甲基麦角胺 | 22336-84-1

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 麦角林及其衍生物
• 中文名称: 甲基麦角胺
• 英文名称: metergotamine
• 英文别名: 5'α-benzyl-12'-hydroxy-1,2'-dimethyl-ergotamane-18,3',6'-trione；5'α-Benzyl-12'-hydroxy-1,2'-dimethyl-ergotaman-18,3',6'-trion；(6aR,9R)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-4,7-dimethyl-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-9-carboxamide
• CAS: 22336-84-1
• 化学式: C₃₄H₃₇N₅O₅
• 分子量: 595.698
• InChiKey: SZUQJDJBJHBVBO-CTTKVJGISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  44
• 可旋转键数：
  4
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  5'α-benzyl-12'-hydroxy-1,2'-dimethyl-8βH-ergotamane-18,3',6'-trione 在 甲醇 、 硫酸 、 溶剂黄146 作用下， 生成 甲基麦角胺
  参考文献：
  名称：

  麦角酸环系统的取代I.吲哚氮的取代。43.关于麦角生物碱的交流

  摘要：

  描述了麦角酸和二氢麦角酸化合物的1-取代产物的生产和性质。引入了以下易于再次水解分离的残基：乙酰基，乙酰乙酰基，羟甲基，乙酰氧基甲基，二甲基氨基甲基，哌啶子基甲基。

  DOI：

  10.1002/hlca.19570400619

文献信息

• N-phenpropylcuclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
  申请人：——

  公开号：US20030105132A1

  公开（公告）日：2003-06-05

  The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C 1-6 alkoxy, —NR 2 R 3 or —NR 4 SO 2 R 5 ; X is the linkage —(CH 2 ) n — or —(CH 2 ) q —O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C 1-4 alkoxy; hydroxy; hydroxy(C 1-3 alkyl); C 3-7 cycloalkyl; carbocyclyl; heterocyclyl; or by C 1-4 alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R 8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5 - or 6 -membered carbocyclic or heterocyclyic ring. 1

  该发明涉及用于治疗性功能障碍的化合物(I)的公式，其中R1是可选择取代的C1-6烷基，可选择取代的碳环烷基，可选择取代的杂环烷基，氢，C1-6烷氧基，—NR2R3或—NR4SO2R5；X是连接基—(CH2)n—或—(CH2)q—O—（其中Y连接到氧原子）；其中连接基X中的一个或多个氢原子可以独立地被C1-4烷氧基，羟基，羟基(C1-3烷基)，C3-7环烷基，碳环烷基，杂环烷基或可选择取代的一个或多个氟或苯基的C1-4烷基替代；n为3、4、5、6或7；q为2、3、4、5或6；Y为苯基或吡啶基，每个基都可以被取代；或相邻碳原子上的两个R8基连同相互连接的碳原子可以形成一个可选择取代的5-或6-成员碳环或杂环环。
• New indazole and indolone derivatives and their use pharmaceuticals
  申请人：Allerton Norfor Charlotte Moira

  公开号：US20050267096A1

  公开（公告）日：2005-12-01

  The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.

  本发明提供了一类多巴胺激动剂的化合物，具体来说是一类选择性作用于D3而非D2的激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤醒障碍（FSAD），性欲不振障碍（HSDD；对性欲缺乏兴趣），女性性高潮障碍（FOD；无法达到高潮）；以及男性性功能障碍，特别是男性勃起功能障碍（MED）。本文提到的男性性功能障碍包括射精障碍，如早泄，无法达到高潮的无性感（无法达到高潮）或性欲障碍，如性欲不振（HSDD；对性欲缺乏兴趣）。这些化合物还可用于治疗神经精神障碍和神经退行性疾病。
• [EN] AMINOPYRIDINE DERIVATIVES AS SELECTIVE DOPAMINE D3 AGONISTS<br/>[FR] DERIVES D'AMINOPYRIDINE UTILISES COMME AGONISTES SELECTIFS DE LA DOPAMINE D3
  申请人：PFIZER LTD

  公开号：WO2005115985A1

  公开（公告）日：2005-12-08

  The present invention provides for compounds of formula (I) which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.

  本发明提供了一类化合物(I)，这些化合物是多巴胺激动剂的一类，更具体地说是一类选择性作用于D3而非D2的激动剂。这些化合物对于治疗和/或预防性功能障碍非常有用，例如女性性功能障碍（FSD），特别是女性性唤醒障碍（FSAD），性欲不振障碍（HSDD；对性欲缺乏兴趣），女性性高潮障碍（FOD；无法达到高潮）；以及男性性功能障碍，特别是男性勃起功能障碍（MED）。本文提到的男性性功能障碍包括射精障碍，如早泄，无法达到高潮（无法达到高潮）或性欲障碍，如性欲不振障碍（HSDD；对性欲缺乏兴趣）。这些化合物还可用于治疗神经精神障碍和神经退行性疾病。
• Acetyl-CoA carboxylase inhibitors
  申请人：Pfizer Inc.

  公开号：US20030187254A1

  公开（公告）日：2003-10-02

  Acetyl Coenzyme A Carboxylase inhibitors, pharmaceutical compositions containing such compounds and the use of such compounds to treat for example, Metabolic Syndrome including atherosclerosis, diabetes and obesity.

  乙酰辅酶A羧化酶抑制剂，含有此类化合物的药物组合物，以及使用此类化合物治疗代谢综合征，包括动脉粥样硬化、糖尿病和肥胖等疾病。
• 3-(1-[3-(1,3-Benzothiazol-6-yl)propylcarbamoyl]cycloalkyl)propanoic acid derivatives as NEP inhibitors
  申请人：Pfizer Inc

  公开号：US20040180941A1

  公开（公告）日：2004-09-16

  The invention relates to inhibitors of neutral endopeptidase enzyme (NEP), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of male and female sexual dysfunction, particularly female sexual dysfunction (FSD), especially wherein the FSD is female sexual arousal disorder (FSAD).

  该发明涉及中性内啮蛋白酶（NEP）抑制剂，其用途，制备过程，制备中使用的中间体以及含有该抑制剂的组合物。这些抑制剂在各种治疗领域中具有用途，包括治疗男性和女性性功能障碍，特别是女性性功能障碍（FSD），尤其是FSD为女性性唤醒障碍（FSAD）的情况。