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    • 4. 发明授权
    • Spiro substituted indanones and tetralones
    • 螺环取代的茚满酮和四氢萘酮
    • US4322437A
    • 1982-03-30
    • US795439
    • 1977-05-10
    • Richard BertholdTrevor G. Payne
    • Richard BertholdTrevor G. Payne
    • A61K31/12A61K31/40A61K31/445A61K31/495A61P3/08A61P7/10A61P9/10A61P9/12C07C213/02C07C213/08C07C217/38C07D207/06C07D211/14C07D241/12C07D295/092A01N37/30A01N33/02C07C93/06
    • C07D295/088C07C217/38C07C2103/94Y10S514/821Y10S514/866
    • 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.
    • 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。