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1. 发明授权

US4826847A Beta-blocking oxindole derivatives 失效
标题翻译： β-阻断羟吲哚衍生物
公开(公告)号：US4826847A
公开(公告)日：1989-05-02
申请号：US948422
申请日：1986-12-30
申请人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
发明人： Helmut Michel , Wolfgang Kampe , Klaus Strein , Wolfgang Bartsch
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/02 , C07D209/34 , C07D209/96 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , A61K31/505
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06
摘要： The present invention provides oxindole derivatives of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The above compounds display nitrate-like as well as .beta.-blocking actions.
摘要翻译：本发明提供下式的羟吲哚衍生物：其中各种取代基在下文定义。上述化合物显示硝酸盐样和β-阻断作用。

2. 发明授权

US4612313A Pharmaceutical phenylacetonitrile derivatives 失效
标题翻译：药用苯乙腈衍生物
公开(公告)号：US4612313A
公开(公告)日：1986-09-16
申请号：US774354
申请日：1985-09-10
申请人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
发明人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
IPC分类号： A61K31/21 , A61K31/275 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , C07C67/00 , C07C253/00 , C07C255/24 , C07C255/32 , C07C255/42 , C07C255/43 , C07C255/53 , C07C255/58 , C07C255/59 , C07D207/08 , C07D211/22 , C07D241/04 , C07D295/16 , C07D295/18 , A61K31/495 , C07C121/80
CPC分类号： C07C255/00 , C07D211/22
摘要： The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的苯乙腈衍生物：其中R 1，R 2，R 3，R 4和R 5可以相同或不同，为氢或卤素原子或烷基，烷氧基，硝基，氨基或酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基，A是下列通式的基团：其中R 6是含有2至12个直链的直链，环状或支链的饱和或不饱和烷基碳原子，R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基，m和n可相同或不同，为2或3，p为1或2，X为是含有2至10个碳原子的直链，环状或支链烷基，其任选被氨基取代，或者是通式如下的基团：其中Y和Z可以相同或不同，是直链或支链烷基基团引入多达8个碳原子或环烷基，烷基环烷基或环烷基烷基，其中这些基团任选地被氧或硫原子中断，通式II中的基团Z之一也可以是氢原子或两个Z基团连接形成含有4至6个碳原子的环，其任选被可被烷基或烷酰基取代的另外的氮原子中断，-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。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。

3. 发明授权

US4863949A Aminopropanol derivatives, processes for the preparation thereof, the use thereof and pharmaceutical compositions containing them 失效
标题翻译：氨基丙醇衍生物，其制备方法，其用途和含有它们的药物组合物
公开(公告)号：US4863949A
公开(公告)日：1989-09-05
申请号：US98719
申请日：1987-09-21
申请人： Herbert Simon , Helmut Michel , Wolfgang Bartsch , Klaus Strein
发明人： Herbert Simon , Helmut Michel , Wolfgang Bartsch , Klaus Strein
IPC分类号： C07D521/00 , A61K31/13 , A61K31/165 , A61K31/17 , A61K31/215 , A61K31/27 , A61K31/33 , A61K31/445 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/02 , C07C67/00 , C07C203/02 , C07C231/00 , C07C233/00 , C07C233/12 , C07C233/34 , C07C235/10 , C07C313/00 , C07C315/04 , C07C317/18 , C07C317/20 , C07C317/28 , C07C317/30 , C07C317/46 , C07C319/20 , C07C323/20 , C07D209/04 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/82 , C07D215/22 , C07D215/227 , C07D235/06 , C07D311/18
CPC分类号： C07D209/08 , C07C255/00 , C07D209/34 , C07D209/42 , C07D215/227 , C07D311/18
摘要： The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.1 -- group and a --CH.sub.2 -- group of the chain B, can form a heteroaliphatic ring containing 4 to 6 carbon atoms and n is 1, 2 or 3; and the physiologically acceptable salts thereof. 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 the treatment and/or prophylaxis of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的化合物：其中Ar是取代或未取代的芳族或杂芳族基团，A是含有至多8个碳原子的直链或支链亚烷基链，-CH 2 - 基团其中可以被含有3至7个碳原子的亚环烷基代替，B是含有至多12个碳原子的直链单环或双环，任选支链，饱和或不饱和的亚烷基链，其中-CH 2 - 基团可以可以被含有3至7个碳原子的亚环烷基和/或最多两个-CH 2 - 基团取代，其中可以被氧或硫原子或-S（= O）或-S（= O）取代） 2基团，X是价键，氧原子或-NR 1基团，其中R 1是氢原子或含有至多6个碳原子的直链或支链，饱和或不饱和的烷基或硝基烷基或R 1，一起与-NR 1基团的氮原子和链B的-CH 2 - 基团可以相同 rm是含有4至6个碳原子的杂脂族环，n为1,2或3; 及其生理上可接受的盐。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和/或预防心脏和循环系统疾病的用途。

