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1. 发明授权

US4172136A 3-Nitropyrazole compounds and anti-microbial compositions 失效
标题翻译： 3-硝基吡唑化合物和抗微生物组合物
公开(公告)号：US4172136A
公开(公告)日：1979-10-23
申请号：US889594
申请日：1978-03-23
申请人： Herbert Berger , Rudi Gall , Kurt Stach, deceased , Max Thiel , Wolfgang Vomel
发明人： Herbert Berger , Rudi Gall , Kurt Stach, deceased , Max Thiel , Wolfgang Vomel
IPC分类号： C07D231/16 , C07D401/02 , C07D403/02
CPC分类号： C07D231/16
摘要： New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO-NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.
摘要翻译：新的具有下式的3-硝基吡唑化合物：其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基，羧基或低级烷氧基羰基或基团-CO-NR4R5，其中R4是氢或羟基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，硫代氨基甲酰基，脲基，硫脲基，羟基苯基，吡啶甲基或是低级烷基，烯基或环烷基取代如果需要，通过氰基，羟基，吡咯烷子基，哌啶子基，氨基，低级烷基氨基，低级二烷基氨基或低级酰基氨基取代基，R 5是氢原子或低级烷基，或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物药剂，特别是在系统性和在尿道感染中是非常有效的。

2. 发明授权

US4105772A 3-Nitropyrazole compounds and anti-microbial compositions 失效
标题翻译： 3-硝基吡唑化合物和抗微生物组合物
公开(公告)号：US4105772A
公开(公告)日：1978-08-08
申请号：US744215
申请日：1976-11-22
申请人： Herbert Berger , Rudi Gall , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Vomel
发明人： Herbert Berger , Rudi Gall , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Vomel
IPC分类号： C07D231/16 , A61K31/41 , C07D231/10
CPC分类号： C07D231/16
摘要： New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO--NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof, are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.
摘要翻译：新的具有下式的3-硝基吡唑化合物：其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基，羧基或低级烷氧基羰基或基团-CO-NR4R5，其中R4是氢或羟基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，硫代氨基甲酰基，脲基，硫脲基，羟基苯基，吡啶甲基或是低级烷基，烯基或环烷基取代如果需要，通过氰基，羟基，吡咯烷子基，哌啶子基，氨基，低级烷基氨基，低级二烷基氨基或低级酰基氨基取代基，R 5是氢原子或低级烷基，或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物剂，特别是在系统性和全球性的治疗中是非常有效的。

3. 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。

4. 发明授权

US3962242A 3-(5-Nitro-2-furyl)-6-cyano-s-triazolo(4,3-b)pyridazine 失效
标题翻译： 3-（5-硝基-2-呋喃基）-6-氰基-S-三唑（4,3-B）吡啶
公开(公告)号：US3962242A
公开(公告)日：1976-06-08
申请号：US545661
申请日：1975-01-30
申请人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Vomel , Winfriede Sauer
发明人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Vomel , Winfriede Sauer
IPC分类号： C07D487/04 , C07D237/26
CPC分类号： C07D487/04
摘要： Nitrofuryl-triazolo[4,3-b]pyridazine compounds of the formula ##SPC1##WhereinR.sub.1 is lower alkoxy radical or a saturated 5- or 6-membered heterocyclic ring attached via a cyclic nitrogen atom, which heterocyclic ring can also contain, in addition to said cyclic nitrogen atom, a cyclic oxygen atom or an optionally lower alkylated cyclic nitrogen atom and R.sub.2 is a hydrogen atom or R.sub.1 and R.sub.2 together represent an additional valency bond,Are outstandingly effective as bacteriostats and are particularly useful in the treatment of bacterial infections in the urinary tract.

