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    • 7. 发明授权
    • Bicyclooctane derivatives
    • 双环辛烷衍生物
    • US4493846A
    • 1985-01-15
    • US243570
    • 1981-03-13
    • Keiichi OnoAkihiko SugieHajime KawakamiShunsuke SamiAtsuyuki KojimaJunki Katsube
    • Keiichi OnoAkihiko SugieHajime KawakamiShunsuke SamiAtsuyuki KojimaJunki Katsube
    • C07C69/708A61K31/557C07C29/09C07C29/128C07C35/32C07C43/196C07C47/198C07C47/277C07C51/00C07C51/08C07C59/125C07C59/13C07C59/31C07C59/46C07C59/62C07C67/00C07C67/08C07C69/734C07C405/00C07D211/32C07D295/08C07D295/18C07C69/608C07C61/13C07C61/28C07C69/616
    • C07C255/00C07C29/095C07C29/1285C07C35/32C07C405/0083C07C43/196C07D211/32C07B2200/07C07B2200/09C07C2102/24Y10S514/925
    • A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkynyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a group of the formula: --(CH.sub.2).sub.n --B (n is 1 or 2 and B is a C.sub.1 -C.sub.4 alkoxyl group, a C.sub.3 -C.sub.7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxyl group), A is a group of either one of the formulae: ##STR4## (R.sup.6 and R.sup.7 are each independently a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and ##STR5## m.sub.1 is 1 or 2 and m.sub.2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts threreof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.
    • 下式的化合物其中X1是游离或酯化的羧基,羟甲基,氰基,下式的基团:(R a和R b各自独立地是氢原子,C 1 -C 4 烷基,C3-C7环烷基,苄基,苯基,被卤素原子或C1-C4烷基取代的苯基,或者当与它们所连接的相邻氮原子一起时, 它们表示5至7元饱和杂环基)或下式的基团:(R a和R b各自如上所定义),Y是亚乙基或亚乙烯基,R 1是氢原子, 羟基或受保护的羟基,R2是氢原子或R1和R2,当它们一起表示在它们连接的碳原子之间形成双键的单键,R3是羟基或被保护的羟基 R4是氢原子或C1-C4烷基,R5是氢原子,C3-C8链烯基,C3-C8烷基 正丁基,C 1 -C 8烷基,C 3 -C 7环烷基或下式基团: - (CH 2)n B(n为1或2,B为C 1 -C 4烷氧基,C 3 -C 7环烷基 或任选被卤素原子取代的苯基或苯氧基,C 1 -C 4烷基,三氟甲基或C 1 -C 4烷氧基),A是以下基团之一: R 7各自独立地为氢原子或C 1 -C 4烷基),并且M 1为1或2,m 2为0,1或2,以及无毒的药学上可接受的盐。 所述化合物具有强的抗溃疡活性,可用于治疗胃肠溃疡。