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    • 2. 发明授权
    • Pyrimidinedione derivatives and antiarrythmic agents containing the same
    • 嘧啶二酮衍生物和含有它们的抗焦虑剂
    • US5308848A
    • 1994-05-03
    • US927738
    • 1992-08-12
    • Michihiko MiyamotoTsutomu KatakamiNobuya KawauchiTadahito NoboriJoji KamiyaMasaaki Ishii
    • Michihiko MiyamotoTsutomu KatakamiNobuya KawauchiTadahito NoboriJoji KamiyaMasaaki Ishii
    • C07D239/54C07D239/545C07D401/12A61K31/505C07D239/10
    • C07D239/545C07D401/12
    • A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a linking structure comprising an alkyl chain containing two nitrogen atoms. This linking structure is represented by ##STR1## [wherein A is --(CH.sub.2).sub.n --, --CO-- or --O--(CH.sub.2).sub.m --; each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.1 and R.sup.2 may be so linked with each other as to make an alkylene chain and thus form a heterocyclic structure; R.sup.5 is a halogen atom, a hydroxyl group, a lower alkyloxycarbonyl group, a lower alkyloxy group which may be substituted by a lower alkyloxy group, or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.5 may be so linked with R.sup.1 as to make an alkylene chain and thus form a heterocyclic structure; n is 0, 1, 2 or 3 (when R.sup.5 is the hydroxyl group, n.noteq.0); m is 0, 1, 2 or 3; and k is 0, 1, 2 or 3 (however, a compound in which A is --O--(CH.sub.2).sub.m -- and R.sup.5 is the hydroxyl group is excluded from the pyrimidinedione derivative)]. The pyrimidinedione derivative and its acid addition salt are useful for a medical treatment of cardiac arrhythmias.
    • 嘧啶二酮衍生物化合物具有其中苯基部分和嘧啶二酮部分通过包含含有两个氮原子的烷基链的连接结构连接的碱性主链。 该连接结构由表示,其中A是 - (CH 2)n - , - CO-或-O-(CH 2)m - ; R 1和R 2各自独立地为氢原子或可以被羟基取代的低级烷基,或者R 1和R 2可以相互连接形成亚烷基链,从而形成杂环结构; R5是卤素原子,羟基,低级烷氧基羰基,可被低级烷氧基取代的低级烷氧基或可被羟基取代的低级烷基,或R5可以与 R1形成亚烷基链,从而形成杂环结构; n是0,1,2或3(当R5是羟基时,n是等于0); m为0,1,2或3; 并且k为0,1,2或3(然而,其中A为-O-(CH 2)m - 且R 5为羟基的化合物不包括在嘧啶二酮衍生物中]]。 嘧啶二酮衍生物及其酸加成盐可用于治疗心律失常。
    • 9. 发明授权
    • Pyridazinone derivatives
    • 哒嗪酮衍生物
    • US4639451A
    • 1987-01-27
    • US504039
    • 1983-06-03
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaJoji KamiyaYasuhito TanakaTakuo Nakano
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaJoji KamiyaYasuhito TanakaTakuo Nakano
    • C07D237/04C07D401/12C07D403/12C07D405/12C07D409/12A61K31/50
    • C07D401/12C07D237/04C07D403/12C07D405/12C07D409/12
    • This invention relates to pyridazinone derivatives of the general formula: ##STR1## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR2## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.5 for a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a benzoyl or a benzyloxycarbonyl group, and R.sup.3 and R.sup.4 may be combined to form a grouping of the formula: ##STR3## which forms a ring), or (iii) a grouping of the formula: ##STR4## (wherein R.sup.6, R.sup.7 and R.sup.8 each stand for a hydrogen atom or a lower alkyl group, B is an oxygen atom or a sulfur atom, R.sup.9 stands for a hydrogen atom or a lower alkanoyl group, and n is 0 or 1)].
    • PCT No.PCT / JP82 / 00415 Sec。 371日期:1983年6月3日 102(e)日期1983年6月3日PCT提交1982年10月20日PCT公布。 第WO83 / 01447号公报 日本1983年4月28日。本发明涉及以下通式的哒嗪酮衍生物:其中R1代表氢原子或低级烷基; R2为氢原子或低级烷基; A为(i)选自苯环,呋喃环,噻吩环和吡啶环的环(其中1-3个取代基或选自氨基,硝基,低级烷酰基氨基,羟基, 低级烷酰氧基,氨磺酰基和卤素原子可以存在),或(ii)下式的基团:其中R3代表氢原子,低级烷基,苯基(低级)烷基,羟基苯基 (低级)烷基,低级烷基巯基(低级)烷基,苄基巯基(低级)烷基,胍基(低级)烷基,硝基胍基(低级)烷基,吲哚基(低级)烷基,氨基甲酰基 低级)烷基或羧基(低级)烷基,R4表示氢原子或低级烷基,R5表示氢原子,低级烷基,低级链烷酰基,苯甲酰基或苄氧基羰基,R3和 R4可以组合以形成下式的分组:形成环的),或(iii)下式的分组:( 其中R6,R7和R8各自代表氢原子或低级烷基,B是氧原子或硫原子,R9代表氢原子或低级烷酰基,n是0或1)]。