4. 发明授权

US4642309A Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效
公开(公告)号：US4642309A
公开(公告)日：1987-02-10
申请号：US780704
申请日：1985-09-26
申请人： Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
发明人： Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P25/02 , C07D209/34 , C07D401/06 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
摘要： The present invention provides indolin-2-one derivatives of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl radical or a radical of the general formula: ##STR2## in which A is a straight-chained or branched C.sub.2 -C.sub.4 alkylene radical and Z is an oxygen or sulphur atom, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, C.sub.2 -C.sub.6 alkanoyl radicals, C.sub.2 -C.sub.4 alkenyl radicals, C.sub.2 -C.sub.4 alkynyl radicals, C.sub.1 -C.sub.6 alkyl radicals, C.sub.1 -C.sub.6 alkoxy radicals, C.sub.2 -C.sub.4 alkenyloxy radicals, C.sub.2 -C.sub.4 alkynyloxy radicals, C.sub.1 -C.sub.6 alkylthio radicals, C.sub.2 -C.sub.6 alkanoylamido radicals or radicals of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 alkyl radicals or C.sub.3 -C.sub.10 cycloalkyl radicals or R.sub.4 and R.sub.5 together represent a C.sub.2 -C.sub.8 alkylene radical optionally interrupted by an oxygen or sulphur atom or by an >N-R.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical, X is a hydrogen atom, Y is a hydrogen atom or a group of the general formula ##STR4## in which Q is a hydrogen atom or, together with X, can also represent a bond and R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxyl or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by halogen, hydroxyl, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulphinyl, C.sub.1 14 C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, methylenedioxy, nitro, cyano or amino, with the proviso that R.sub.1 cannot be a C.sub.1 -C.sub.6 alkyl radical when X and Y are both hydrogen atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides intermediates of the general formula: ##STR5## in which R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxy or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by hydroxyl, halogen, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 14 C.sub.6 alkylsulphinyl, cyano C.sub.1 -C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, nitro amino or methylenedioxy.Furthermore, the invention provides processes for the preparation of the above indolin-2-one derivatives and the above intermediates, as well as pharmaceutical compositions containing the above indolin-2-one derivatives.

5. 发明授权

US4438116A Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them 失效
标题翻译：具有降血压和β-阻断性能的喹喔啉氧基 - 氨基 - 丙醇化合物，它们的用途和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。

6. 发明授权

US4378363A Certain heterocyclic-carboxamido-phenoxy-aminopropanols, compositions containing same and methods of using same 失效
标题翻译：某些杂环 - 甲酰胺基 - 苯氧基 - 氨基丙醇，含有它们的组合物及其使用方法
公开(公告)号：US4378363A
公开(公告)日：1983-03-29
申请号：US207527
申请日：1980-11-17
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4406 , A61K31/4418 , A61K31/455 , A61P9/00 , A61P25/02 , C07D207/26 , C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D209/43 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85
CPC分类号： C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85 , Y10S514/821
摘要： This invention relates to new aminopropanol compounds having beta-adrenergic activity. In addition, the invention is directed to pharmaceutical compositions containing such compounds for the treatment of cardiac and circulatory infirmities and to methods for treating such infirmities.More particularly, the invention relates to new aminopropanol compound of the formula ##STR1## wherein R.sub.1 is a low alkyl moiety, which can be substituted, if desired, by a group Z-R.sub.5 ;R.sub.2 is hydrogen or a low alkanoyl group;R.sub.3 is a mono- or bicyclic heterocyclic compound having 1 to 2 hetero atoms, which can be mono- or polysubstituted, if desired, by halogen, amino, hydroxyl, low alkoxyl, low alkyl;R.sub.4 is hydrogen, a low alkanoyl group or an aroyl group;R.sub.5 is hydrogen or a carbocyclic or heterocyclic aryl moiety, which can be mono- or polysubstituted, if desired, by hydroxyl, low alkyl, low alkenyl, low alkoxyl or low alkenyloxyl;X is a valence bond or a methylene group; andZ is a valence bond, an oxygen atom, or a sulfur atom, and their pharmacologically compatible salts.
摘要翻译：本发明涉及具有β-肾上腺素能活性的新的氨基丙醇化合物。此外，本发明涉及含有用于治疗心脏和循环系统疾病的化合物的药物组合物以及用于治疗这些病症的方法。更具体地，本发明涉及式（I）的新的氨基丙醇化合物，其中R 1是低级烷基部分，如果需要，可以被Z-R5基团取代; R2是氢或低烷酰基; R3是具有1至2个杂原子的单环或双环杂环化合物，如果需要，可以被卤素，氨基，羟基，低烷氧基，低级烷基单取代或多取代; R4是氢，低级烷酰基或芳酰基; R5是氢或碳环或杂环芳基部分，如果需要，可以被羟基，低级烷基，低级链烯基，低烷氧基或低链烯氧基单取代或多取代; X是价键或亚甲基; Z是价键，氧原子或硫原子，以及它们的药理学上相容的盐。

7. 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。

8. 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。

9. 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。

10. 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。

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