Bedoradrine sulfate | 194785-31-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: Bedoradrine sulfate
• 英文别名: 2-[[(7S)-7-[[(2R)-2-hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl)phenyl]ethyl]amino]-5,6,7,8-tetrahydronaphthalen-2-yl]oxy]-N,N-dimethylacetamide;sulfuric acid
• CAS: 194785-31-4
• 化学式: C48H66N4O14S
• 分子量: 955.1
• InChiKey: VPCOODFYDJWLHD-YMZXMBPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  67
• 可旋转键数：
  18
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  288
• 氢给体数：
  10
• 氢受体数：
  16

反应信息

• 作为产物：
  描述：

  贝多拉君 以87的产率得到Bedoradrine sulfate
  参考文献：
  名称：

  3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives

  摘要：

  本发明涉及3,4-二取代苯乙醇氨基四环戊二酰胺衍生物，其通式表示为：##STR1## （其中A表示较低的烷基链；B表示氨基、二（较低烷基）氨基或3至7环的脂环氨基，该环中可能含有一个氧原子；n是1或2的整数；标有*的碳原子表示R构型、S构型或它们的混合物中的一个碳原子；标有（S）的碳原子表示S构型的碳原子），以及其药学上可接受的盐。这些衍生物具有选择性β2-肾上腺素能受体刺激作用，能减轻心脏的负担，如心动过速，并可用作威胁性流产和早产的预防剂、支气管扩张剂、以及泌尿结石疼痛缓解和结石排除剂。

  公开号：

  US06133266A1

文献信息

• 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：US06133266A1

  公开（公告）日：2000-10-17

  The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.

  本发明涉及3,4-二取代苯乙醇氨基四环戊二酰胺衍生物，其通式表示为：##STR1## （其中A表示较低的烷基链；B表示氨基、二（较低烷基）氨基或3至7环的脂环氨基，该环中可能含有一个氧原子；n是1或2的整数；标有*的碳原子表示R构型、S构型或它们的混合物中的一个碳原子；标有（S）的碳原子表示S构型的碳原子），以及其药学上可接受的盐。这些衍生物具有选择性β2-肾上腺素能受体刺激作用，能减轻心脏的负担，如心动过速，并可用作威胁性流产和早产的预防剂、支气管扩张剂、以及泌尿结石疼痛缓解和结石排除剂。
• PREVENTIVE OR REMEDY FOR INTRAUTERINE LATE EMBRYONIC DEVELOPMENT OR PREGNANCY TOXEMIA
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1591115A1

  公开（公告）日：2005-11-02

  The present invention provides agents for the prevention or treatment of intrauterine growth retardation or gestational toxicosis comprising as an active ingredient phenylethanolaminotetralin derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof such as a sulfate salt thereof, which exert a remarkable improving effect on fetal weight loss and static gangrene in the tip of fetal extremities and a remarkable improving effect on elevation of maternal urinary protein and plasma triglyceride level with ease of anxiety on palpitation of dams or the like. Examples of administration forms include, for example, tablets, capsules, injections and so on. As diseases to be treated, for example, asymmetrical intrauterine growth retardation and hyperlipidemia associated with gestational toxicosis are specially preferable.

  本发明提供了用于预防或治疗宫内发育迟缓或妊娠中毒症的制剂，其有效成分包括式（I）代表的苯乙醇胺四氢萘衍生物或其药学上可接受的盐，如其硫酸盐，该制剂对胎儿体重减轻和胎儿四肢末端的静止性坏疽有显著的改善作用，对母体尿蛋白和血浆甘油三酯水平的升高有显著的改善作用，对母体的心悸等焦虑有缓解作用。 给药形式包括片剂、胶囊剂、注射剂等。作为要治疗的疾病，例如与妊娠中毒症有关的不对称宫内发育迟缓和高脂血症尤其可取。
• Gaba receptor mediated modulation of neurogenesis
  申请人：Braincells, Inc.

  公开号：EP2314289A1

  公开（公告）日：2011-04-27

  The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a GABA agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.

  本公开描述了通过刺激或增加神经发生来治疗中枢和周围神经系统疾病和病症的方法。本公开包括基于使用 GABA 制剂（可选择与一种或多种其他神经发生剂结合使用）的组合物和方法，以刺激或激活新神经细胞的形成。
• Modulation of neurogenesis by PDE inhibition
  申请人：Braincells, Inc.

  公开号：EP2377530A2

  公开（公告）日：2011-10-19

  The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a PDE agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.

  本公开描述了通过刺激或增加神经发生来治疗中枢和周围神经系统疾病和病症的方法。本公开包括基于使用 PDE 药剂（可选择与一种或多种其他神经发生剂结合使用）的组合物和方法，以刺激或激活新神经细胞的形成。
• Neurogenesis by modulating angiotensin
  申请人：Braincells, Inc.

  公开号：EP2377531A2

  公开（公告）日：2011-10-19

  The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.

  本发明描述了通过刺激或增加神经发生来治疗中枢和外周神经系统疾病和病症的方法。本发明包括基于调节血管紧张素活性以刺激或激活新神经细胞形成的组合物和方法。