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    Amine derivatives
    6.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号：US5023378A

    公开(公告)日：1991-06-11

    申请号：US418208

    申请日：1989-10-06

    申请人： Michael D. Dowle ,  David Middlemiss ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts

    发明人： Michael D. Dowle ,  David Middlemiss ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts

    IPC分类号： C07C323/25

    CPC分类号： C07C323/25

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable acid addition salts, metabolically labile esters and solvates thereof in whichR.sup.1 represents a halogen atom or a methyl, ethyl, n-propyl or n-butyl group;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen atoms or one or two of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent a methy or ethyl group;X represents a C.sub.4-7 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl or hydroxyl groups; or optionally containing one or two double or triple bonds; or optionally interrupted by an oxygen or sulphur atom, or by a sulphone (--SO.sub.2 --) or urea (--NHCONH--) group; andY represents a phenyl ring optionally carrying one to three substituents selected from hydroxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino, carboxamido, C.sub.1-4 alkylsulphonylamino and nitro groups and halogen atoms with the proviso that when X is a C.sub.4-7 alkylene chain optionally containing one double bond then Y cannot represent phenyl or phenyl carrying one substituent which is halogen.The compounds according to the invention decrease total peripheral vascular resistance, increase cardiac output and produce a fall in blood pressure. They may be used in the treatment or prophylaxis of renal insuficiency and cardiovascular disorders such as hypertension, ischaemic heart disease or heart failure, for example acute or congestive heart failure.

    摘要翻译： 本发明提供通式（I）的化合物及其生理学上可接受的酸加成盐，其代谢不稳定的酯及其溶剂合物，其中R 1表示卤素原子或甲基，乙基，正丙基或正丁基 组; R2，R3，R4和R5各自表示氢原子，R2，R3，R4和R5中的一个或两个表示甲基或乙基; X表示任选被一个或多个C 1-4烷基或羟基取代的C 4-7亚烷基链; 或任选地含有一个或两个双键或三键; 或任选被氧或硫原子中断，或由砜（-SO 2 - ）或脲（-NHCONH-）基团中断; 并且Y表示任选地携带一至三个选自羟基，C 1-4烷基，C 1-4烷氧基，氨基，甲酰氨基，C 1-4烷基磺酰基氨基和硝基和卤素原子的取代基的苯环，条件是当X为C 4- 7亚烷基链任选地含有一个双键，则Y不能代表携带一个是卤素取代基的苯基或苯基。 根据本发明的化合物降低总周围血管阻力，增加心输出量并产生血压下降。 它们可用于治疗或预防肾功能不全和心血管疾病如高血压，缺血性心脏病或心力衰竭，例如急性或充血性心力衰竭。