CAS: 106730-54-5; 5-(Imidazo[1,2-A]Pyridin-6-yl)-6-Methyl-2-Oxo-1,2-Dihydropyridine-3-Carbonitrile

上下游产品

CAS号106730-70-5 4-(dimethylamin... | CAS号107-91-5 氰乙酰胺 | CAS号1072-97-5 2-氨基-5-溴吡啶 | CAS号36052-24-1 6-氨基烟酸甲酯 | CAS号116355-16-9 咪唑并[1,2-a]吡啶-6-甲醛 | CAS号116355-20-5 6-(2-methyl-2-p... | CAS号116355-08-9 1-imidazo[1,2-a... | CAS号136117-69-6 咪唑并[1,2-a]吡啶-6-甲酸甲酯 | CAS号6188-23-4 6-溴-咪唑并[1,2-a]吡啶

6-溴-咪唑并[1,2-A]吡啶置于盐酸,Sodium Methylate,臭氧体系中,用 甲醇,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 13.0H,反应生成奥普力农
参考文献:Imidazo(1,2-A)Pyridines. I. Synthesis And Inotropic Activity Of New 5-Imidazo(1,2-A)Pyridinyl-2(1H)-Pyridinone Derivatives.
标题:Imidazo(1,2-A)Pyridines. I. Synthesis And Inotropic Activity Of New 5-Imidazo(1,2-A)Pyridinyl-2(1H)-Pyridinone Derivatives.
摘要:合成了一系列1,2-二氢-5-咪唑[1,2-α]吡啶基-2(1H)-吡啶酮,并评估了它们的正性变力活性.1,2-二氢-5-咪唑[1,2-α]吡啶-6-基-6-甲基-2-氧-3-吡啶腈(11A)盐酸盐一水合物(E-1020)被发现是一种强效且选择性的磷酸二酯酶iii抑制剂,以及一种长效,强效,口服活性正性变力剂.还制备了额外的咪唑[1,2-α]吡啶-2-基(3A),-3-基(16),-7-基(20)和-8-基(24A)化合物.将吡啶取代从2位改变到6位,静脉注射强心效力(Ed50)从52增加到23 μg/kg,增加了2倍,而在3-,7-或8位取代则降低了效力.在2位异构体中,引入卤素基团增强了活性,3-氯-1,2-二氢-5-(6-氟咪唑[1,2-α]吡啶-2-基)-6-甲基-2(1H)吡啶酮(3U)是该系列中最强效的(静脉ed50 11 μg/kg).E-1020目前正在开发用于治疗充血性心力衰竭.
Doi:10.1248/cpb.39.1556

专利信息

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:WO-2009035652-A1
优先权日:2007-09-13
标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-2014336387-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof

专利号:US-6472425-B1
优先权日:1997-10-31
标 题:Methods for treating female sexual dysfunctions
发明人：GARVEY DAVID S; SAENZ DE TEJADA INIGO
权利人:NITROMED INC
摘要:The present invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or releases nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.

专利号:EP-2727915-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof