公开(公告)号：US4835280A

公开(公告)日：1989-05-30

申请号：US72917

申请日：1987-07-14

申请人： Alfred Martens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckman ,  Klaus Strein ,  Egon Roesch

发明人： Alfred Martens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckman ,  Klaus Strein ,  Egon Roesch

IPC分类号： C07D403/12 ,  C07D405/12 ,  C07D487/04

CPC分类号： C07D403/12 ,  C07D405/12 ,  C07D487/04

摘要： The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.

摘要翻译： 本发明提供下式的吲哚衍生物：下式的有用的药物活性吡咯并苯并咪唑或其互变异构体：（I）这些化合物可用于治疗心脏或 循环系统疾病，特别是那些对血压变化作出反应，心输出量增加和/或微循环变化的疾病。

公开(公告)号：US4479962A

公开(公告)日：1984-10-30

申请号：US403968

申请日：1982-08-02

申请人： Fritz Wiedemann ,  Helmut Michel ,  Wolfgang Weckerle ,  Egon Roesch ,  Klaus Strein

发明人： Fritz Wiedemann ,  Helmut Michel ,  Wolfgang Weckerle ,  Egon Roesch ,  Klaus Strein

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/433 ,  A61K31/495 ,  A61K31/496 ,  A61P9/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/32 ,  C07D209/42 ,  C07D209/43 ,  C07D209/44 ,  C07D209/88 ,  C07D231/56 ,  C07D235/04 ,  C07D235/06 ,  C07D235/08 ,  C07D235/26 ,  C07D241/40 ,  C07D241/42 ,  C07D249/18 ,  C07D285/14

CPC分类号： C07D285/14 ,  C07D209/08 ,  C07D209/88 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08 ,  C07D235/26 ,  C07D241/42 ,  C07D249/18

摘要： The present invention provides heteroaryloxypropanolamines and pharmaceutical compositions containing them, for combating, and for the prophylaxis of, cardiac and circulatory diseases. The heteroaryloxypropanolamines of the present invention are of the general formula: ##STR1## wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straight-chained or branched alkylene chain containing 2 to 6 carbon atoms, R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulfur or oxygen and R.sub.6, R.sub.7 and R.sub.8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R.sub.6 and R.sub.7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

摘要翻译： 本发明提供含有它们的异丙氧基丙醇胺和含有它们的药物组合物，用于对抗和预防心脏和循环系统疾病。 本发明的杂芳氧基丙酰胺具有以下通式：其中A是双环或三环杂芳族基，其任选地部分氢化，X是含有2-6个碳原子的直链或支链亚烷基链，R 1 和R 2可以相同或不同，为氢原子或低级烷基或苄基，R 3，R 4和R 5可相同或不同，为氢原子或低级烷基，苄基，甲酰基，低级烷酰基，氰基 ，羟甲基，低级烷氧基羰基或氨基甲酰基或二价取代基硫或氧，R 6，R 7和R 8可以相同或不同，为氢或卤原子，低级烷基，硝基，氨基，低级烷硫基或低级烷氧基或 R6和R7一起表示任选不饱和的三亚甲基链; 及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法，以及含有它们的药物组合物。

公开(公告)号：US4438116A

公开(公告)日：1984-03-20

申请号：US302894

申请日：1981-09-16

申请人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

发明人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

IPC分类号： A61K31/505 ,  A61P9/00 ,  C07D241/38 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  A61K31/495 ,  C07D241/42

CPC分类号： C07D241/38 ,  C07D241/44 ,  Y10S514/929

摘要： An aminopropanol compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from hydrogen and lower alkyl; orR.sub.1 and R.sub.2 together represent an alkylene radical;R.sub.3 is hydrogen or acyl;A is one of the following structures ##STR2## wherein R.sub.4 is hydrogen or lower alkyl optionally substituted by hydroxyl halogen and lower alkylthio; andR.sub.5 and R.sub.6 are individually selected from lower alkyl;B is alkylamino which optionally carries a phenyl and a phenoxy radical optionally substituted by at at least one of halogen, hydroxyl or lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl; orB is an aryl- or heteroaryloxymethylpiperidine radical optionally substituted by at least one of halogen hydroxyl or lower alkyl, hydroxyl alkyl or carboxamido alkyl, or by lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino;and the pharmacologically acceptable salts thereof, are outstandingly effective beta blockers and blood-pressure depressants.

摘要翻译： 式IMAMA的氨基丙醇化合物，其中R 1和R 2分别选自氢和低级烷基; 或者R 1和R 2一起表示亚烷基; R3是氢或酰基; A是下列结构之一，其中R4是氢或任选被羟基卤素和低级烷硫基取代的低级烷基; 并且R 5和R 6分别选自低级烷基; B是烷基氨基，其任选地带有苯基和苯氧基，其任选被至少一个卤素，羟基或低级烷基，低级酰基，低级烷硫基，酰氨基，氨基羰基，低级烷氧基，低级烯氧基，苯氧基，低级烯基，低级烷基磺酰基 ，低级烷基亚磺酰基或卤代烷基; 或B是任选被卤素羟基或低级烷基，羟基烷基或甲酰胺基烷基中的至少一个取代的芳基或杂芳氧基甲基哌啶基，或由低级烷氧基，低级酰基，氨基，甲酰氨基，低级烷基羰基酰氨基或低级烷基磺酰基氨基取代; 和其药理学上可接受的盐是显着有效的β受体阻滞剂和降压药。

公开(公告)号：US4428955A

公开(公告)日：1984-01-31

申请号：US372415

申请日：1982-04-27

申请人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Egon Roesch ,  Otto-Henning Wilhelms

发明人： Walter-Gunar Friebe ,  Wolfgang Kampe ,  Egon Roesch ,  Otto-Henning Wilhelms

IPC分类号： C07D409/14 ,  A61K31/35 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07D311/22 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D405/12 ,  Y10S514/87

摘要： The present invention provides benzopyranyl ethers of the general formula: ##STR1## wherein A is an alkylene radical containing 2 to 4 carbon atoms and R is a hydrogen atom or an acyl radical; as well as the salts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for treating allergic diseases.

