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1. 发明授权

US4069330A Nitropyrazole compounds and anti-microbial compositions 失效
标题翻译：硝基吡唑化合物和抗微生物组合物
公开(公告)号：US4069330A
公开(公告)日：1978-01-17
申请号：US678588
申请日：1976-04-20
申请人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Schaumann , Wolfgang Vomel
发明人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Schaumann , Wolfgang Vomel
IPC分类号： G09F7/02 , C07D231/16 , G09F3/20 , H01B7/36 , H01R13/46 , A61K31/415
CPC分类号： H01B7/368 , C07D231/16
摘要： New nitropyrazole compounds of the formula ##STR1## wherein R.sub.1 is alkyl or hydroxyalkylR.sub.2 and R.sub.3, which may be the same or different, are alkyl orR.sub.2 and R.sub.3 together represent a 4- or 5-membered alkylene bridge which is optionally interrupted by an oxygen atom or by the grouping >N-R, in which R is an alkyl or hydroxyalkyl radical;And the pharmacologically compatible salts thereof, possess excellent anti-microbial action not only in vitro but also in vivo, especially systemically.
摘要翻译：其中R 1是烷基或羟基烷基的新的硝基吡唑化合物，其可以相同或不同，R 2和R 3可以是烷基或R 2和R 3一起代表4-或5-元亚烷基桥，其任选地被氧原子或通过NR> NR，其中R是烷基或羟烷基; 和药物相容性好的药物，不仅仅是体内，而且在体内非常有效地进行非常有效的抗微生物作用。

2. 发明授权

US4152446A Aminopropanol compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：用于治疗心脏和循环系统疾病的氨基丙醇化合物和组合物
公开(公告)号：US4152446A
公开(公告)日：1979-05-01
申请号：US805558
申请日：1977-06-10
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/08 , C07D209/12 , C07D209/42 , A61K31/40 , C07D209/04
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof;Are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

3. 发明授权

US4070373A Tricyclic aminoalkyl derivatives 失效
标题翻译：三环氨基烷基衍生物
公开(公告)号：US4070373A
公开(公告)日：1978-01-24
申请号：US291426
申请日：1972-09-22
申请人： Werner Winter , Max Thiel , Kurt Stach, deceased , by Werner Plattner, administrator , Wolfgang Schaumann , Karl Dietmann
发明人： Werner Winter , Max Thiel , Kurt Stach, deceased , by Werner Plattner, administrator , Wolfgang Schaumann , Karl Dietmann
IPC分类号： C07D311/90 , C07D313/12 , C07D337/12 , C07D337/16
CPC分类号： C07D337/16 , C07D311/90 , C07D313/12 , C07D337/12 , C07C2103/18
摘要： Novel tricyclic aminoalkyl derivatives are disclosed which are characterized by valuable pharmacological activities and namely by cardiac and circulatory activities. The tricyclic aminoalkyl derivatives are compounds of the formula: ##STR1## wherein X is an oxygen or a sulfur atom, a saturated or unsaturated, straight chain or branched alkylene group containing up to 3 carbon atoms, an oxymethylene, thiamethylene or thiaethylene group or a valency bond, R.sub.1 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen or hydroxyl, R.sub.3 is hydrogen or together with R.sub.2 represents a further valency bond, R.sub.4 and R.sub.5 which may be the same or different are each hydrogen or lower alkyl, A is alkylene which is substituted by an optionally acylated hydroxyl group, Y is an oxygen or sulfur atom or an optionally alkylated imino group and Z is aryl, aralkyl, cycloalkyl or cycloalkyl-alkyl which may be substituted by halogen, hydroxyl, nitro, amino, alkoxy, aralkoxy, alkyl, trifluoromethyl, alkylamino or alkylsulfonyl group, and the acid addition salts thereof with pharmacologically acceptable acids.
摘要翻译：公开了新颖的三环氨基烷基衍生物，其特征在于有价值的药理活性，即通过心脏和循环活性。三环氨基烷基衍生物是下式的化合物：其中X是氧或硫原子，含有至多3个碳原子的饱和或不饱和的直链或支链亚烷基，亚甲基，亚亚甲基或亚硫代亚乙基或化合键，R 1是氢，卤素，烷基，烷氧基或三氟甲基，R 2是氢或羟基，R 3是氢或与R 2一起代表另外的价键，可以相同或不同的R 4和R 5各自是氢或低级烷基 A是被任意酰化的羟基取代的亚烷基，Y是氧或硫原子或任选烷基化的亚氨基，Z是可以被卤素，羟基，硝基取代的芳基，芳烷基，环烷基或环烷基 - 烷基，氨基，烷氧基，芳烷氧基，烷基，三氟甲基，烷基氨基或烷基磺酰基，及其与药理学上可接受的酸的酸加成盐。

