Spiro substituted indanones and tetralones
    4.
    发明授权
    Spiro substituted indanones and tetralones 失效
    螺环取代的茚满酮和四氢萘酮

    公开(公告)号:US4322437A

    公开(公告)日:1982-03-30

    申请号:US795439

    申请日:1977-05-10

    摘要: The present invention relates to a compound of formula I, ##STR1## wherein A is straight chain alkylene of 2 to 4 carbon atoms, or straight chain alkenylene of 2 to 4 carbon atoms,n is 1, 2 or 3,R is hydrogen or halogen of atomic number from 9 to 35, andeither (i) R.sub.1 is a group of formula II, ##STR2## wherein R.sub.2 and R.sub.3, independently, are hydrogen or alkyl of 1 to 4 carbon atoms, andR.sub.4 is alkyl of 1 to 4 carbon atoms, alkoxyalkyl of 2 to 5 carbon atoms, alkylthioalkyl of 2 to 5 carbon atoms, phenylalkyl or phenoxyalkyl or phenylthioalkyl, wherein the alkyl moiety has from 1 to 3 carbon atoms, or phenyl, the phenyl ring of each of the last four radicals being unsubstituted or mono-substituted by, or disubstituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, hydroxy or halogen of atomic number from 9 to 35, andR.sub.5 is hydrogen,or (ii) R.sub.1 and R.sub.5 together with the nitrogen atom to which they are bound are (a) 2,2,6,6-tetramethylpiperidinyl, (b) 2,2,5,5-tetramethylpyrrolidinyl,or (c) piperazinyl substituted in the 4 position by alkyl of 1 to 4 carbon atoms or phenyl which is unsubstituted, or mono-substituted by, or di-or tri-substituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or halogen of atomic number from 9 to 35,useful as anti-hypertensives.

    摘要翻译: 本发明涉及式Ⅰ化合物,其中A为2至4个碳原子的直链亚烷基或2至4个碳原子的直链亚烯基,n为1,2或3,R为氢 或原子序数为9至35的卤素,和(i)R 1是式II,其中R 2和R 3独立地是氢或1-4个碳原子的烷基,R 4是 1至4个碳原子,2至5个碳原子的烷氧基烷基,2至5个碳原子的烷硫基烷基,苯基烷基或苯氧基烷基或苯硫基烷基,其中烷基部分有1至3个碳原子,或苯基, 最后四个基团是未取代的或被1至4个碳原子的烷基,1至4个碳原子的烷氧基单独取代或原子数为9至35的羟基或卤素单取代,R5为氢或( ii)R 1和R 5与它们所连接的氮原子一起是(a)2,2,6,6-四甲基哌啶基,(b)2,2, 或(c)在4位上被1至4个碳原子的烷基取代的哌嗪基或未被取代的或被1或2的烷基独立地被二取代或二取代或三取代的苯基取代的哌嗪基 4个碳原子,1至4个碳原子的烷氧基或9至35个原子序数的卤素,可用作抗高血压药。

    Alkylthiophenoxyalkylamines and the pharmaceutical use thereof
    10.
    发明授权
    Alkylthiophenoxyalkylamines and the pharmaceutical use thereof 失效
    烷基噻吩氧基烷基胺及其药物用途

    公开(公告)号:US4147805A

    公开(公告)日:1979-04-03

    申请号:US928668

    申请日:1978-07-28

    申请人: Duane F. Morrow

    发明人: Duane F. Morrow

    CPC分类号: C07D409/12

    摘要: A new class of alkylthiophenoxyalkylamine derivatives and methods for preparation are described. The compounds have vasodilating and antispasmodic activity, inhibit blood platelet aggregation and are substantially free of beta-adrenergic blocking effects. They are particularly valuable in the treatment of disease states responsive to vasodilation such as obstructive peripheral vascular diseases and cerebral vascular deficiencies. Representative and preferred embodiments of the invention are N-[3-[4-(methylthio)phenoxy]propyl]octylamine and N-[3-[4-(1-methylethyl)thio]phenoxy]-propyl]octylamine.

    摘要翻译: 描述了一类新的烷基硫代氧烷基胺衍生物及其制备方法。 该化合物具有血管扩张和解痉药活性,抑制血小板聚集并且基本上不含β-肾上腺素能阻滞作用。 它们在治疗响应于血管舒张的疾病状态(例如阻塞性外周血管疾病和脑血管缺陷)方面特别有价值。 本发明的代表性和优选的实施方案是N- [3- [4-(甲硫基)苯氧基]丙基]辛胺和N- [3- [4-(1-甲基乙基)硫代]苯氧基] - 丙基]辛胺。