利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

54 条记录 (耗时 0.024 秒)

    2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes
    1.
    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。

    Adenosine-5'-carboxylic acid amides
    3.
    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-Substituted aziridine-2-carboxylic acid derivatives
    5.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives 失效

    公开(公告)号：US4517183A

    公开(公告)日：1985-05-14

    申请号：US495548

    申请日：1983-05-17

    申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

    CPC分类号： C07D203/22 ,  Y10S514/885

    摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

    N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives
    6.
    发明授权
    N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives 失效
    N-取代的氮丙啶-2-羧酸免疫刺激剂衍生物

    公开(公告)号：US4397848A

    公开(公告)日：1983-08-09

    申请号：US236375

    申请日：1981-02-20

    申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

    CPC分类号： C07D203/22 ,  Y10S514/885

    摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

    摘要翻译： 本发明提供含有下列通式的N-取代的氮丙啶-2-羧酸衍生物的药物组合物：其中X是羧基，氰基，烷氧基羰基或任选取代的氨基甲酰基，R是 氢原子或任选取代的脂族烃基或环烷基或环烯基，R 1为氢原子或烷基或苯基; 和其药学上可接受的盐，与药物稀释剂或载体混合。 本发明还提供了作为新化合物的通式（I'）的N-取代的氮丙啶-2-羧酸衍生物，但条件是当X是氨基甲酰基或烷氧基羰基并且R 1是氢原子时，R不是 甲基，乙基，异丙基或苄基; 及其药理学上可接受的盐，也提供制备这些新化合物的方法。 此外，本发明涉及通式（I'）的化合物及其药理学上可接受的盐在与免疫系统的弱化相关的疾病中的用途。

    N(6)-disubstituted adenoisine compounds and therapeutic compositions
    9.
    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。

    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods
    10.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods 失效
    N-取代的氮丙啶-2-羧酸衍生物及其免疫刺激组合物和方法

    公开(公告)号：US4410532A

    公开(公告)日：1983-10-18

    申请号：US334614

    申请日：1981-12-28

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D213/36

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.

    摘要翻译： 具有式“IMAGE”的2-氰基氮丙啶衍生物，其中R'是具有至多8个碳原子的直链或支链，饱和或单或多不饱和脂族烃基，其被含芳族含氮杂环基团取代， 5或6个环成员和1,2或3个任选被卤素取代的氮原子，具有至多8个碳原子的烷氧基，至多8个碳原子的烷基，羟基，至多9个碳原子的烷氧基，氨基甲酰基，二烷基氨基烷基 其具有至多8个碳原子的部分，环烷基氨基，具有3-10个碳原子的环烷基部分，乙酰氨基，硝基，氰基，乙酰基，具有至多8个碳原子的烷硫基，具有至多8个碳原子的烷基亚磺酰基，烷基磺酰基， 8个碳原子，氨磺酰基，苯基，三氟甲基，苯氧基，乙酰氧基或亚甲二氧基; 或其药理学上可接受的盐显示免疫刺激活性。