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11. 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.

12. 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。

13. 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。

14. 发明授权

US4704381A Use of adenosine derivatives as anti-allergic compounds and pharmaceutical compositions containing them 失效
标题翻译：使用腺苷衍生物作为抗过敏化合物和含有它们的药物组合物
公开(公告)号：US4704381A
公开(公告)日：1987-11-03
申请号：US701139
申请日：1985-02-13
申请人： Wolfgang Schaumann , Otto-Henning Wilhelms , Androniki Roesch , Wolfgang Kampe
发明人： Wolfgang Schaumann , Otto-Henning Wilhelms , Androniki Roesch , Wolfgang Kampe
IPC分类号： C07H19/167 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P37/08 , C07H19/16 , C07H19/06
CPC分类号： C07H19/16 , A61K31/70
摘要： The present invention is concerned with the use of adenosine derivatives for the treatment of allergic diseases, as well as for bronchosphatic and broncho-constrictive reactions brought about by inflammation. The above adenosine derivatives can be used alone or together with xanthine derivatives. The invention is further concerned with compositions containing compounds of adenosine derivatives and optionally compounds of xanthine derivatives together with appropriate pharmaceutical carriers.
摘要翻译：本发明涉及腺苷衍生物用于治疗过敏性疾病以及由炎症引起的支气管和支气管收缩反应的用途。上述腺苷衍生物可以单独使用或与黄嘌呤衍生物一起使用。本发明还涉及含有腺苷衍生物和任选的黄嘌呤衍生物化合物与合适的药物载体的组合物。

15. 发明授权

US4486442A Anti-allergy bicyclic phenol ethers 失效
标题翻译：抗过敏双酚酚醚
公开(公告)号：US4486442A
公开(公告)日：1984-12-04
申请号：US469856
申请日：1983-02-25
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Androniki Roesch nee Apostolides , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Androniki Roesch nee Apostolides , Wolfgang Schaumann
IPC分类号： A61K31/443 , A61K31/445 , A61P37/08 , C07D307/83 , C07D401/12 , C07D405/12 , C07D409/12
CPC分类号： C07D401/12 , C07D307/83 , C07D405/12
摘要： The present invention provides bicyclic phenol ethers of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom or an acyl radical,X is an oxygen or sulphur atom or an --NH-- group;Y is a --CO--CHR.sub.3 -- group or a ##STR2## group; R.sub.3 is a hydrogen atom, a lower alkyl radical which can be optionally substituted by an aryl radical, or a cycloalkyl radical containing 3 to 7 carbon atoms; andR.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, lower alkyl radicals, lower alkyl radicals, alkenyl radicals containing 2 to 16 carbon atoms, which can be optionally substituted by an aryl radical, or an aryl radical; orR.sub.4 and R.sub.5, together with the carbon atom to which they are attached, form a cycloalkyl ring containing 3 to 7 carbon atoms; and thesalts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的双环酚醚：其中R 1为氢原子或低级烷基，R 2为氢原子或酰基，X为氧或硫原子或 - NH-基团; Y是-CO-CHR3-基团或基团; R3是氢原子，可任意被芳基取代的低级烷基或含有3至7个碳原子的环烷基; 和可以相同或不同的R 4和R 5是氢原子，低级烷基，低级烷基，含有2至16个碳原子的烯基，其可任选被芳基或芳基取代; 或R 4和R 5与它们所连接的碳原子一起形成含有3至7个碳原子的环烷基环; 其盐与药理学上可接受的酸。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。

16. 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。

17. 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。

18. 发明授权

US4608383A Cardioactive pyrazole and imidazole aryloxypropanolamines 失效
公开(公告)号：US4608383A
公开(公告)日：1986-08-26
申请号：US538693
申请日：1983-10-03
申请人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
发明人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
IPC分类号： A61K31/38 , A61K31/045 , A61K31/135 , A61K31/138 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/04 , C07C217/32 , C07C217/72 , C07C217/78 , C07C219/06 , C07C219/08 , C07C219/14 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/46 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/54 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D241/44 , C07D249/18 , C07D333/36 , C07D473/16 , C07D473/32 , C07D473/34 , C07D487/00 , C07D487/04 , C07D231/54 , C07D233/48 , C07D233/88
CPC分类号： C07D473/16 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D333/36 , C07D473/34 , C07D487/04
摘要： The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, notro, hydraxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, halomethyl, aminomethyl, lower acylaminomethyl, di(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acyaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. These compounds are useful for the prophylaxis and combatting of cardiac and circulatory diseases.

19. 发明授权

US4468520A 3-Cyano-indoles as cardioselective agents 失效
标题翻译： 3-氰基 - 吲哚作为心脏选择剂
公开(公告)号：US4468520A
公开(公告)日：1984-08-28
申请号：US288075
申请日：1981-07-29
申请人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch , Karl Dietmann , Gisbert Sponer
发明人： Helmut Michel , Wolfgang Kampe , Roland Ofenloch , Karl Dietmann , Gisbert Sponer
IPC分类号： C07D209/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , C07D209/08 , C07D209/42 , C07D209/43 , C07D209/04
CPC分类号： C07D209/08
摘要： The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically 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 prophylaxis and treatment of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的氨基丙醇衍生物：其中R1是氢原子或低级烷酰基或芳酰基，R2是低级烷基或通式如下的基团：其中 X是价键，亚甲基或氧或硫原子，Ar是单环，碳或杂环芳基，R6和R7可以相同或不同，是氢原子或低级烷基，R8和 R9可相同或不同，为氢或卤原子，羟基，低级烷酰基，烯基，炔基，烷基，低级烷氧基，芳烷氧基，烯氧基，炔氧基，低级烷硫基，氨基羰基自由基，氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基，R'2为氢原子或苄基，R 3为羧基或低级烷氧基羰基，氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基，R1具有与上述相同的含义，R 5是氢原子或低级烷基; 其任选活性形式和外消旋物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预防和治疗心脏和循环系统疾病的用途。

20. 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。

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