阿萨可雌甾醇 | 313-05-3

• 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
• 中文名称: 阿萨可雌甾醇
• 中文别名: 阿扎胆醇；二氢胆甾醇
• 英文名称: Azacosterol
• 英文别名: (3S,8R,9S,10R,13S,14S,17S)-17-[3-(dimethylamino)propyl-methylamino]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
• CAS: 313-05-3
• 化学式: C₂₅H₄₄N₂O
• 分子量: 388.6
• InChiKey: FMTFZYKYVZBISL-HUVRVWIJSA-N

物化性质

• 熔点：
  146-148°
• 比旋光度：
  D -54.5°
• 沸点：
  490.6±40.0 °C(Predicted)
• 密度：
  1.04

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  26.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。
• [EN] FOSFLUCONAZOLE DERIVATIVES, SYNTHESIS, AND USE IN LONG ACTING FORMULATIONS<br/>[FR] DÉRIVÉS DE FOSFLUCONAZOLE, SYNTHÈSE, ET UTILISATION DANS DES FORMULATIONS À LONGUE DURÉE D'ACTION
  申请人：SEPS PHARMA N V

  公开号：WO2010105910A1

  公开（公告）日：2010-09-23

  The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.

  该发明涉及公式(I)的化合物及其盐、N-氧化物、季铵盐和立体异构体，其中R1至R8如权利要求中所定义。该发明进一步涉及用于制备公式(I)化合物的前体和方法。该发明还涉及公式(I)的化合物，用于作为药物，特别是用于预防或治疗真菌感染。
• PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF
  申请人：Barre Lionel

  公开号：US20080021070A1

  公开（公告）日：2008-01-24

  The invention relates to compounds of formula (I): Wherein Z, R 3 to R 9 are as described herein. The invention also relates to methods of preparation of compounds of formula (I) and intermediates thereof. The compounds of this invention are active at CB1 cannabinoid receptor site, and are therefore, useful as pharmaceutical agents in treating a variety of diseases caused by the effects of CB1 cannabinoid receptors.

  这项发明涉及式(I)的化合物： 其中Z，R3至R9如本文所述。该发明还涉及制备式(I)化合物及其中间体的方法。本发明的化合物在CB1大麻素受体位点具有活性，因此在治疗由CB1大麻素受体效应引起的各种疾病中作为药用剂是有用的。
• AMINE POLYMERS FOR USE AS BILE ACID SEQUESTRANTS
  申请人：Connor Eric

  公开号：US20140356316A1

  公开（公告）日：2014-12-04

  The present invention provides crosslinked amine polymers effective for binding and removing bile salts from the gastrointestinal tract. These bile acid binding polymers or pharmaceutical compositions thereof can be administered to subjects to treat various conditions, including hypercholesteremia, diabetes, pruritus, irritable bowel syndrome-diarrhea (IBS-D), bile acid malabsorption, and the like.

  本发明提供了交联胺聚合物，用于有效地结合和清除胆盐从胃肠道。这些胆酸结合聚合物或其药物组合物可以被用于治疗各种疾病，包括高胆固醇血症、糖尿病、瘙痒、肠易激综合征-腹泻（IBS-D）、胆酸吸收不良等。
• 1,5-DIARYLPYRROLE DERIVATIVES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS
  申请人：BARTH Francis

  公开号：US20080015245A1

  公开（公告）日：2008-01-17

  The invention relates to compounds having formula (I): Wherein X, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.

  该发明涉及具有以下结构式（I）的化合物：其中X，R1，R2，R3，R4，R5和R6如本文所定义。该发明还涉及一种制备所述化合物的方法以及在治疗中的应用。