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    Adenosine-5'-carboxylic acid amides
    2.
    发明授权
    Adenosine-5'-carboxylic acid amides 失效
    腺苷-5'-羧酸酰胺

    公开(公告)号：US4224438A

    公开(公告)日：1980-09-23

    申请号：US161338

    申请日：1971-07-09

    申请人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    发明人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    IPC分类号： C07H19/16 ,  A61K31/70 ,  C07H19/18

    CPC分类号： C07H19/16

    摘要： Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.

    摘要翻译： 具有以下通式的腺苷-5'-羧酸衍生物：其中Z为两个氢原子或二价低级亚烷基，其中R 1和R 2独立为 氢，羟基，氨基，低级烷基，低级烯基，任选N-烷基化的低级氨基烷基，环烷基，羟基烷基或哌啶基，或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基 或亚氨基，亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。 这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。 虽然酯具有一些活性，但它们可用于制备以标记的冠状动脉为特征的酰胺。

    N(6)-disubstituted adenoisine compounds and therapeutic compositions
    3.
    发明授权
    N(6)-disubstituted adenoisine compounds and therapeutic compositions 失效
    N（6） - 二取代腺苷化合物和治疗组合物

    公开(公告)号：US3966916A

    公开(公告)日：1976-06-29

    申请号：US525795

    申请日：1974-11-21

    申请人： Wolfgang Kampe ,  Erich Fauland ,  Kurt Stach ,  Harald Stork ,  Felix Helmut Schmidt

    发明人： Wolfgang Kampe ,  Erich Fauland ,  Kurt Stach ,  Harald Stork ,  Felix Helmut Schmidt

    IPC分类号： C07H19/16 ,  A61K31/70

    CPC分类号： C07H19/16

    摘要： New N(6)-disubstituted adenosine compound of the formula ##SPC1##WhereinR.sub.1 is lower alkyl substituted by at least one of hydroxyl, alkoxy or acyloxy; or is cycloalkyl or straight-chained or branched lower alkenyl;R.sub.2 and R.sub.3 are hydrogen, halogen, or nitro or lower alkyl, alkoxy or alkylthio andR.sub.4 is hydrogen or acyl; when R.sub.4 is acyl, R.sub.1 can also be lower alkyl;And the pharmacologicaly compatible salts thereof; exhibits shown anti-lipolytic, anti-hyperlipaemic and anti-hypercholesterolaemic action.

    摘要翻译： 新的N（6） - 二取代的腺苷化合物，式WHERE R1是被羟基，烷氧基或酰氧基中的至少一个取代的低级烷基; 或是环烷基或直链或支链低级链烯基; R2和R3是氢，卤素或硝基或低级烷基，烷氧基或烷硫基，R4是氢或酰基; 当R 4是酰基时，R 1也可以是低级烷基; 及其药理学兼容性; 展示了抗脂肪，抗高血压和抗高血脂药物作用。

    2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes
    4.
    发明授权
    2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes 失效
    2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷

    公开(公告)号：US4370323A

    公开(公告)日：1983-01-25

    申请号：US776068

    申请日：1977-03-09

    申请人： Wolfgang Kampe ,  Max Thiel ,  Erich Fauland ,  Uwe Bicker ,  Gottfried Hebold

    发明人： Wolfgang Kampe ,  Max Thiel ,  Erich Fauland ,  Uwe Bicker ,  Gottfried Hebold

    IPC分类号： C07D203/06 ,  A61K31/395 ,  A61K31/396 ,  A61K31/435 ,  A61P35/00 ,  A61P37/04 ,  C07D203/08 ,  C07D203/12 ,  C07D203/14 ,  C07D333/00 ,  C07D335/00 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D451/14 ,  C07D403/06 ,  C07D401/14

    CPC分类号： C07D203/08 ,  C07D451/14 ,  Y10S514/885

    摘要： A 2-cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methane ##STR1## wherein R is a nitrile or carbamoyl group, andR.sub.1 and R.sub.2 each independently is a hydrogen atom, an aliphatic hydrocarbon radical containing up to 10 carbon atoms optionally substituted by hydroxyl, alkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, cyano, 1, 2 or 3 halogens, cycloalkyl, phenyl or phenoxy; nitrile, carboxyl, alkoxycarbonyl or optionally hydrogenated monocyclic heteroaryl or phenyl optionally substituted by alkyl, alkoxy, hydroxy, alkoxcarbonyl, dialkylamino, alkylthio, trifluoromethyl, nitro, carbamoyl, nitrile, sulphonamido, hydroxyalkyl, methylenedioxy, or halogen; or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a ring containing up to 8 ring members of which at least one may be oxygen, sulphur, SO, SO.sub.2 NH, N-alkyl, N-acyl or N-alkoxycarbonylalkyl, and which can be substituted by alkyl, alkoxy, hydroxyl, alkylenedioxy, alkoxycarbonyl, hydroxyalkyl, alkoxycarbonylalkyl, dialkylamino, oxo or 2-cyanoaziridino groups, or can be fused to 1 or 2 benzene rings or can be bridged by alkylene radicals containing up to 3 carbon atoms.The compounds are characterized by cytostatic and immune response-stimulating activity.

    摘要翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷，其中R是腈或氨基甲酰基，R 1和R 2各自独立地为氢原子，含有至多 任选被羟基，烷氧基，氨基，烷基氨基，二烷基氨基，烷氧基羰基，氰基，1,2或3卤素，环烷基，苯基或苯氧基取代的10个碳原子; 腈，羧基，烷氧基羰基或任选氢化的单环杂芳基或任选被烷基，烷氧基，羟基，烷氧基羰基，二烷基氨基，烷硫基，三氟甲基，硝基，氨基甲酰基，腈，磺酰胺基，羟烷基，亚甲二氧基或卤素取代的苯基。 或R 1和R 2与它们所连接的碳原子一起形成含有至多8个环成员的环，其中至少一个可以是氧，硫，SO，SO 2 + L，NH，N-烷基， 酰基或N-烷氧基羰基烷基，其可以被烷基，烷氧基，羟基，亚烷基二氧基，烷氧基羰基，羟基烷基，烷氧基羰基烷基，二烷基氨基，氧代或2-氰基氮丙啶基取代，或者可以与1或2个苯环稠合，或可以被 含有至多3个碳原子的亚烷基。 该化合物的特征在于细胞抑制和免疫应答刺激活性。