CAS: 90961-53-8; Tedisamil

上下游产品

3,7-Bis(Cyclopropylmethyl)Spiro[3,7-Diazabicyclo[3.3.1]Nonane-9,1'-Cyclopentane]-2,4,6,8-Tetrone 90961-91-4

📜Spiro[cyclopentane-1,9'-(3,7-Diaza-Bicyclo[3.3.1]Nonane)]-2',4',6',8'-Tetraone置于lithium Aluminium Tetrahydride,Potassium Carbonate体系中,用 四氢呋喃,甲苯 作为反应溶剂,化学反应 4.0H,反应生成 替地沙米
参考文献:Synthesis,Pharmacological Characterization,And Quantitative Structure−activity Relationship Analyses Of 3,7,9,9-Tetraalkylbispidines: Derivatives With Specific Bradycardic Activity
标题:Synthesis,Pharmacological Characterization,And Quantitative Structure−activity Relationship Analyses Of 3,7,9,9-Tetraalkylbispidines: Derivatives With Specific Bradycardic Activity
摘要:A Series Of 3,7,9,9-Tetraalkyl-3,7-Diazabicyclo[3.3.1]Nonane Derivatives (Bispidines) Was Synthesized And Identified As Potential Antiischemic Agents. Pharmacological Experiments In Vitro As Well As In Vivo Are Described,And The Results Are Listed. For Selection Of Those Compounds Fitting Best To The Desired Profile Of A Specific Bradycardic Antianginal Agent-Decrease In Heart Rate Without Affecting Contractility And Blood Pressure-These Results Were Scored And Ranked. Quantitative Structure-Activity Relationship (Qsar) Analyses Were Performed And Discussed A Posteriori By Means Of Hansch,Nonelementary Discriminant And Factor Analysis To Get Insight Into The Molecular Features Determining The Biological Profile. Highly Significant Equations Were Obtained,Indicating Hydrophobic And Steric Effects. Both Pharmacological Ranking And Qsar Considerations Showed Compound 6 As The Optimum Within The Structural Class Under Investigation. Compound 6 (Tedisamil,Kc8857) Has Been Selected As The Most Promising Compound And Was Chosen For Further Pharmacological And Clinical Investigations As An Antiischemic Drug.
DOI:10.1021/jm970120Q

专利信息

专利号:US-6469065-B1
优先权日:1996-02-02
标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; 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.

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.