Alkoxyphenylindolinone derivatives, medicaments containing them and
their use
    6.
    发明授权
    Alkoxyphenylindolinone derivatives, medicaments containing them and their use 失效
    烷氧基吲哚啉酮衍生物,含有它们的药物及其用途

    公开(公告)号:US4882329A

    公开(公告)日:1989-11-21

    申请号:US303996

    申请日:1989-01-30

    CPC分类号: C07D401/12 C07D209/34

    摘要: Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indolinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.

    摘要翻译: 具有R(1),R(2),R(3)和R(4)的式(I)的化合物拮抗剂尤其是H,烷基,烷氧基,卤素,在一些情况下为苯基; m为1-4; n为0-3; X是CH 2,O,S,CO,CHOH或CR 2,R(5)是含有氮原子的各种基团。 它们通过同样新的且含有代替R(5)离去基团Y(Cl,Br,I)的化合物II与适当的(环状)氨基化合物反应而获得。 另一种合成方法包括在碱存在下,具有非醚化羟基的合适的吲哚啉酮衍生物IV与含有末端离去基团Z(Cl,Br,I)的侧链的反应。 此外,具有末端环氧基团的醚侧链的二氢吲哚衍生物VI可以与(环状)胺反应,得到化合物I.

    Benzothiazine derivatives
    7.
    发明授权
    Benzothiazine derivatives 失效
    苯并噻嗪衍生物

    公开(公告)号:US4595685A

    公开(公告)日:1986-06-17

    申请号:US684711

    申请日:1984-12-21

    摘要: Benzothiazine derivatives of the formula I ##STR1## with (R(1), R(1)', R(1)", R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C.sub.1 -C.sub.3)-alkyl; R(6) equal to one of the following groups, ##STR2## with R(7) and R(8) equal to hydrogen, alkyl, cycloalkyl, phenyl; R(9) equal to hydrogen, alkyl, phenyl, pyridyl, pyrimidinyl or benzoyl; R(10) equal to hydrogen, alkyl, phenyl; R(11) equal to hydrogen, hydroxyl, alkoxy or, together with R(12), a bond; and R(12) equal to hydrogen or, together with R(11), a bond; m equal to 1, 2, 3 or 4; n equal to 0 or 1; p equal to 0, 1, 2, 3 or 4, and X equal to oxygen or two hydrogen atoms, and salts of the compounds of the formula I with physiologically tolerated acids and a process for the preparation of compounds I, likewise a method of treatment of disturbances of the calcium balance of a human body are described.

    摘要翻译: 式(I)与(R(1),R(1)',R(1)“,R(4)和R(4)'等于氢,烷基,烷氧基, 卤素,硝基,羟基,乙酰氨基或氨基; R(2)等于氢,烷基,烯基,苯基; R(3)等于氢,烷基,链烯基,苯基; R(5)等于氢或(C1-C3 ) - 烷基; R(6)等于以下基团之一,其中R(7)和R(8)等于氢,烷基,环烷基,苯基; R(9)等于氢, 烷基,苯基,吡啶基,嘧啶基或苯甲酰基; R(10)等于氢,烷基,苯基; R(11)等于氢,羟基,烷氧基或与R(12) 等于氢或与R(11)一起键; m等于1,2,3或4; n等于0或1; p等于0,1,2,3或4,X等于 氧或两个氢原子,以及式I化合物与生理学上可耐受的酸的盐以及制备化合物I的方法,同样是治疗钙粘蛋白紊乱的方法 描述一个人的身体。

    Method of treating cardiac insufficiency
    8.
    发明授权
    Method of treating cardiac insufficiency 失效
    治疗心功能不全的方法

    公开(公告)号:US5684016A

    公开(公告)日:1997-11-04

    申请号:US445543

    申请日:1995-05-22

    CPC分类号: C07K5/0222 A61K38/556

    摘要: The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 and R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.

    摘要翻译: 本发明涉及通过使用其中n为1或2的式I(I)的化合物治疗心功能不全的方法,R 1,R 2,R 2和R 3相同或不同,并且各自表示氢或有机基团 并且R4和R5与携带它们的原子一起形成单环,双环或三环杂环体系。 本发明还涉及式I化合物和含有这些化合物用于治疗上述疾病的药剂。