公开(公告)号：US4243807A

公开(公告)日：1981-01-06

申请号：US737518

申请日：1976-11-01

Applicant: Walter-Gunar Friebe ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator

Inventor： Walter-Gunar Friebe ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator

IPC: C07D211/18 ,  C07D211/22 ,  C07D213/26 ,  C07D213/30

CPC classification number: C07D211/22 ,  C07D211/18

Abstract: 4-Phenoxymethyl-piperidines of the formula ##STR1## wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.

Abstract translation: 其中R为氢，卤素，硝基，低级烷基或低级烷氧基的式为“IMAGE”的4-苯氧基甲基 - 哌啶，以游离碱或酸加成盐的形式提供，它们可用作生产中的中间体 的抗高血压药通过与（a）丙基氯然后与腺嘌呤缩合，或（b）丙基吲哚。

公开(公告)号：US4229464A

公开(公告)日：1980-10-21

申请号：US943512

申请日：1978-09-18

Applicant: Wolfgang Kampe ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

Inventor： Wolfgang Kampe ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

IPC: C07D209/43 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P25/02 ,  C07D209/08 ,  C07D209/12 ,  C07D209/32 ,  C07D209/42 ,  C07D209/18 ,  C07D209/20

CPC classification number: C07D209/42 ,  C07D209/08 ,  C07D209/12 ,  Y10S514/927

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4049811A

公开(公告)日：1977-09-20

申请号：US676269

申请日：1976-04-12

Applicant: Herbert Berger ,  Alfred Rhomberg ,  Kurt Stach ,  Wolfgang Vomel ,  Winfriede Sauer

Inventor： Herbert Berger ,  Alfred Rhomberg ,  Kurt Stach ,  Wolfgang Vomel ,  Winfriede Sauer

IPC: C07D221/08 ,  C07D221/10 ,  C07D221/16 ,  A61K31/47

CPC classification number: C07D221/08 ,  C07D221/10 ,  C07D221/16

Abstract: Cycloalkano-quinolone derivatives having anti-microbial activity characterized by the formula: ##STR1##wherein one of R.sub.1 and R.sub.2 designates hydrogen, halogen, nitro, amino, hydroxyl, acylamino, acyloxy, alkoxy or aryloxy and the other taken together with R.sub.3 forms an alkylene bridge containing 2 to 6 carbon atoms, X is hydrogen, lower alkyl, which may be substituted by a member of the group consisting of halogen, hydroxyl, acyloxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylmercapto, arylmercapto, arylsulfonyl, and alkylsulfonyl, or X is unsubstituted alkenyl including alkadienyl, or alkynyl and Y is hydroxyl, amino or lower alkoxy, and the pharmaceutically acceptable salts thereof.

Abstract translation: 具有以下结构式表征的抗微生物活性的环烷醇 - 喹诺酮衍生物：其中R 1和R 2之一表示氢，卤素，硝基，氨基，羟基，酰氨基，酰氧基，烷氧基或芳氧基，另一个与R 3一起形成 含有2至6个碳原子的亚烷基桥，X是氢，可以被卤素，羟基，酰氧基，烷氧基，芳氧基，芳烷氧基，巯基，烷基巯基，芳基巯基，芳基磺酰基和烷基磺酰基中的成员所取代的低级烷基 或X为未取代的烯基，包括链二烯基或炔基，Y为羟基，氨基或低级烷氧基，及其药学上可接受的盐。

公开(公告)号：US4034096A

公开(公告)日：1977-07-05

申请号：US595953

申请日：1975-07-14

Applicant: Alfred Rhomberg ,  Herbert Berger ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Vomel ,  Winfriede Sauer

Inventor： Alfred Rhomberg ,  Herbert Berger ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Vomel ,  Winfriede Sauer

IPC: C07D221/16 ,  C07D215/56

CPC classification number: C07D221/16

Abstract: New cyclopenteno-quinolone derivatives of the formula ##STR1## wherein R is a saturated or unsaturated aliphatic hydrocarbyl, e.g., alkyl and alkenyl,X is hydrogen or alkyl, andY is halogen, azido, alkylthio, alkyl-sulfonyl, or nitrile or unsubstituted or substituted (e.g., alkyl mono or di-substituted) amino;And the pharmacologically compatible salts thereof; are outstandingly effective as bacteriostats in mammals.

