CAS: 103377-41-9; N-(6,11-Dihydrodibenzo[b,E]Thiepin-11-yl)-4-(4-(4-Fluorophenyl)Piperazin-1-yl)Butanamide

📜6,11-二氢二苯并[b,E]噻频-11-胺置于sodium Iodide体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 9.0H,反应生成1-哌嗪丁酰胺,N-(6,11-二氢二苯并[b,E]噻庚英-11-基)-4-(4-氟苯基)-
参考文献:新型的钙拮抗剂.2. 11-[[[4-[4-(4-氟苯基)-1-哌嗪基]丁酰基]氨基]-6,11-二氢二苯并[b,E]-噻吩马来酸酯的合成及生物活性.
标题:新型的钙拮抗剂.2. 11-[[[4-[4-(4-氟苯基)-1-哌嗪基]丁酰基]氨基]-6,11-二氢二苯并[b,E]-噻吩马来酸酯的合成及生物活性.
摘要:合成了一系列[(ε-氨基链烷酰基)氨基]-6,11-二氢二苯并[b,E]噻吩和-5H-二苯并[a,D]环庚烯及相关化合物,并通过钙诱导的收缩来评估其钙拮抗活性.钾去极化的大鼠主动脉.二苯并三环体系的半经验分子轨道计算表明,钙拮抗活性随两个苯环平面之间的夹角的减小而增加.Am1净电荷计算表明,电桥部分的中性或正电荷分布对于活动是必要的.11-[[[4-[4-(4-氟苯基)-1-哌嗪基]丁酰基]氨基]-6,11-二氢二苯并[b,E]噻吩马来酸酯(16,Aj-2615)在口服自发性高血压大鼠(shr)中显示出比地尔硫卓和硝苯地平更缓和,更持久的降压作用.化合物16在大鼠的乙酰甲胆碱诱导的st升高和血管加压素诱导的st抑郁试验中也具有抗心绞痛作用.16至5H-二苯并[a,D]环庚烯(19,5-[[4-[4-(4-氟苯基)-1-哌嗪基]-丁酰基]氨基]-5H-二苯并[ A,D]环庚烯)对心
Doi:10.1021/jm00107A009

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:US-2005187222-A1
优先权日:1996-02-02
标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds
发明人：GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.