醇/水分配系数(LogP)：
  7.5
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  69.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• PREVENTIVES FOR POSTOPERATIVE RECURRENCE OF PREMENOPAUSAL BREAST CANCER
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1382350A1

  公开（公告）日：2004-01-21

  The agent for preventing the postoperative recurrence of premenopausal breast cancer comprising a GnRH agonist or antagonist of the present invention can prevent the postoperative recurrence of premenopausal breast cancer without severe side effects. In addition, by using the agent of the present invention in the form of a long term sustained-release type microcapsule, the drug action can be maintained for a long time without frequently administering the drug, and thus, prevention of the postoperative recurrence of premenopausal breast cancer having a long recurrence-preventing term and having high convenience becomes possible.

  由本发明的GnRH激动剂或拮抗剂组成的预防绝经前乳腺癌术后复发的制剂可预防绝经前乳腺癌术后复发，且无严重副作用。此外，通过以长期缓释型微胶囊的形式使用本发明的制剂，可以在不频繁给药的情况下长期保持药物作用，因此可以预防绝经前乳腺癌术后复发，其预防复发的期限长，且具有很高的便利性。
• PREVENTIVES/REMEDIES FOR HOTFLASH
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1495768A1

  公开（公告）日：2005-01-12

  It is intended to provide a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, in particular, a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, wherein said compound is capable of entering the brain.

  本发明旨在提供一种预防或治疗潮热的药物，它包括一种具有促性腺激素释放激素拮抗活性的非肽化合物，特别是一种预防或治疗潮热的药物，它包括一种具有促性腺激素释放激素拮抗活性的非肽化合物，其中所述化合物能够进入大脑。
• PROCESS FOR PRODUCING SUSTAINED-RELEASE COMPOSITION
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1532985A1

  公开（公告）日：2005-05-25

  A process for producing a sustained-release composition which comprises mixing an aqueous solution containing a physiologically active substance and an acid or base in a molar amount of 1.5 or more times that of the physiologically active substance with a solution of a biodegradable polymer and then drying the mixture is provided.

  本发明提供了一种生产缓释组合物的工艺，包括将含有生理活性物质和酸或碱的水溶液（摩尔量为生理活性物质的 1.5 倍或以上）与生物可降解聚合物溶液混合，然后干燥混合物。
• PREMATURE OVULATION PREVENTIVE AGENT
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1917978A1

  公开（公告）日：2008-05-07

  The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process.

  本发明提供了一种用于体外受精或胚胎移植过程的过早排卵抑制剂，它含有一种具有促性腺激素释放激素拮抗作用的非肽类化合物。本发明的体外受精或胚胎移植过程中使用的过早排卵抑制剂毒性低，允许口服，对体外受精或胚胎移植过程中的过早排卵具有卓越的抑制作用。
• Use of LHRH antagonists at non-castrating doses
  申请人：Æterna Zentaris GmbH

  公开号：EP2095818A1

  公开（公告）日：2009-09-02

  The invention relates to medicaments comprising at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonist, for use in treatment or prophylaxis of physiological and/or pathological conditions, wherein the at least one LHRH antagonist is to be administered in an intermediate dose, which does not cause chemical (hormonal) castration.

  本发明涉及包含至少一种 LHRH 拮抗剂，特别是至少一种拟肽 LHRH 拮抗剂的药物，用于治疗或预防生理和/或病理状况，其中至少一种 LHRH 拮抗剂的给药剂量为中间剂量，不会导致化学（激素）阉割。