(R)-4,7-dihydro-2-[4-(2,3-dihydroxypropionylamino)phenyl]-7-(2,6-difluorobenzyl)-3-(N-benzyl-N-methylaminomethyl)-5-isobutyryl-4-oxothieno[2,3-b]pyridine | 253434-11-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: (R)-4,7-dihydro-2-[4-(2,3-dihydroxypropionylamino)phenyl]-7-(2,6-difluorobenzyl)-3-(N-benzyl-N-methylaminomethyl)-5-isobutyryl-4-oxothieno[2,3-b]pyridine
• 英文别名: (2R)-N-[4-[3-[[benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-5-(2-methylpropanoyl)-4-oxothieno[2,3-b]pyridin-2-yl]phenyl]-2,3-dihydroxypropanamide
• CAS: 253434-11-6
• 化学式: C₃₆H₃₅F₂N₃O₅S
• 分子量: 659.754
• InChiKey: XAVPOAPBNMTYRS-SSEXGKCCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  47
• 可旋转键数：
  12
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  138
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• Thienopyridine compounds, their production and use
  申请人：——

  公开号：US20010001104A1

  公开（公告）日：2001-05-10

  The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.

  本发明的化合物具有出色的促性腺激素释放激素拮抗活性，并可用于预防或治疗性激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌、子宫癌、乳腺癌、垂体肿瘤）、前列腺肥大、子宫肌瘤、子宫内膜异位症、性早熟、闭经综合征、多囊卵巢综合征、痤疮等，或作为妊娠调节剂（例如避孕药）、不孕症疗法或月经调节剂。
• SUSTAINED RELEASE COMPOSITIONS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1291023A1

  公开（公告）日：2003-03-12

  A composition prepared by containing or blending a physiologically active non-peptide substance and a biodegradable polymer having two or more carboxylic groups at its end or a salt thereof features: (1) larger content of the physiologically active non-peptide substance can be contained, as well as release of the same can be controlled or accelerated, whereby secure pharmaceutical effect is achieved; (2) when the physiologically active non-peptide substance causes subcutaneous stimulation, an activity of canceling the stimulation by strongly acidic group at its end is expected; and (3) high glass transition point and high stability.

  通过含有或混合生理活性非肽物质和具有两个或两个以上羧基末端的可生物降解聚合物或其盐制备的组合物具有以下特点：（1）可以含有更多生理活性非肽物质，并且可以控制或加速其释放，从而实现安全的药效；（2）当生理活性非肽物质引起皮下刺激时，预计具有在其末端具有强酸性基团的活性来取消刺激；以及（3）高玻璃转变温度和高稳定性。
• Preventives/remedies for alzheimer's disease
  申请人：——

  公开号：US20030134863A1

  公开（公告）日：2003-07-17

  The present invention provides an agent for the prophylaxis or treatment of Alzheimer's disease. The agent for the prophylaxis or treatment of Alzheimer's disease of the present invention containing a compound having a GnRH antagonistic action shows low toxicity and has a superior preventive and therapeutic effect on Alzheimer's disease.

  本发明提供了一种用于预防或治疗阿尔茨海默病的药剂。本发明的用于预防或治疗阿尔茨海默病的药剂含有具有GnRH拮抗作用的化合物，显示出低毒性，并对阿尔茨海默病具有卓越的预防和治疗效果。
• MEDICINAL SOLUTIONS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1374855A1

  公开（公告）日：2004-01-02

  The present invention relates to a pharmaceutical solution containing a physiologically active non-peptide substance, an organic acid and a biocompatible organic solvent, and provides a pharmaceutical solution wherein a physiologically active non-peptide substance is dissolved at a high concentration.

  本发明涉及一种含有生理活性非肽物质、有机酸和生物相容性有机溶剂的药物溶液，并提供了一种药物溶液，其中生理活性非肽物质以高浓度溶解。
• [EN] THIENOPYRIDINE COMPOUNDS, THEIR PRODUCTION AND USE<br/>[FR] COMPOSES DE THIENOPYRIDINE, ET PROCEDE DE PRODUCTION ET D'UTILISATION CORRESPONDANT
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2000000493A1

  公开（公告）日：2000-01-06

  The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc., or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.

  本发明的化合物具有优异的促性腺激素释放激素拮抗活性，可用于预防或治疗性激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌、子宫癌、乳腺癌、垂体肿瘤）、前列腺增生、子宫肌瘤、子宫内膜异位症、性早熟、闭经综合症、多囊卵巢综合症、青春痘等，或作为妊娠调节剂（例如避孕药）、不孕症治疗药物或月经调节剂。