5. 发明授权

US3957766A Novel nitrofuran compounds and pharmaceutical compositions 失效
标题翻译：新型硝基化合物和药物组合物
公开(公告)号：US3957766A
公开(公告)日：1976-05-18
申请号：US290682
申请日：1972-09-20
申请人： Herbert Berger , Rudi Gall , Hartmut Merdes , Kurt Stach , Winfriede Sauer , Wolfgang Vomel
发明人： Herbert Berger , Rudi Gall , Hartmut Merdes , Kurt Stach , Winfriede Sauer , Wolfgang Vomel
IPC分类号： C07D487/04 , C07D295/06 , C07D295/12 , C07D471/04
CPC分类号： C07D487/04
摘要： Certain novel nitrofuran compounds of the formula: ##SPC1##WhereinHet is an aromatic heterocylic linkage;B is a bond or vinylene;Y is O or S;m is 0 or 1;X is hydrogen, lower alkyl or alkanoyl; andThe R's are variously defined;Are outstandingly effective bacteriostats and bactericides.

6. 发明授权

US3989832A Combating bacteria with nitroimidazolyl-triazolo-pyridiazine compounds 失效
标题翻译：抗菌与硝基咪唑基 - 三唑并 - 嘧啶化合物
公开(公告)号：US3989832A
公开(公告)日：1976-11-02
申请号：US600533
申请日：1975-07-31
申请人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
发明人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
IPC分类号： C07D487/04 , A01N9/00 , A01N9/22
CPC分类号： C07D487/04
摘要： Nitroimidazolyl-s-triazolo[4,3-b]pyridazines of the formula: ##SPC1##Wherein R is hydrogen or lower alkyl optionally substituted in the 2-position by hydroxyl or by lower acyloxy or lower alkoxy;A is hydrogen, halogen, azido, cyano; lower alkyl, alkoxy, alkylthio, alkylsulfonyl, carboxyl; lower alkoxycarbonyl, lower alkoxycarbonimidoyl; or hydrazino, carbamoyl, amidino or a carboximidohydrazide group optionally substituted by one or two lower acyl, alkyl or cycloalkyl radicals; orA is a radical of the formula: ##EQU1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or a number of organic radicals or, taken together, can be an alkylene bridge; andR.sub.3 is hydrogen or lower alkyl; or, together with R.sub.2, R.sub.3 can form an alkylene bridge;n is 0 or 1;And the pharmaceutically compatible thereof, possess high in vivo effectiveness as antimicrobials.
摘要翻译：具有下式的硝基咪唑基-s-三唑并[4,3-b]哒嗪

7. 发明授权

US4006141A Nitroimidazolyl-triazolo-pyridazine compounds 失效
标题翻译：硝基咪唑基 - 三唑并 - 哒嗪化合物
公开(公告)号：US4006141A
公开(公告)日：1977-02-01
申请号：US601116
申请日：1975-07-31
申请人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
发明人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Nitroimidazolyl-s-triazolo[4,3-b]pyridazines of the formula: ##STR1## wherein R is hydrogen or lower alkyl optionally substituted in the 2-position by hydroxyl or by lower acyloxy or lower alkoxy;A is hydrogen, halogen, azido, cyano; lower alkyl alkoxy, alkylthio, alkylsulfonyl, carboxyl; lower alkoxycarbonyl, lower alkoxycarbonimidoyl; or hydrazino, carbamoyl, amidino or a carboximidohydrazide group optionally substituted by one or two lower acyl, alkyl or cycloalkyl radicals; orA is a radical of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or a number of organic radicals or, taken together, can be an alkylene bridge; andR.sub.3 is hydrogen or lower alkyl; or, together with R.sub.2, R.sub.3 can form an alkylene bridge;n is 0 or 1;And the pharmaceutically compatible thereof, possess high in vivo effectiveness as antimicrobials.
摘要翻译：具有下式的硝基咪唑基-s-三唑并[4,3-b]哒嗪：其中R是氢或在2-位被羟基或低级酰氧基或低级烷氧基任选取代的低级烷基; A是氢，卤素，叠氮基，氰基; 低级烷基烷氧基，烷硫基，烷基磺酰基，羧基; 低级烷氧基羰基，低级烷氧羰基亚氨基; 或肼基，氨基甲酰基，脒基或任选被一个或两个低级酰基，烷基或环烷基取代的碳代酰肼基; 或者A是下式的基团：其中R 1和R 2分别是氢或多个有机基团，或者一起可以是亚烷基桥; 并且R 3是氢或低级烷基; 或者与R 2一起形成亚烷基桥; N IS 0或1; 并且与药物相容，作为抗病毒药物具有高度的生物有效性。

