Anti-ischemic medicament
    1.
    发明授权
    Anti-ischemic medicament 失效
    抗缺血药物

    公开(公告)号:US5512572A

    公开(公告)日:1996-04-30

    申请号:US331607

    申请日:1994-11-22

    CPC分类号: A61K31/50

    摘要: A method for preventing or treating myocardial ischemia in a mammalian organism is disclosed. The compound 4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl!hydrazono!propanedinitrile or its enantiomer or a pharmaceutically acceptable salt there is administered to a mammalian organism in need of such prevention or treatment. The compound may be administered in its racemic form or in a form which is substantially free of the (+)-enantiomer or substantially free of the (-)-enantiomer.

    摘要翻译: PCT No.PCT / FI93 / 00191 Sec。 371日期:1994年11月22日 102(e)日期1994年11月22日PCT提交1993年5月5日PCT公布。 第WO93 / 21921号公报 日本11月11日,日本公开了一种预防或治疗哺乳动物生物体内的心肌缺血的方法。 将化合物[[4-(1,4,5,6-四氢-4-甲基-6-氧代-3-哒嗪基)苯基]亚肼基]丙二腈或其对映体或药学上可接受的盐向哺乳动物生物体施用 需要这样的预防或治疗。 化合物可以其外消旋形式或基本上不含(+) - 对映异构体或基本上不含( - ) - 对映体的形式施用。

    Substituted pyridazinones
    2.
    发明授权
    Substituted pyridazinones 失效
    取代哒嗪酮

    公开(公告)号:US5151420A

    公开(公告)日:1992-09-29

    申请号:US489187

    申请日:1990-03-08

    摘要: Substituted benzylideneiminophyenylpyridazinones or dihydropyridazinones of formula I ##STR1## in which R.sub.1 and R.sub.8 independently mean hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, trifluoromethyl, hydroxy alkyl, halogen alkyl, alkoxy alkyl, pyridyl, furyl, thienyl or cycloalkyl or one of optionally substituted groups; aryl, aralkyl, aralkenyl or nitrogen containing heterocyclic ring joining through an alkyl or alkenyl group and R.sub.3, R.sub.4 and R.sub.5 independently mean hydrogen, lower alkyl, hydroxy alkyl, halogen, hydroxy, alkoxy, acyloxy, aroyloxy, formyl, acyl, cyano, amino, carboxy or trifluoromethyl, R.sub.6 and R.sub.7 independently mean hydrogen, amino, lower alkyl, hydroxy, nitro or cyano or R.sub.2 and R.sub.7 together form a --CH.sub.2 --NH-- or --CH.dbd.N-- group and A means phenyl, naphtyl or a nitrogen containing heterocyclic ring. The compounds may be used in the treatment of congestive heart failure.

    摘要翻译: 取代的亚苄基亚氨基腺苷哒嗪酮或式I的二氢哒嗪酮,其中R 1和R 8独立地表示氢或低级烷基,R 2是氢,低级烷基,三氟甲基,羟基烷基,卤素烷基,烷氧基烷基,吡啶基,呋喃基,噻吩基或环烷基或一个 任选取代的基团; 通过烷基或烯基连接的芳基,芳烷基,芳烯基或含氮杂环,R 3,R 4和R 5独立地表示氢,低级烷基,羟基烷基,卤素,羟基,烷氧基,酰氧基,芳氧基,甲酰基,酰基,氰基,氨基 ,羧基或三氟甲基,R6和R7独立地表示氢,氨基,低级烷基,羟基,硝基或氰基,或R2和R7一起形成-CH 2 -NH-或-CH = N-基团,A表示苯基,萘基或氮 含杂环。 该化合物可用于治疗充血性心力衰竭。

    Heterocyclic lactam compounds
    9.
    发明授权
    Heterocyclic lactam compounds 失效
    杂环内酰胺化合物

