(2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their
pharmaceutical uses

    公开(公告)号:US4737495A

    公开(公告)日:1988-04-12

    申请号:US868986

    申请日:1986-05-30

    摘要: The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group, andHet represents a 5- or 6-membered heteroaromtic ring bonded via a carbon or nitrogen atom, which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, and onto which additionally a phenyl ring can be condensed, in which case the bond can also be via the phenyl nucleus, or an imidazo[1,2-a]pyridyl group wherein the carbon structure of the above-mentioned groups can be substituted by a methylenedioxy or ethylenedioxy group or can be mono- or disubstituted by a halogen atom or an alkyl, hydroxy, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkyl-carbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group, and at the same time any imino group present in the above-mentioned heteroaromatic groups can be substituted by an alkyl, phenylalkyl or phenyl group, the N-oxides and the acid addition salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly the effect of lowering heart rate and oxygen requirement of the heart. They can be used to treat sinus tachycardia or ischaemic heart disease.

    Substituted 2-phenylamino-2-imidazolines as bradycardiacs
    19.
    发明授权
    Substituted 2-phenylamino-2-imidazolines as bradycardiacs 失效
    取代的2-苯基氨基-2-咪唑啉作为心动过缓

    公开(公告)号:US4277487A

    公开(公告)日:1981-07-07

    申请号:US58165

    申请日:1979-07-17

    CPC分类号: C07D233/50

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a hydrogen atom, a chlorine atom, or a methyl group, with the proviso that not both R.sub.1 and R.sub.2 are hydrogen, andR represents a radical selected from the group consisting of --(CH.sub.2).sub.2 --C(CH.sub.3).dbd.CH.sub.2, --(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH.sub.2, --O--(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --C(CH.sub.3).dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH--CH.sub.3, ##STR2## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    摘要翻译: 其中R 1和R 2可以相同或不同,表示氢原子,氯原子或甲基,条件是不是R1和R2均不为氢,R表示 选自 - (CH 2)2 -C(CH 3)= CH 2, - (CH 2)2 -CH = CH 2,-O-CH 2 -CH = CH 2,-O-(CH 2)2 -CH = CH 2 ,-O-CH 2 -C(CH 3)= CH 2,-O-CH 2 -CH = CH-CH 3,其中其无毒的药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。