8. 发明授权

US3948912A Nitroimidazolyl-triazolo-pyridazine compounds and therapeutic compositions 失效
标题翻译：硝基咪唑基 - 三唑并 - 哒嗪化合物和治疗组合物
公开(公告)号：US3948912A
公开(公告)日：1976-04-06
申请号：US559285
申请日：1975-03-17
申请人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
发明人： Herbert Berger , Rudi Gall , Kurt Stach , Wolfgang Vomel , Rita Hoffmann
IPC分类号： C07D403/14 , A61K31/5025 , C07D487/04 , C07D237/26
CPC分类号： C07D487/04
摘要： New nitroimidazolyl-triazolo-pyridazines of the formula: ##SPC1##WhereinZ is methyl or amino which can be substituted by lower alkyl,And the pharmacologically compatible acid-addition salts thereof, exhibit outstanding anti-microbial activity against bacteria and protozoa, and also systemic effectiveness.
摘要翻译：新的具有下式的硝基咪唑基 - 三唑并 - 哒嗪：

9. 发明授权

US4267174A Immune-stimulating and cancerostatic 1-acyl-2-cyanoaziridines 失效
标题翻译：免疫刺激和癌性1-酰基-2-氰基氮丙啶
公开(公告)号：US4267174A
公开(公告)日：1981-05-12
申请号：US916389
申请日：1978-06-16
申请人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Rolf Kuhn
发明人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Rolf Kuhn
IPC分类号： C07D499/64 , A61K31/396 , A61K31/43 , A61K31/495 , A61P31/00 , A61P35/00 , A61P37/04 , C07D203/00 , C07D203/18 , C07D203/24 , C07D231/16 , C07D231/20 , C07D231/22 , C07D307/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D487/04 , C07D499/04 , C07F9/564 , F42B3/087 , A61K31/395
CPC分类号： C07D307/68 , C07D203/18 , C07D203/24 , C07D231/16 , C07D231/20 , C07D231/22 , C07F9/564 , Y10S514/885
摘要： 1-Acyl-2-cyanoaziridines of the formula ##STR1## wherein R is an acyl radical of a carboxylic, sulphonic, sulphinic, sulphenic, phosphonic or phosphoric acid,exhibit immune-stimulating and cancerostatic activities.
摘要翻译：其中R是羧酸，磺酸，亚磺酸，磺酸，膦酸或磷酸的酰基的式“IMAGE”的1-酰基-2-氰基氮丙啶表现出免疫刺激和癌症活性。

10. 发明授权

US4282212A Immune-stimulating 1-(N-acylcarbamoyl)-2-cyanoaziridines 失效
标题翻译：免疫刺激1-（N-酰基氨基甲酰基）-2-氰基氮丙啶
公开(公告)号：US4282212A
公开(公告)日：1981-08-04
申请号：US838426
申请日：1977-09-30
申请人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Gottfried Hebold
发明人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Gottfried Hebold
IPC分类号： C07D203/12 , C07D203/06 , C07D203/08 , C07D203/18 , C07D203/20 , C07D203/24 , C07D237/24 , C07D317/68 , C07D333/38 , C07D409/12 , C07D417/12 , C07F9/22 , C07F9/24 , C07F9/564 , A61K31/395
CPC分类号： C07C265/16 , C07D203/06 , C07D203/20 , C07D203/24 , C07D237/24 , C07D317/68 , C07D333/38 , C07F9/564
摘要： 1-(N-Acyl-carbamoyl)-2-cyanoaziridines of the formula ##STR1## wherein X is oxygen or sulphur,Z is hydrogen or an organic radical, andY is a carbonyl, sulphonyl, sulphinyl, sulphenyl, phosphoryl or phosphonyl radical,and salts thereof, exhibit immune-stimulating and cancerostatic activities.
摘要翻译：其中X是氧或硫，Z是氢或有机基团，Y是羰基，磺酰基，亚磺酰基，磺酰基，磷酰基或膦酰基的1-（N-酰基 - 氨基甲酰基）-2-氰基氮丙啶及其盐具有免疫刺激和癌症活性。

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