申请人:SHIONOGI SEIYAKU KABUSHIKI KAISHA
trading under the name of
SHIONOGI & CO. LTD.
公开号:EP0304330A1
公开(公告)日:1989-02-22
Compounds of the formula:
(wherein R is phenoxy optionally substituted by a halogen, methoxy, or methyl group,
one of A and B is
and the other is
R1 is hydrogen or C1-C5 alkyl;
Z1 is phenyl, benzyl. or isoxazolyl each optionally substituted by a halogen, methoxy, or methyl group; Z2 is hydrogen, C1-C5 alkyl, C2-C5 alkenyl, or phenyl optionally mono-, di-, or tri-substituted by a halogen, methoxy, or methyl group; or Z1 and Z2 taken together with the adjacent nitrogen atom may form 5-membered heterocyclic group: Z3 is Ci-C5 hydroxyalkyl, di(C1-C5 alkyl)sulfamoyl, 6-membered heterocyclic group, phenyl, benzyl, or phenylsulfonyl each phenyl moiety of the last three members being optionally substituted by a halogen, methoxy, or methyl group: Z4 is phenyl optionally substituted by a halogen, methoxy, or methyl group or 5- or 6-membered heterocyclic group which is optionally substituted by a halogen, methoxy, or methyl group and which can be optionally condensed with a benzene ring; Z5 is thienyl or phenyl each optionally substituted by a halogen, methoxy, or methyl group; Z6 is thienyl or phenyl each optionally substituted by a halogen, methoxy, or methyl group; m is an integer from 0 to 2; n is an integer from 2 to 3), and their acid addition salts may be useful as drugs for senile dementia, or as psychotropic, or antiamnesia agents.
式中的化合物:
(其中 R 是任选被卤素、甲氧基或甲基取代的苯氧基、
A 和 B 中的一个是
另一个是
R1 是氢或 C1-C5 烷基;
Z1 是苯基、苄基或
异恶唑基,各自任选被卤素、甲氧基或甲基取代;Z2 是氢、C1-C5 烷基、C2-C5 烯基或苯基,任选被卤素、甲氧基或甲基单取代、二取代或三取代;或 Z1 和 Z2 与相邻的氮原子一起可形成 5 元杂环基团:Z3 是 Ci-C5 羟烷基、二(C1-C5 烷基)
氨基磺酰基、6 元杂环基团、苯基、苄基或苯磺酰基,后三个成员中的每个苯基可任选被卤素、甲氧基或甲基取代:Z4 是任选被卤素、甲氧基或甲基取代的苯基,或任选被卤素、甲氧基或甲基取代且可任选与苯环缩合的 5 或 6 元杂环基团; Z5 是
噻吩基或苯基,各自任选被卤素、甲氧基或甲基取代;Z6 是
噻吩基或苯基,各自任选被卤素、甲氧基或甲基取代;m 是 0 至 2 的整数;n 是 2 至 3 的整数),它们的酸加成盐可用作治疗老年痴呆症的药物,或用作精神药物或抗失眠药物。