4. 发明授权

US4076829A Aminopropanol compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：用于治疗心脏和循环系统疾病的氨基丙醇化合物和组合物
公开(公告)号：US4076829A
公开(公告)日：1978-02-28
申请号：US626512
申请日：1975-10-28
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/43 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/02 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/14
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , Y10S514/927
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen andThe pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：式（I）的新的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟基烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是相同或不同，代表氢或低级烷基，R2是低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R是烷硫基烷基或R1是新戊酰氧基烷基时，R2也可以是氢，并且其药学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

5. 发明授权

US4229464A Aminopropanol substituted indole compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：氨基丙醇取代的吲哚化合物和用于治疗心脏和循环系统疾病的组合物
公开(公告)号：US4229464A
公开(公告)日：1980-10-21
申请号：US943512
申请日：1978-09-18
申请人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/43 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/02 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/18 , C07D209/20
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , Y10S514/927
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏和循环系统疾病方面非常有效。

6. 发明授权

US4212866A Pharmaceutically active derivatives of 9-[3-(4-amino-piperidino)-propyl]-adenines 失效
标题翻译： 9- [3-（4-氨基 - 哌啶子基） - 丙基] - 腺苷的药物活性衍生物
公开(公告)号：US4212866A
公开(公告)日：1980-07-15
申请号：US006050
申请日：1979-01-24
申请人： Walter-Gunar Friebe , Max Thiel , Androniki Roesch , Otto-Henning Wilhelms , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Max Thiel , Androniki Roesch , Otto-Henning Wilhelms , Wolfgang Schaumann
IPC分类号： A61K31/52 , A61P29/00 , A61P37/08 , C07D211/58 , C07D473/34 , C07D473/00
CPC分类号： C07D473/34 , C07D211/58 , Y10S514/826
摘要： Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R.sub.1 and the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom or an acyl radical,or salts thereof with pharmacologically acceptable acids, characterized by anti-allergic, anti-inflammatory and anti-oedematous activity.
摘要翻译：新颖的式[IMAGE]的9- [3-（4-氨基 - 哌啶子基） - 丙基] - 腺嘌呤衍生物，其中R1是氢原子或低级烷基，R2是氢原子，芳基，低级烷基基团，羟基低级烷基或与R 1和它们所连接的氮原子一起形成杂环，并且R 3是氢原子或酰基，或其与药理学上可接受的酸的盐，其特征在于抗过敏，抗炎和抗水肿活性。

7. 发明授权

US4348401A N-Phenoxyalkylpiperidine derivatives 失效
标题翻译： N-苯氧基烷基哌啶衍生物
公开(公告)号：US4348401A
公开(公告)日：1982-09-07
申请号：US185839
申请日：1980-09-10
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Max Thiel , Wolfgang Schaumann , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Max Thiel , Wolfgang Schaumann , Otto-Henning Wilhelms
IPC分类号： A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61P11/14 , A61P37/00 , C07D211/22 , C07D211/58 , C07D401/12 , C07D409/12 , C07D409/14 , A61K31/455 , C07D403/12 , C07D407/12
CPC分类号： C07D211/58 , C07D211/22 , Y10S514/87
摘要： An N-phenoxyalkylpiperidine derivative of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, an acyl radical or an optionally substituted aryl radical, R.sub.2 is a hydroxymethyl radical, a cyano group, an amidino group, an amidino group substituted by hydroxyl, a 1H tetrazol-5-yl radical or a --CO--R.sub.3 radical, R.sub.3 is a hydroxyl group, a lower alkoxy radical, an amino group, or an amino group substituted by a 1H-tetrazol-5-yl radical, X is an imino group or an oxymethyl radical, A is an alkylene radical containing 2 to 4 carbon atoms, and B is a valency bond or a 4-hydroxypyrimidin-2,5-diyl radical; or a pharmacologically acceptable salt thereof. The compounds exhibit anti-histaminic, anti-oedematous and anti-phlogistic activity.
摘要翻译：其中R 1是氢原子，酰基或任意取代的芳基，R 2是羟甲基，氰基，脒基，被羟基取代的脒基， 1H-四唑-5-基或-CO-R 3基团，R 3是羟基，低级烷氧基，氨基或被1H-四唑-5-基取代的氨基，X是亚氨基基团或氧甲基，A是含有2至4个碳原子的亚烷基，B是价键或4-羟基嘧啶-2,5-二基; 或其药理学上可接受的盐。该化合物表现出抗组胺，抗氧化和抗病毒活性。

