CAS: 137975-06-5; N-[4-[5-(Dimethylamino)-2,3,4,5-Tetrahydro-1-Benzazepine-1-Carbonyl]Phenyl]-2-Methylbenzamide

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CAS号933-88-0 邻甲基苯甲酰氯 | CAS号122-04-3 对硝基苯甲酰氯 | CAS号155061-62-4 5-二甲胺基-2,3,4,5-... | CAS号181210-18-4 2,3,4,5-Tetrahy...

5-Dimethylamino-1-(4-Nitro-Benzoyl)-2,3,4,5-Tetrahydro-1H-Benzoazepine置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 乙醇,二氯甲烷 用作溶剂,25.0 °C,101.33 Kpa 条件下,反应 5.5H,反应生成莫扎伐普坦
参考文献:口服活性非肽加压素v2受体拮抗剂:一系列新的1-[4-(苯甲酰基氨基)苯甲酰基]-2,3,4,5-四氢-1H-苯并ze庚因和相关化合物.
标题:口服活性非肽加压素v2受体拮抗剂:一系列新的1-[4-(苯甲酰基氨基)苯甲酰基]-2,3,4,5-四氢-1H-苯并ze庚因和相关化合物.
摘要:本文介绍了一系列新型的非肽加压素v2受体拮抗剂.已经证明1-[4-(苯甲酰基氨基)苯甲酰基]-2,3,4,5-1H-苯并ze庚因和1-[4-(苯甲酰基氨基)苯甲酰基]-2,3,4,5-1H-1,5-苯二氮卓类药物对v2(和v1A)受体具有很高的亲和力.在1-[4-(苯甲酰基氨基)苯甲酰基]-2,3,4,5-1H-苯并ze庚因系列中,已证明在苯并ze庚因环上具有烷基氨基的化合物具有口服活性.末端苯甲酰基环邻位的亲脂性基团对于高v2受体亲和力和口服活性均很重要.基于这些有利的性质,已经开始将31B用作口服和静脉内水族药物的临床试验.
Doi:10.1021/jm960133O

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-101613317-A
优先权日:2009-06-17
标题 :The synthesis technique of the mozavaptan of treatment congestive heart failure (CHF)