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1. 发明授权

US4436742A 4-Hydroxy-2,1,3-benzthiadiazole compounds and .beta.-adrenergic method of use therefor 失效
标题翻译： 4-羟基-2,1,3-苯并噻二唑化合物和β-肾上腺素能方法
公开(公告)号：US4436742A
公开(公告)日：1984-03-13
申请号：US208741
申请日：1980-11-20
申请人： Erich Fauland , Wolfgang Kampe , Kurt Stach , Wolfgang Bartsch , Egon Roesch
发明人： Erich Fauland , Wolfgang Kampe , Kurt Stach , Wolfgang Bartsch , Egon Roesch
IPC分类号： C07D285/10 , C07D285/14 , C07D285/06
CPC分类号： C07D285/14
摘要： New amine derivatives of 4-hydroxy-2,1,3-benzthiadiazoles of the formula: ##STR1## wherein R is straight-chained or branched alkyl and the pharmacologically compatible salts thereof, that are markedly effected as inhibitors of adrenogenic .beta.-receptors and thus useful for the treatment and prophylaxis of cardiac and circulatory diseases.
摘要翻译：具有下式的4-羟基-2,1,3-苯并噻二唑的新胺衍生物：其中R是直链或支链烷基及其药理学上相容的盐，其显着作为肾上腺素β的抑制剂受体，因此可用于治疗和预防心脏和循环系统疾病。

2. 发明授权

US4016262A Therapeutic compositions and methods employing N(6)-disubstituted adenosine compounds 失效
标题翻译：使用N（6） - 二取代腺苷化合物的治疗组合物和方法
公开(公告)号：US4016262A
公开(公告)日：1977-04-05
申请号：US582529
申请日：1975-05-30
申请人： Erich Fauland , Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, executor , Harald Stork , Karl Dietmann
发明人： Erich Fauland , Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, executor , Harald Stork , Karl Dietmann
IPC分类号： C07H19/16 , A61K31/70
CPC分类号： C07H19/16
摘要： N(6)-disubstituted adenosine compounds of the formula: ##STR1## wherein R.sub.1 is alkenyl, cycloalkenyl or cycloalkenyl-alkyl; andR.sub.2 is alkenyl, cycloalkenyl, straight or branched-chain alkyl, cycloalkyl, bicycloalkyl, alkyl-cycloalkyl, or alkyl-bicycloalkyl;And the pharmacologically compatible salts thereof; exhibit outstanding anti-lipolytic, anti-hyperlipaemic and anti-hypercholesterolaemic action.
摘要翻译：具有下式的N（6） - 二取代的腺苷化合物：其中R 1是烯基，环烯基或环烯基 - 烷基; R 2为烯基，环烯基，直链或支链烷基，环烷基，二环烷基，烷基 - 环烷基或烷基 - 双环烷基; 及其药理学兼容性; 展示超耐药，抗高血压和抗高胆固醇血管作用。

3. 发明授权

US3966916A N(6)-disubstituted adenoisine compounds and therapeutic compositions 失效
标题翻译： 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。

4. 发明授权

US3982012A 4-Hydroxy-benzimidazole compounds and therapeutic compositions 失效
标题翻译： 4-羟基 - 苯并咪唑化合物和治疗组合物
公开(公告)号：US3982012A
公开(公告)日：1976-09-21
申请号：US585645
申请日：1975-06-10
申请人： Erich Fauland , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Wolfgang Schaumann
发明人： Erich Fauland , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Wolfgang Schaumann
IPC分类号： C07D235/06 , A61K31/4184 , C07D235/08
CPC分类号： C07D235/08
摘要： New 4-hydroxy-benzimidazole compounds of the formula: ##EQU1## wherein R.sub.1 is straight-chained or branched alkyl andR.sub.2 is hydrogen atom or lower alkylAnd the pharmacologically compatible salts thereof; are outstandingly effective in the treatment and prophylaxis of cardiac and circulatory diseases, and provide substantially greater margins of safety than prior art adrenergic .beta.-receptor inhibitors.
摘要翻译：新的下式的4-羟基 - 苯并咪唑化合物：OH | O-CH 2 -CH-CH 2 -NH-R 1（I）其中R 1是直链或支链烷基，R 2是氢原子或低级烷基，并且其药理学上可兼容的盐 ; 在治疗和预防心脏病和循环系统疾病方面非常有效，并且提供比现有抗生素β受体抑制剂更安全的重要安全标志。

5. 发明授权

US4224438A Adenosine-5'-carboxylic acid amides 失效
标题翻译：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。

6. 发明授权

US4370323A 2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes 失效
标题翻译： 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。

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