(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.

    Process for the production of 8.alpha., 12-oxido-13,
14,15,16-tetranorlabdane
    9.
    发明授权
    Process for the production of 8.alpha., 12-oxido-13, 14,15,16-tetranorlabdane 失效
    生产8α,12-氧化-13,14,15,16-四硝基拉丹的方法

    公开(公告)号:US5811560A

    公开(公告)日:1998-09-22

    申请号:US836162

    申请日:1997-05-05

    IPC分类号: C07B41/04 C07D307/92

    CPC分类号: C07D307/92

    摘要: The invention pertains to a method for preparing 8-alpha,12-oxido-13,14,15,16, -tetranorlabdane by cyclizing a mixture of hydroxy-olefins (I)-(III. See the specification for their formulae. The cyclization is carried out in the presence of 10 to 100 wt. % acid, relative to the mixture of compounds (I) to (III).

    摘要翻译: PCT No.PCT / EP95 / 04225 Sec。 371日期:1997年5月5日 102(e)日期1997年5月5日PCT提交1995年10月27日PCT公布。 公开号WO97 / 14310PC 日期1996年5月17日本发明涉及通过环化羟基烯烃(I) - (III。)的混合物来制备8-α,12-氧化-13,14,15,16-四硝基拉丹丹的方法 相对于化合物(I)至(III)的混合物,环化反应在10至100重量%的酸存在下进行。

    Process for the production of 8 .alpha.,
12-oxido-13,14,15,16-tetranorlabdane
    10.
    发明授权
    Process for the production of 8 .alpha., 12-oxido-13,14,15,16-tetranorlabdane 失效
    生产8α,12-氧化-13,14,15,16-四硝基拉丹的方法

    公开(公告)号:US5670670A

    公开(公告)日:1997-09-23

    申请号:US647929

    申请日:1996-05-31

    CPC分类号: C07D307/92

    摘要: In a process for the production of 8.alpha.,12-oxido-13,14,15,16-tetranorlabdane by dehydration of 8.alpha.,12-dihydroxy-13,14,15,16-tetranorlabdane (diol), wherein the diol is subjected to cyclizing dehydration in the presence of 5 to 80% by weight, based on the diol, of at least one alumino layer silicate selected from K catalysts which have an acid charge of less than 100 mval/100 g.

    摘要翻译: PCT No.PCT / EP94 / 03889 Sec。 371日期:1996年5月31日 102(e)日期1996年5月31日PCT 1994年11月24日PCT PCT。 WO95 / 15320BC公开号 日期:1995年6月8日在8α,12-二羟基-13,14,15,16-四去甲二醇(二醇)脱水制备8α,12-氧化-13,14,15,16-四硝基拉丹的方法中, 其中所述二醇在基于二醇的5-80重量%存在下进行环化脱水的至少一种选自具有小于100m 2 / 100g酸性电荷的K催化剂的铝硅酸盐硅酸盐。