摘要翻译： 本发明提供以下通式的苯并吡喃基醚：其中A是含有2至4个碳原子的烷基，R是氢原子或酰基; 以及其与药理学上可接受的酸的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。 此外，本发明涉及这些化合物用于治疗过敏性疾病的用途。

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。

公开(公告)号：US3997667A

公开(公告)日：1976-12-14

申请号：US544721

申请日：1975-01-28

申请人： Ernst-Christian Witte ,  Kurt Stach ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch

发明人： Ernst-Christian Witte ,  Kurt Stach ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch

IPC分类号： C07D295/08 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096

CPC分类号： C07D295/088

摘要： New 1-[3-naphth-1-yloxy)-propyl]-piperazine compounds of the formula: ##STR1## wherein X is hydrogen or methoxy;And the pharmacologically compatible salts thereof;Are outstandingly effective in lowering blood pressure and are thus useful as anti-hypertensive agents.

摘要翻译： 新的1- [3-萘-1-基氧基） - 丙基] - 哌嗪化合物，其结构式如下：其中X是氢或甲氧基; 及其药理学兼容性; 在降低血液压力方面非常有效，并且有效地作为抗高血压药物。

公开(公告)号：US3991188A

公开(公告)日：1976-11-09

申请号：US593089

申请日：1975-07-03

申请人： Ansgar Lerch ,  Alfred Popelak ,  Kurt Stach ,  Egon Roesch ,  Klaus Hardebeck

发明人： Ansgar Lerch ,  Alfred Popelak ,  Kurt Stach ,  Egon Roesch ,  Klaus Hardebeck

IPC分类号： A61K31/63 ,  A61K31/625

CPC分类号： A61K31/63 ,  Y10S514/869

摘要： New 3-alkyl-4-sulfamoyl-aniline compounds of the formula ##SPC1##WhereinR.sub.1 is phenyl, furyl or thienyl;R.sub.2 is carboxyl or tetrazolyl-(5)R.sub.4 is a straight-chain or branched alkyl radical of from 2 to 5 carbon atoms; andn is 1 or 2;And the pharmacologically compatible salts thereof; are outstandingly effective saluretic compounds, particularly when administered enterally.

摘要翻译： 式WHEREIN R1的新的3-烷基-4-氨磺酰基 - 苯胺化合物是苯基，呋喃基或噻吩基; R2是羧基或四唑基 - （5）R4是2至5个碳原子的直链或支链烷基; 和N IS 1 OR 2; 及其药理学兼容性; 具有非常有效的挥发性化合物，特别是在进行管理时尤其如此。

公开(公告)号：US4695567A

公开(公告)日：1987-09-22

申请号：US820259

申请日：1986-01-17

申请人： Alfred Mertens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Egon Roesch

发明人： Alfred Mertens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Egon Roesch

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/50 ,  A61K31/505 ,  A61P9/00 ,  A61P9/04 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04 ,  C07D403/06

CPC分类号： C07D403/12 ,  C07D405/12 ,  C07D487/04

摘要： The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.

摘要翻译： 本发明提供了以下通式的吡咯并苯并咪唑或其互变异构体：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 7环烷基; R2是氢，氰基，C1-C6烷基，C2-C6烯基或被羟基，C1-C6烷基，C1-C6烷氧基，氨基，C1-C6烷基氨基，C2-C12二烷基氨基或肼基取代的羰基或R2 并且R 1与它们所连接的碳一起形成C 3 -C 8螺环烷基环，或者R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基，X是价键，C 1 -C 4亚烷基或亚乙烯基，T是 氧或硫; 并且Het是呋喃基，噻吩基，吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基，噻二唑基，吡嗪基，嘧啶基或哒嗪基，其中杂环五元和六元环是未取代的或被一个或多个C 1 -C 6烷基 C 1 -C 6烷氧基，C 1 -C 6烷硫基，羟基，氧代，硝基，氨基，卤素，羧基，C 2 -C 7烷氧基羰基，氨基羰基或氰基; 或其生理上可接受的盐与无机或有机酸反应。 这些化合物可用于治疗心脏或循环系统疾病，特别是那些响应血压变化，心输出量增加和/或微循环变化的化合物。

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。

公开(公告)号：US4367235A

公开(公告)日：1983-01-04

申请号：US171940

申请日：1980-07-18

申请人： Carl H. Ross ,  Walter-Gunar Friebe ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Egon Roesch

发明人： Carl H. Ross ,  Walter-Gunar Friebe ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Egon Roesch

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61P9/00 ,  A61P25/02 ,  C07D235/02 ,  C07D235/26

CPC分类号： A61K31/415 ,  C07D235/02 ,  C07D235/26

摘要： 2-benzimidazolinone compounds of the formula ##STR1## wherein R is lower alkyl,R.sub.1 and R.sub.2, which can be the same or different, are lower straight-chained or branched alkyl and one of R.sub.1 and R.sub.2 can also be hydrogen orR.sub.1 and R.sub.2 together represent an alkylene radical and R.sub.3 is hydrogen or acyl, i.e., alkanoyl or aromatic carboxylic acid moieties;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.

摘要翻译： 其中R是低级烷基，可以相同或不同的R 1和R 2的低级直链或支链烷基，R 1和R 2之一也可以是氢或R 1和R 2 一起代表亚烷基，R3是氢或酰基，即烷酰基或芳族羧酸部分; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。