Implix | 8060-43-3

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Implix
• 英文别名: (8S,9S,10R,13S,14S,17S)-17-acetyl-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one;(8R,9S,13S,14S,17S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
• CAS: 8060-43-3
• 化学式: C39H54O4
• 分子量: 586.8
• InChiKey: VBKJKYFABSYSJQ-HNOSYHRKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.33
• 重原子数：
  43
• 可旋转键数：
  1
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.74
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] COMBINATION OF ESTROGENS PLUS ANTIPROGESTINS WITH SIGNIFICANT PARTIAL AGONISTIC EFFECT AS AN EFFECTIVE TREATMENT OF MENOPAUSAL SYMPTOMS AND FOR PREVENTION OF THE OCCURRENCE OF BREAST CANCER<br/>[FR] COMBINAISON D'ŒSTROGÈNES ET D'ANTIPROGESTATIFS À EFFET AGONISTE PARTIEL SIGNIFICATIF POUR LE TRAITEMENT EFFICACE DES SYMPTÔMES DE LA MÉNOPAUSE ET POUR LA PRÉVENTION DU CANCER DU SEIN
  申请人：EVESTRA INC

  公开号：WO2016090139A1

  公开（公告）日：2016-06-09

  Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

  本文描述了一种解决现有方法缺陷的激素替代疗法的组合物和方法。本文描述了具有药效的部分激动抗孕激素。雌激素（如雌二醇、雌三醇和复方雌激素）与所述的部分激动抗孕激素的联合应用可用于激素替代疗法。
• Non-Mammalian GnRH analogs and uses thereof in regulation of fertility and pregnancy
  申请人：Siler-Khodr, Theresa M.

  公开号：EP1586581A2

  公开（公告）日：2005-10-19

  Chicken II and salmon GnRH or its analog decapeptides resistant to degradation by peptidase incorporating D-arginine, D-leucine, D-tBu-Serine, D-Trp or other active D amino acids at position 6 and ethylamide, aza-Gly-amide or other Gly amide at position 10. The non-mammalian GnRH or its analogs demonstrate preferential binding to male and female reproductive system GnRH receptors as well as tumor cell GnRH receptors in these systems. Biopotency is greater within the reproductive system and at tumor cells than at the pituitary. These non-mammalian GnRH or its analogs may be used in pharmaceutical preparations, and specifically in various treatment methods as a contraceptive or post-coital contraceptive agent. The non-mammalian GnRH or its analogs are also provided in pharmaceutical preparations that may be used clinically for maintaining pregnancy when used in very low doses and administered in pulsatile fashion, as well as in preparations for the treatment of male and female reproductive system disorders including cancers of these systems or other system with GnRH II receptors. The aza-Gly (10) amide non-mammalian analogs are yet other embodiments of the non-mammalian GnRH analogs provided as a part of the invention.

  鸡 II 和鲑鱼 GnRH 或其类似物可抗肽酶降解，在第 6 位含有 D-精氨酸、D-亮氨酸、D-tBu-丝氨酸、D-Trp 或其他活性 D 氨基酸，在第 10 位含有乙酰胺、偶氮甘氨酰胺或其他甘氨酰胺。非哺乳动物 GnRH 或其类似物显示出与男性和女性生殖系统 GnRH 受体以及肿瘤细胞 GnRH 受体的优先结合。在生殖系统和肿瘤细胞中的生物活性高于垂体。这些非哺乳动物 GnRH 或其类似物可用于药物制剂，特别是在各种治疗方法中用作避孕药或性交后避孕药。这些非哺乳动物 GnRH 或其类似物还可用于药物制剂，在临床上以极低剂量和脉冲方式给药时可用于维持妊娠，以及用于治疗男性和女性生殖系统疾病，包括这些系统的癌症或具有 GnRH II 受体的其他系统。杂-甘氨酰（10）酰胺非哺乳动物类似物是作为本发明的一部分提供的非哺乳动物 GnRH 类似物的其他实施方案。
• GNRH ANTAGONISTS FOR DEACREASING RISK OF RETAINED PREGNANCY
  申请人：Previvo Genetics, LLC

  公开号：EP3025753A1

  公开（公告）日：2016-06-01

  Uterine lavage is performed to withdraw at least 50% of in vivo fertilized preimplantation embryos produced after superovulation of a woman and artificial insemination using sperm of her sexual partner. Subject of the invention is a GnRH antagonist (e.g. cetrotide) alone or combined to a progesterone receptor antagonist (e.g. mifepristone) used for decreasing the risk of retained pregnancy by possibly non-withdrawn embryos. After genetic diagnosis or sex determination or gene therapy, or any combination of any two or more of them, of the recovered embryos and selection of at least one of the embryos to be implanted, the selected embryos are returned to the woman for implantation in her uterus.

