CAS: 112727-80-7; Renzapride
该化合物是一种化学化合物,被归类为选择性血清素5-HT4受体激素5-HT4受体激素和5-HT3受体抗体抗体.主要调查的是其在胃肠紊乱中的潜在治疗用途,特别是增强胃肠功能和减轻与肠胃肠炎等条件有关的症状.Renzapride的分子结构具有管状环特征,有助于其药理活动.其行动机制包括刺激5-HT4受体,导致渗透性增加和改善肠道中转,同时堵塞5-HT3受体,有助于减少胃溃疡和不适.Renzapride已经研究其在所有临床环境中的功效和安全性特征,尽管并非所有市场都广泛存在.与许多药理学剂一样,潜在的副作用包括胃肠炎,头痛和头晕.
- 英文名称Renzapride
- 中文名称伦扎必利
- IUPAC名称4-amino-N-((1S,4R,5S)-1-azabicyclo[3.3.1]nonan-4-yl)-5-chloro-2-methoxybenzamide
- 其它别名Benzamide,4-amino-N-1-azabicyclo[3.3.1]non-4-yl-5-chloro-2-methoxy-, endo-(?à)-; 1-Azabicyclo[3.3.1]nonane,benzamide deriv.; Benzamide,4-amino-N-1-azabicyclo[3.3.1]non-4-yl-5-chloro-2-methoxy-, endo-; Renzapride; [(?à)-endo]-4-Amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide
- CAS编号112727-80-7
- MFCD编号:MFCD00869601
- FDA UNII编号:9073C0W4E9
- 分子式:C16H22ClN3O2分子量:323.82
- 产品CID: 159428
- 同类组份化合物CAS112727-80-7 (free base)109872-41-5 (HCl)
- 产品分类有机原料 → 苯类化合物 → 苯取代衍生物
物理性质
MSDS等安全信息
合成工艺路线路线简述
📜(Rs)-Endo-4-Amino-1-Azabicyclo[3.3.1]Nonane置于sodium Hydroxide,三乙胺体系中,用 乙醇,甲苯 用作溶剂,化学反应 6.0H,反应生成伦扎必利
参考文献:具有构象受限的侧链的取代苯甲酰胺.5. Azabicyclo [xyz]衍生物作为5-Ht4受体激动剂和胃动力刺激剂.
标题:具有构象受限的侧链的取代苯甲酰胺.5. Azabicyclo [xyz]衍生物作为5-Ht4受体激动剂和胃动力刺激剂.
摘要:描述了含氮杂双环[xyz]侧链的苯甲酰胺的合成及其5-Ht4受体激动剂和5-Ht3受体拮抗剂的性质.这些化合物被设计为模拟喹oli嗪和吲哚并idine啶的更高能构象.两种活动均获得了很高的效价,尽管尚不存在完全平行的sar.O和s的引入仅导致效力的边际差异,这对于5-Ht 3拮抗作用更为明显.将甲基α引入碱性氮导致5-Ht 4受体激动剂效力降低.鉴定了伦扎必利(5F)进行进一步评估,两种对映体均具有相同的药理学特征,氮杂三环9B也具有相同的药理学特征,其中三者分别包含两种独立对映体的空间体积.
Doi:10.1021/jm00058A004
海关参考信息
- 2903919090-氯苯
2905110000-甲醇
2908191000-对氯苯酚
2912110000-甲醛 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-7189852-B2
优先权日:2003-09-09
标题 :Synthesis
发明人：PALMER RICHARD MICHAEL JOHN; MEYERS NICHOLAS LESLIE; KNIGHT JOHN
权利人:ALIZYME THERAPEUTICS LTD
摘要:The present invention provides an improved process for the production of [(±)-endo]-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride, compositions thereof, and intermediates thereto.
专利号:WO-2005058896-A3
优先权日:2003-12-18
标 题:Synthesis of a polymorph of 4-amino-5-chloro-2-methoxy-n-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride hydrate
专利号:JP-2007514726-A
优先权日:2003-12-18
标题:Synthesis of polymorphs of 4-amino-5-chloro-2-methoxy-N- (1-azabicyclo [3.3.1] non-4-yl) benzamide hydrochloride hydrate
专利号:US-2023271983-A1
优先权日:2020-07-29
标题 :Functionalized isonitriles and products, preparation and uses thereof
发明人：SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
权利人:UNIV SANTIAGO COMPOSTELA
摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:AU-2004299338-A1
优先权日:2003-12-18
标 题 :Synthesis of a polymorph of 4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride hydrate
专利号:ZA-200604876-B
优先权日:2003-12-18
标题:Synthesis of a polymorph of 4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride hydrate
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
合成参考文献
参考文献:10.1007/bf00178714
摘要:Leung E, Pulido-Rios MT, Bonhaus DW, Pekins LA, Zeitung KD, Hsu SA, Clark RD, Wong EH, Eglen RM. Comparison of 5-HT4 receptors in guinea-pig colon and rat oesophagus: effects of novel agonists and antagonists. Naunyn Schmiedebergs Arch Pharmacol. 1996 Jul;354(2):145–56. doi: 10.1007/bf00178714.
参考文献:10.1007/s11894-015-0473-x
摘要:Wadhwa A, Camilleri M, Grover M. New and Investigational Agents for Irritable Bowel Syndrome. Curr Gastroenterol Rep. 2015 Dec;17(12):46. doi: 10.1007/s11894-015-0473-x.
参考文献:10.1007/bf00171343
摘要:Meulemans AL, Helsen LF, Schuurkes JA. The role of nitric oxide (NO) in 5-HT-induced relaxations of the guinea-pig stomach. Naunyn Schmiedebergs Arch Pharmacol. 1993 Oct;348(4):424–30. doi: 10.1007/bf00171343.
参考文献:10.2165/00003495-199753020-00003
摘要:Veyrat-Follet C, Farinotti R, Palmer JL. Physiology of chemotherapy-induced emesis and antiemetic therapy. Predictive models for evaluation of new compounds. Drugs. 1997 Feb;53(2):206–34. doi: 10.2165/00003495-199753020-00003.
参考文献:10.1007/bf02738530
摘要:Miranda A, Sood M. Treatment options for chronic abdominal pain in children and adolescents. Curr Treat Options Gastroenterol. 2006 Sep;9(5):409–15. doi: 10.1007/bf02738530.
📝 需求与反馈
尽可能描述清楚需求与问题信息
