CAS: 210101-16-9; N-(4-(2-Methyl-1,4,5,6-Tetrahydrobenzo[b]Imidazo[4,5-D]Azepine-6-Carbonyl)Phenyl)-[1,1'-Biphenyl]-2-Carboxamide

上下游产品

4'-(4-Bromo-5-Oxo-2,3,4,5-Tetrahydro-1H-1-Benzoazepine-1-Carbonyl)-2-Phenylbenzanilide 261787-69-3
4'-(5-Oxo-2,3,4,5-Tetrahydro-1H-1-Benzoazepine-1-Carbonyl)-2-Phenylbenzanilide 168626-54-8

📜4'-(5-Oxo-2,3,4,5-Tetrahydro-1H-1-Benzoazepine-1-Carbonyl)-2-Phenylbenzanilide置于氢溴酸,溴,Potassium Carbonate,溶剂黄146体系中,用 乙腈 用作溶剂,化学反应 2.5H,反应生成考尼伐坦
参考文献:V1A和v2受体的非肽精氨酸加压素拮抗剂:4-(1,4,5,6-四氢咪唑并[4,5-D] [1]苯并氮杂-6-羰基)苯并尼衍生物和4'的合成和药理特性-(5,6-二氢-4H-噻唑并[5,4-D] [1]苯并氮杂-6-羰基)苯并尼衍生物.
标题:V1A和v2受体的非肽精氨酸加压素拮抗剂:4-(1,4,5,6-四氢咪唑并[4,5-D] [1]苯并氮杂-6-羰基)苯并尼衍生物和4'的合成和药理特性-(5,6-二氢-4H-噻唑并[5,4-D] [1]苯并氮杂-6-羰基)苯并尼衍生物.
摘要:精氨酸加压素(avp)主要在外周具有双重作用,即通过v1A和v2受体进行血管收缩和水分吸收.它可能在多种疾病中起作用,包括充血性心力衰竭(chf),高血压,肾脏疾病,水肿和低钠血症.我们基于对v1A和v2受体的阻断可能对chf患者有益的假设,尝试开发出一系列针对v1A和v2受体的口服活性avp拮抗剂.在此报告中,一系列与4'-(1,4,5,6-四氢咪唑并[4,5-D] [1]苯并氮杂氮杂-6-羰基)苯甲酰苯胺和4'-(5,6-合成了二氢-4H-噻唑并[5,4-D] [1]苯并ze庚因-6-羰基)苯甲酰苯并检查了其对v1A和v2受体的avp拮抗剂活性.结果发现4'-(1,4,5,6-四氢咪唑并[4,5-D] [1]苯并ze庚因-6-碳基)-2-苯基苯甲腈衍生物对v1A和v2受体均显示强效结合亲和力.特别地,显示了4'-(2-甲基-1,4,5,6-四氢咪唑并[4,5-D] [1]苯并氮杂-6-
Doi:10.1248/cpb.48.21

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:CN-105481863-A
优先权日:2015-12-09
标题:Synthesis of 2-methyl-6-(4-methylbenzenesulfonyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine*

专利号:CN-105481863-B
优先权日:2015-12-09
标题:Synthesis of 2-methyl-6-(4-methylbenzenesulfonyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine*

专利号:US-2008280877-A1
优先权日:2007-05-10
标 题:Azetidines
发明人：DACK KEVIN NEIL; SKERRATT SARAH ELIZABETH; YEAP SIEW KUEN
权利人:PFIZER
摘要:The invention relates to EP2 antagonist azetidines of formula (I) n n n n n n n n n n wherein Ar, R 1 , X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.

专利号:US-2010256109-A1
优先权日:2007-11-15
标 题 :Azetidines As EP2 Antagonists
发明人：SKERRATT SARAH ELIZABETH; DACK KEVIN NEIL
权利人:SKERRATT SARAH ELIZABETH; DACK KEVIN NEIL
摘要:The present invention relates to a class of EP2 antagonistazetidines of general formula (I), wherein the variables and substituents are as defined herein, and especially to EP2 antagonist compounds, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids (leiomyomata) and to intermediates usefulin their synthesis and to compositions containing them.