  进行子宫灌洗是为了提取妇女超排卵和使用其性伴侣的精子进行人工授精后产生的至少50%的体内受精着床前胚胎。本发明的主题是一种 GnRH 拮抗剂（例如西曲肽），单独使用或与孕酮受体拮抗剂（例如米非司酮）联合使用，用于降低可能未抽出胚胎的保留妊娠风险。对取出的胚胎进行基因诊断或性别鉴定或基因治疗，或其中任何两种或两种以上的组合，并选择至少一个胚胎植入后，将选定的胚胎送回妇女体内植入子宫。
• Non-mammalian GnRH analogs and uses thereof in regulation of fertility and pregnancy
  申请人：——

  公开号：US20020065226A1

  公开（公告）日：2002-05-30

  Specially designed non-mammalian GnRH analog decapeptides resistant to degradation by the placental enzyme, C-ase-1, or a post-proline peptidase, are disclosed. The GnRH analogs are further defined as analogs of chicken II GnRH or salmon GnRH. These non-mammalian analogs incorporate D-arginine, D-leucine, D-tBu-Serine, D-Trp or other active D amino acids at position 6 and ethylamide, aza-Gly-amide or other Gly amide at position 10. The D-Arg (6)-chicken II GnRH-ethylamide, D-Arg (6)-chicken II GnRH-aza-Gly (10)-amide, the D-Arg (6)-salmon GnRH ethylamide, and D-Arg (6)-salmon GnRH-aza-Gly (10)-amide analogs are also provided, and demonstrate preferential binding to chorionic GnRH, ovarian, endometrial, tubal, uterine, prostate and testicular receptors. Biopotency is greater at the ovary and endometrium than at the pituitary. These non-mammalian GnRH analogs may be used in pharmaceutical preparation, and specifically in various treatment methods as a contraceptive or post-coital contraceptive agent. The non-mammalian GnRH analogs are also provided in pharmaceutical preparations that may be used clinically for maintaining pregnancy when used in very low doses and administered in pulsatile fashion, as well as in preparations for the treatment of endometriosis, ovarian cysts, and leimyomas. In another aspect, the non-mammalian GnRH analogs may be used a luteolytic agents. The aza-Gly (10) amide non-mammalian analogs are yet other embodiments of the non-mammalian GnRH analogs provided as a part of the invention.

  本研究公开了专门设计的非哺乳动物 GnRH 类似物十肽，可抵抗胎盘酶 C-ase-1 或脯氨酸后肽酶的降解。GnRH 类似物进一步定义为鸡 II GnRH 或鲑鱼 GnRH 的类似物。这些非哺乳动物类似物在第 6 位含有 D-精氨酸、D-亮氨酸、D-tBu-丝氨酸、D-Trp 或其他活性 D 氨基酸，在第 10 位含有乙酰胺、偶氮甘氨酰胺或其他甘氨酰胺。还提供了 D-Arg（6）-鸡 II GnRH-乙酰胺、D-Arg（6）-鸡 II GnRH-氮-甘氨酰（10）-酰胺、D-Arg（6）-鲑鱼 GnRH 乙酰胺和 D-Arg（6）-鲑鱼 GnRH-氮-甘氨酰（10）-酰胺类似物，并显示出与绒毛膜 GnRH、卵巢、子宫内膜、输卵管、子宫、前列腺和睾丸受体的优先结合。卵巢和子宫内膜的生物活性高于垂体。这些非哺乳动物 GnRH 类似物可用于药物制剂，特别是在各种治疗方法中用作避孕药或性交后避孕药。这些非哺乳动物 GnRH 类似物还可用于药物制剂，在临床上以极低剂量和脉冲方式给药时可用于维持妊娠，还可用于治疗子宫内膜异位症、卵巢囊肿和卵巢白膜瘤。另一方面，非哺乳动物 GnRH 类似物可用作黄体溶解剂。杂-甘氨酰（10）酰胺非哺乳动物类似物是作为本发明的一部分提供的非哺乳动物 GnRH 类似物的其他实施方案。
• Implantation rates after in vitro fertilization, and treatment of infertility and early pregnancy loss with a nitric oxide donor or substrate alone or in combination with progesterone, and a method for contraception with nitric oxide inhibitors in combination with antiprogestins or other agents
  申请人：——

  公开号：US20020169205A1

  公开（公告）日：2002-11-14

  A method is provided for the improvement of implantation rates and/or pregnancy rates in a female mammal, comprising administering to a female mammal in whom pregnancy is desired an effective amount of (a) a nitric oxide synthase substrate, a nitric oxide donor, or both, optionally in combination with (b) a progestin, and, (c) optionally, in further combination with an estrogen. A method is also provided for fertility control for a female mammal, comprising administering to a female mammal in whom pregnancy is not desired and at risk for becoming pregnant an effective amount of nitric oxide synthase inhibitor in combination with an antiprogestin. Pharmaceutical compositions are also provided.

  本发明提供了一种提高雌性哺乳动物植入率和/或怀孕率的方法，包括向希望 怀孕的雌性哺乳动物施用有效量的以下物质 (a) 一氧化氮合酶底物、一氧化氮供体或两者，可选择与以下物质结合使用 (b) 一种孕激素，以及 (c) 可选择与雌激素进一步结合使用。还提供了一种用于控制雌性哺乳动物生育力的方法，包括向不希望怀孕且有怀孕风险的雌性哺乳动物施用有效量的一氧化氮合酶抑制剂与抗孕激素。还提供了药物组合物。