Abstract translation: 其中R是饱和或不饱和脂族烃基，例如烷基和链烯基，X是氢或烷基，Y是卤素，叠氮基，烷硫基，烷基磺酰基或腈或未取代的新的环戊烯 - 喹诺酮衍生物 或取代的（例如烷基单或二取代的）氨基; 及其药理学兼容性; 作为母体中的细菌具有非常有效的作用。

公开(公告)号：US4006141A

公开(公告)日：1977-02-01

申请号：US601116

申请日：1975-07-31

Applicant: Herbert Berger ,  Rudi Gall ,  Kurt Stach ,  Wolfgang Vomel ,  Rita Hoffmann

Inventor： Herbert Berger ,  Rudi Gall ,  Kurt Stach ,  Wolfgang Vomel ,  Rita Hoffmann

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US3966743A

公开(公告)日：1976-06-29

申请号：US504589

申请日：1974-09-09

Applicant: Herbert Berger ,  Alfred Rhomberg ,  Kurt Stach ,  Wolfgang Vomel ,  Winfriede Sauer

Inventor： Herbert Berger ,  Alfred Rhomberg ,  Kurt Stach ,  Wolfgang Vomel ,  Winfriede Sauer

IPC: C07D221/08 ,  C07D221/10 ,  C07D221/16 ,  C07D215/56

CPC classification number: C07D221/16 ,  C07D221/08 ,  C07D221/10

Abstract: Cycloalkano-quinolone derivatives having anti-microbial activity characterized by the formula: ##SPC1##Wherein one of R.sub.1 and R.sub.2 designates hydrogen, halogen, nitro, amino, hydroxyl, acylamino, acyloxy, alkoxy or aryloxy and the other taken together with R.sub.3 forms an akylene bridge containing 2 to 6 carbon atoms, X is hydrogen, lower alkyl, which may be substituted by a member of the group consisting of halogen, hydroxyl, acyloxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylmercapto, arylmercapto, arylsulfonyl, and alkylsulfonyl, or X is unsubstituted alkenyl including alkadienyl, or alkynyl and Y is hydroxyl, amino or lower alkoxy, and the pharmaceutically acceptable salts thereof.

Abstract translation: 具有抗细菌活性的环烷醇 - 喹诺酮衍生物，其特征在于下式：

公开(公告)号：US3948912A

公开(公告)日：1976-04-06

申请号：US559285

申请日：1975-03-17

Applicant: Herbert Berger ,  Rudi Gall ,  Kurt Stach ,  Wolfgang Vomel ,  Rita Hoffmann

Inventor： Herbert Berger ,  Rudi Gall ,  Kurt Stach ,  Wolfgang Vomel ,  Rita Hoffmann

IPC: C07D403/14 ,  A61K31/5025 ,  C07D487/04 ,  C07D237/26

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 新的具有下式的硝基咪唑基 - 三唑并 - 哒嗪：

公开(公告)号：US3947404A

公开(公告)日：1976-03-30

申请号：US367312

申请日：1973-06-05

Applicant: Fritz Kaiser ,  Wolfgang Schaumann ,  Kurt Stach ,  Wolfgang Voigtlander

Inventor： Fritz Kaiser ,  Wolfgang Schaumann ,  Kurt Stach ,  Wolfgang Voigtlander

IPC: C07J19/00 ,  A61K20060101 ,  C07D20060101

Abstract: New dihydrodigoxin derivatives of the formula ##SPC1##Wherein one of R.sub.1 and R.sub.2 represents a methyl or ethyl radical and the other represents hydrogen, methyl, ethyl or acetyl (i.e. alkanoyl; and R.sub.3 is hydrogen or an acetyl group; are outstandingly effective for therapy of cardiac insufficiencies, particularly via peroral administration.

Abstract translation: 式R 1和R 2的新的二氢二磷杂衍生物代表甲基或乙基，另一个表示氢，甲基，乙基或乙酰基（即烷酰基; R 3是氢或乙酰基）;对治疗心脏功能不全有显着的效果 ，特别是通过口腔管理。

公开(公告)号：US4172136A

公开(公告)日：1979-10-23

申请号：US889594

申请日：1978-03-23

Applicant: Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  Max Thiel ,  Wolfgang Vomel

Inventor： Herbert Berger ,  Rudi Gall ,  Kurt Stach, deceased ,  Max Thiel ,  Wolfgang Vomel

IPC: C07D231/16 ,  C07D401/02 ,  C07D403/02

CPC classification number: C07D231/16

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4152446A

公开(公告)日：1979-05-01

申请号：US805558

申请日：1977-06-10

Applicant: Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

Inventor： Wolfgang Kampe ,  Kurt Stach ,  Max Thiel ,  Wolfgang Bartsch ,  Karl Dietmann ,  Egon Roesch ,  Wolfgang Schaumann

IPC: C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  A61K31/40 ,  C07D209/04

CPC classification number: C07D209/42 ,  C07D209/08 ,  C07D209/12

Abstract: 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.

Abstract translation: 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。