    公开(公告)号:US4963677A

    公开(公告)日:1990-10-16

    申请号:US268450

    申请日:1988-11-08

    摘要: A compound of the formula ##STR1## and pharmaceutically acceptable salts thereof, in which A is --N.dbd.N--NH--, --X--C(R.sub.2).dbd.N--, --N.dbd.C(R.sub.2)--X--, --X--C(R.sub.2)--CH(R.sub.2).dbd.N-- or --N.dbd.C(R.sub.2)--CH(R.sub.2)--X--, wherein X is sulphur, oxygen or nitrogen and R.sub.2 is provided that where two R.sub.2 -groups are present in the A group one of the R.sub.2 groups is hydrogen, amino, substituted amino, C.sub.1-6 alkyl, substituted acylamino or one of the following groups: ##STR2## wherein R.sub.a is hydrogen, amino, substituted amino, C.sub.1-6 alkoxy, heterocyclic five membered ring or --NHCOR', wherein R' is C.sub.1-6 alkyl, aryl or heterocyclic five membered ring, R.sub.b is hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or hydroxy, R.sub.c is hydrogen, C.sub.1-6 alkyl or oxygen and R.sub.d is C.sub.1-6 alkyl or oxygen, R.sub.e is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sub.f is C.sub.1-6 alkyl, provided that where two R.sub.2 -groups are present in the A group, one of the R.sub.2 groups is hydrogen; B is --(CH.sub.2).sub.m --C(R.sub.3 R.sub.4)--(CH.sub.2).sub.n --, --C(R.sub.3).dbd.CH--, --CH.dbd.C(R.sub.3)--, --O--[C(R.sub.3 R.sub.4)].sub.n --, --[C(R.sub.3 R.sub.4)].sub.n --O--, --S--[C(R.sub.3 R.sub.4)].sub.n -- or --[C(R.sub.3 R.sub.4)].sub.n --S-- wherein R.sub.3 and R.sub.4, which can be independently the same or different, are hydrogen, C1-.sub.6 alkyl, aryl (preferably phenyl) or pyridyl and m and n are independently zero or 1; D is either oxygen or sulphur; the two R-groups are indepenently hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, amino, acylamino or substituted acylamino, nitro, halogen, cyano, aldehyde, carboxy, carbamoyl; R.sub.1 is a hydrogen or C.sub.1-6 alkyl or R and R.sub.1 form together a fused 6-membered heterocyclic ring. The compound is effective in the treatment of congestive heart failure.

    摘要翻译: 其中A为-N = N-NH-,-XC(R2)= N-,-N = C(R2)-X的式I化合物及其药学上可接受的盐 - ,-XC(R2)-CH(R2)= N-或-N = C(R2)-CH(R2)-X-,其中X为硫,氧或氮,R2为两个R2-基团 存在于A基团中的一个R2基团是氢,氨基,取代的氨基,C 1-6烷基,取代的酰基氨基或以下基团之一: 其中R a是氢,氨基,取代的氨基,C 1-6烷氧基,杂环五元环或-NHCOR',其中R'是C 1-6烷基,芳基或杂环五元环,R b是氢, C 1-6烷氧基,C 1-6烷硫基或羟基,R c是氢,C 1-6烷基或氧,R d是C 1-6烷基或氧,Re是氢,羟基或C 1-6烷氧基,R f是C 1-6烷基,条件是其中两个R 2 - A组存在,R2基团之一为氢; B是 - (CH 2)m C(R 3 R 4) - (CH 2)n - , - C(R 3)= CH-,-CH = C(R 3) - ,-O- [C(R 3 R 4)] n - (R3R4)] nO-,-S- [C(R3R4)] n - 或 - [C(R3R4)] nS-,其中R3和R4可以独立地相同或不同,是氢,C1-6烷基,芳基 (优选苯基)或吡啶基,m和n分别为0或1; D是氧或硫; 两个R基团是独立的氢,C 1-6烷氧基,C 1-6烷基,氨基,酰氨基或取代的酰基氨基,硝基,卤素,氰基,醛,羧基,氨基甲酰基; R 1是氢或C 1-6烷基,或R 1和R 1一起形成稠合的6元杂环。 该化合物可有效治疗充血性心力衰竭。