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    • 3. 发明授权
    • Anti-arrhythimic
5-endo-(3-indolecarbonyloxy)-N-[amino-(lower)alkyl]bicyclo[2,2,1]heptane
-2,3-di-endo-carboxylic acid imides
    • 抗心律不齐的5-内 - (3-吲哚羰基氧基)-N- {8氨基 - (低级)烷基{9双环{8,2,1 {9庚烷-2,3-二 - 内 - 羧酸酰亚胺
    • US3980668A
    • 1976-09-14
    • US594918
    • 1975-07-10
    • Ronald Leslie BuchananAlex Michael Jelenevsky
    • Ronald Leslie BuchananAlex Michael Jelenevsky
    • C07D209/42A61K31/40A61K31/403A61K31/404A61P9/06C07D209/76C07D403/12
    • C07D403/12A61K31/40
    • A series of 5-endo-(3-indolecarbonyloxy)-N-[amino-(lower)alkyl]bicyclo[2.2.1]heptane-2,3-di-endo-carboxylic acid imides having the formula ##SPC1##Wherein R.sup.1 is H, Cl, Br, F or (lower)alkyl, R.sup.7 is H or methyl, R.sup.2 and R.sup.3 are alike or different and each is H, Cl, Br, F, (lower)alkyl, nitro, CF.sub.3, OH or (lower)alkoxy, n is an integer of 2 to 4 inclusive and R.sup.4 and R.sup.5 are alike or different and each is H, (lower)alkyl or when taken together with the nitrogen a radical of the formula ##SPC2##In which R.sup.6 is (lower)alkyl; or a pharmaceutically acceptable acid addition salt thereof have been found to possess unique prophylactic and therapeutic activity as anti-arrhythmia agents. An example of such a compound possessing excellent activity is 5-endo-(3-indolecarbonyloxy)-N-(3-dimethylaminopropyl)bicyclo-[2.2.1]heptane-2,3-di-endo-carboxylic acid imide hydrochloride.
    • 具有式WHEREIN R1的一系列5-内 - (3-吲哚羰基氧基)-N- [氨基 - (低级)烷基]双环[2.2.1]庚-3,3-二 - 内 - 羧酸酰亚胺是H ,Cl,Br,F或(低级)烷基,R7是H或甲基,R2和R3是相同或不同的,分别是H,Cl,Br,F,(低级)烷基,硝基,CF3,OH或(低级) 烷氧基,n是2〜4的整数,R4和R5相同或不同,各自为H,(低级)烷基,或者当与氮一起时,R 6为(低级)烷基; 或其药学上可接受的酸加成盐已被发现具有独特的预防和治疗活性作为抗心律不齐剂。 具有优异活性的这种化合物的实例是5-内 - (3-吲哚羰基氧基)-N-(3-二甲基氨基丙基)双环[2.2.1]庚烷-2,3-二 - 内 - 羧酸酰亚胺盐酸盐。
    • 4. 发明授权
    • Anti-arrhythmic 5-endo-substituted oxy-N-(aminoloweralkyl)bicycle [2.2.2.]o
c
    • 抗心律不齐的5-端取代的氧-N-(氨基低级烷基)自行车{8 2.2.2。{9辛烷-2,3-二 - 内 - 羧酸酰亚胺
    • US3980667A
    • 1976-09-14
    • US555651
    • 1975-03-05
    • Richard Anthony PartykaHenry Michael HolavaAlex Michael Jelenevsky
    • Richard Anthony PartykaHenry Michael HolavaAlex Michael Jelenevsky
    • C07D209/76C07D307/77C07D209/48
    • C07D307/77C07D209/76
    • Series of 5-endo-benzoyloxy-N-[amino(lower)-alkyl]bicyclo[2.2.2]octane-2,3-di-endo-carboxylic acid imides, 5-endo-(3-indolecarbonyloxy)-N-[amino-(lower)alkyl]bicyclo[2.2.2]octane-2,3-di-endo-carboxylic acid imides, 5-endo-n-substituted-carbamoyloxy-N-[amino(lower)alkyl]bicyclo[2.2.2]octane-2,3-di-endo-carboxylic acid imides and 5-endo-(1-naphthoyloxy)-N-[amino(lower)alkyl]bicyclo[2.2.2]octane-2,3-di-endo-carboxylic acid imides have been found to possess unique prophylactic and therapeutic activity as anti-arrhythmia agents. An example of such a compound possessing activity is 5-endo-(3-indolecarbonyloxy)-N-(3-dimethylaminopropyl)bicyclo[2.2.2]octane-2,3-di-endo-carboxylic acid imide hydrochloride of the formula ##SPC1##
    • 5-内 - 苯甲酰氧基-N- [氨基(低级) - 烷基]双环[2.2.2]辛烷-2,3-二 - 羧酸酰亚胺系列,5-内 - (3-吲哚羰基氧基)-N - [氨基 - (低级)烷基]双环[2.2.2]辛-2-基-2,3-二 - 内 - 羧酸酰亚胺,5-内 - 取代 - 氨基甲酰氧基-N- [氨基(低级)烷基]双环 [2.2.2]烷-2,3-二 - 内 - 羧酸酰亚胺和5-内 - (1-萘氧基)-N- [氨基(低级)烷基]双环[2.2.2]辛烷-2,3 已经发现二 - 内 - 羧酸酰亚胺作为抗心律失常药具有独特的预防和治疗活性。 这种具有活性的化合物的实例是式(I)的5-内 - (3-吲哚羰基氧基)-N-(3-二甲基氨基丙基)双环[2.2.2]咔啉-2,3-二 - 内 - 羧酸酰亚胺盐酸盐