公开(公告)号：US4503067A

公开(公告)日：1985-03-05

申请号：US479921

申请日：1983-04-04

申请人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

发明人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61P9/08 ,  A61P25/02 ,  C07D209/88 ,  C07D317/64 ,  C07D401/12 ,  C07D405/12 ,  C07D209/82

CPC分类号： C07D209/88 ,  C07D317/64

摘要： Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

摘要翻译： 式（I）的羧基 - （4） - 氧丙醇胺化合物，其中R 1是氢，低级烷酰基或芳酰基; R2是氢，低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基，或者当X是氧时，R4与R5一起可以代表-CH2-O-; X是价键，-CH 2 - ，氧或硫; Ar是单环或双环芳基或吡啶基; R5和R6分别选自氢，卤素，羟基，低级烷基，氨基羰基，低级烷氧基，芳烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。

公开(公告)号：US4146630A

公开(公告)日：1979-03-27

申请号：US846057

申请日：1977-10-27

申请人： Wolfgang Kampe ,  Walter-Gunar Friebe ,  Fritz Wiedemann ,  Gisbert Sponer ,  Wolfgang Bartsch ,  Karl Dietmann

发明人： Wolfgang Kampe ,  Walter-Gunar Friebe ,  Fritz Wiedemann ,  Gisbert Sponer ,  Wolfgang Bartsch ,  Karl Dietmann

IPC分类号： C07D401/12 ,  A61K31/403 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D209/90 ,  C07D211/22 ,  C07D231/56

CPC分类号： C07D211/22 ,  C07D231/56

摘要： A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.

公开(公告)号：US3998810A

公开(公告)日：1976-12-21

申请号：US487423

申请日：1974-07-10

申请人： Fritz Wiedemann ,  Max Thiel ,  Kurt Stach ,  Karl Dietmann ,  Gisbert Sponer

发明人： Fritz Wiedemann ,  Max Thiel ,  Kurt Stach ,  Karl Dietmann ,  Gisbert Sponer

IPC分类号： A61K31/135 ,  A61K31/00 ,  A61K31/395 ,  A61K31/54 ,  A61K31/5415 ,  A61P9/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/30 ,  C07D209/82 ,  C07D209/86 ,  C07D223/24 ,  C07D223/28 ,  C07D279/24 ,  C07D279/28

CPC分类号： C07D209/86

摘要： New N-substituted 1-amino-3-phenoxy-propan-2-ol compounds of the formula: ##EQU1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or, taken together, represent a sulfur linkage, an ethylene radical or a valency bond;B is straight or branched chain alkylene or hydroxyalkylene of from 2 to 5 carbon atoms; andR.sub.3 is hydrogen or alkyl of up to 3 carbon atoms;And the physiologically compatible salts thereof; possess valuable cardiac and circulatory activity.

公开(公告)号：US4438128A

公开(公告)日：1984-03-20

申请号：US273543

申请日：1981-06-15

申请人： Fritz Wiedemann ,  Wolfgang Kampe ,  Karl Dietmann ,  Gisbert Sponer

发明人： Fritz Wiedemann ,  Wolfgang Kampe ,  Karl Dietmann ,  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

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, carboxamido, 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, nitro, hydroxylamino, 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, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-(lower alkoxycarbonyl)-ethyl, 2-carboxyethyl, 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.

公开(公告)号：US4029783A

公开(公告)日：1977-06-14

申请号：US638874

申请日：1975-12-08

申请人： Fritz Wiedemann ,  Max Thiel ,  Kurt Stach ,  Karl Dietmann ,  Gisbert Sponer

发明人： Fritz Wiedemann ,  Max Thiel ,  Kurt Stach ,  Karl Dietmann ,  Gisbert Sponer

IPC分类号： C07D209/86 ,  A61K31/54 ,  C07D279/24

CPC分类号： C07D209/86

摘要： New N-substituted 1-amino-3-phenoxy-propan-2-ol compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or, taken together, represent a sulfur linkage, an ethylene radical or a valency bond;B is straight or branched chain alkylene or hydroxyalkylene of from 2 to 5 carbon atoms; andR.sub.3 is hydrogen or alkyl of up to 3 carbon atoms;And the physiologically compatible salts thereof; possess valuable cardiac and circulatory activity.

摘要翻译： 新的N-取代的1-氨基-3-苯氧基 - 丙-2-醇，其分子式为：其中R 1和R 2各自为氢或一起表示硫键，乙烯 激进或价格债券; B是2至5个碳原子的直链或支链亚烷基或羟基亚烷基; 并且R 3是氢或至多3个碳原子的烷基; 及其生理适应性肥皂; 有价值的心脏和循环活动。

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：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：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。

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。

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。