8. 发明授权

US4092416A Benzopyrone derivatives exhibiting anti-allergic activity 失效
标题翻译：苯丙酮衍生物具有抗过敏活性
公开(公告)号：US4092416A
公开(公告)日：1978-05-30
申请号：US746551
申请日：1976-12-01
申请人： Werner Winter , Max Thiel , Kurt Stach, deceased , Androniki Roesch , by Werner Plattner, administrator , Wolfgang Schaumann
发明人： Werner Winter , Max Thiel , Kurt Stach, deceased , Androniki Roesch , by Werner Plattner, administrator , Wolfgang Schaumann
IPC分类号： A61K31/495 , A61P37/08 , C07C45/71 , C07D295/108 , C07D295/15 , C07D309/12 , C07D311/22 , C07D317/22 , C07D295/10
CPC分类号： C07D295/108 , C07C45/71 , C07D295/15 , C07D309/12 , C07D311/22 , C07D317/22
摘要： Benzopyrones of the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or a hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl radical,R.sub.2, r.sub.3, r.sub.4 and R.sub.5 each independently is hydrogen, a halogen atom, a hydroxyl radical, a lower alkyl or lower alkoxy radical, or a lower alkyl or lower alkoxy radical substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring,A is a lower alkylene radical, andn is 0, 1 or 2,And salts thereof exhibit anti-allergic activity.
摘要翻译：其中R1是氢原子或卤原子或羟基，低级烷基，烷氧基，烷硫基或三氟甲基的式为“IMAGE”的苯并吡喃酮，R 2，R 3，R 4和R 5各自独立地是氢，卤原子，羟基，或被羟基，卤素，甲磺酰氧基或甲苯磺酰氧基中的至少一个取代的低级烷基或低级烷氧基，或由环氧乙烷，二恶烷或二氧戊环形成的环，A为低级亚烷基，N为0， 1或2，以及其展示抗过敏活性。

9. 发明授权

US3996361A N.sup.6 -Substituted-9-[3-(4-phenyl-piperazino)-propyl]-adenines 失效
标题翻译： N {HU 6 {B-取代-9- {8- 3-（4-苯基 - 哌嗪基） - 丙基{9-腺嘌呤
公开(公告)号：US3996361A
公开(公告)日：1976-12-07
申请号：US531420
申请日：1974-12-10
申请人： Walter-Gunar Friebe , Max Thiel , Werner Winter , Androniki Roesch , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Max Thiel , Werner Winter , Androniki Roesch , Wolfgang Schaumann
IPC分类号： C07D473/34 , A61K31/395 , A61K31/50 , A61K31/52 , C07D20060101 , C07D241/04 , C07D295/04 , C07D295/12 , C07D295/13 , C07D403/06 , C07D403/14 , C07D405/06 , C07D473/00 , C07D475/06
CPC分类号： Y10S514/826
摘要： A N.sup.6 -substituted-9-[3-(4-phenyl-piperazino)-propyl]-adenine of the formula ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl radical, andR.sub.2 is a lower alkyl radical, a lower alkyl radical substituted by at least one of phenyl and hydroxyl, a lower alkenyl radical, a cycloalkyl radical or an aryl radical, orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a piperidine, pyrrolidine or morpholine ring, andR.sub.3 is hydrogen, halogen, a lower alkyl radical or a lower alkoxy radical,Or a salt thereof with a pharmacologically compatible acid, which compounds are characterized by marked anti-edematous activity as well as by activity in reducing capillary permeability.
摘要翻译：式（I）的N6-取代-9- [3-（4-苯基 - 哌嗪子基） - 丙基] - 腺嘌呤，其中R 1是氢或低级烷基，R 2是低级烷基，被苯基和羟基中的至少一个取代的低级烷基，低级烯基，环烷基或芳基，或者R 1和R 2与它们所连接的氮原子一起形成哌啶，吡咯烷或吗啉环，以及 R3是氢，卤素，低级烷基或低级烷氧基，或其盐与药理学上相容的酸，其化合物由标记的抗病毒活性表征，以及活性降低毛细管渗透性。

10. 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。

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