继续进行有关一系列新的角和线性偶氮双环和三环衍生物的抗病毒活性的研究计划,现在我们简化并修饰了4-氯-2-(4-硝基苯基)-3 H-咪唑[4,通过消除中心环或咪唑环的打开,先前产生活性最高的衍生物的5- g ]喹啉1分别获得各种咪唑并吡啶和N-亚苄基喹啉胺。 标题化合物中的细胞毒性和抗病毒活性对两个DNA病毒科的代表,孔中作为对含有单链,无论是正链(单链RNA的RNA病毒科的代表基于细胞的测定中测试+)或负义单链RNA(-)和双链基因组(dsRNA)。一些咪唑并[4,5- b ]吡啶以新衍生物的形式出现,在2至16μM的浓度范围内具有抗痘苗病毒(VV)的抗病毒活性。特别是,化合物2b的功效比用作参考药物的西多福韦强约10倍。同样,咪唑并[4,5- c ]吡啶和N-亚苄基喹啉胺衍生物在1.2至28μM的浓度范围内具有抗牛病毒性腹泻病毒(BVDV)的活性。所有上述化合物1,图3a和3f中显示出EC
Novel 2-Phenyl-Imidazo[4,5-B]Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase for the Treatment of Dementia and Neurodegenerative Disorders
申请人:Arvidsson Per I.
公开号:US20080255106A1
公开(公告)日:2008-10-16
Compounds of formula I
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are as defined in the specification, as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Novel Imidazo [4,5-b] Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase 3 for Use in the Treatment of Dementia and Neurodegenerative Disorders
申请人:Arvidsson Per I
公开号:US20080255085A1
公开(公告)日:2008-10-16
Compounds of formula I
wherein X is
or Y;
and wherein A, Y, R
1
, R
2
, R
3
, R
4
and R
5
are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines
assays for cytotoxicity and antiviralactivityagainst representatives of two DNA virus families as wells as against representatives of RNA virus families containing single-stranded, either positive-sense (ssRNA+) or negative-sense (ssRNA−), and double-stranded genomes (dsRNA). Some imidazo[4,5-b]pyridines emerged as new derivatives endowed with antiviralactivityagainst Vaccinia Virus (VV) at concentrations
继续进行有关一系列新的角和线性偶氮双环和三环衍生物的抗病毒活性的研究计划,现在我们简化并修饰了4-氯-2-(4-硝基苯基)-3 H-咪唑[4,通过消除中心环或咪唑环的打开,先前产生活性最高的衍生物的5- g ]喹啉1分别获得各种咪唑并吡啶和N-亚苄基喹啉胺。 标题化合物中的细胞毒性和抗病毒活性对两个DNA病毒科的代表,孔中作为对含有单链,无论是正链(单链RNA的RNA病毒科的代表基于细胞的测定中测试+)或负义单链RNA(-)和双链基因组(dsRNA)。一些咪唑并[4,5- b ]吡啶以新衍生物的形式出现,在2至16μM的浓度范围内具有抗痘苗病毒(VV)的抗病毒活性。特别是,化合物2b的功效比用作参考药物的西多福韦强约10倍。同样,咪唑并[4,5- c ]吡啶和N-亚苄基喹啉胺衍生物在1.2至28μM的浓度范围内具有抗牛病毒性腹泻病毒(BVDV)的活性。所有上述化合物1,图3a和3f中显示出EC