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    • 43. 发明授权
    • 1-Phenoxy-2-hydroxy-3-alkynylamino-propanes and salts thereof
    • 1-苯氧基-2-羟基-3-炔基氨基丙烷及其盐
    • US4220659A
    • 1980-09-02
    • US924791
    • 1978-07-14
    • Herbert KoppeWerner KummerHelmut StahleGojko Muacevic
    • Herbert KoppeWerner KummerHelmut StahleGojko Muacevic
    • C07C101/42A01N9/20
    • Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is --COOR.sub.6, where R.sub.6 is hydrogen or alkyl of 1 to 4 carbon atoms; --OCO--R.sub.9, where R.sub.9 is alkyl of 1 to 6 carbon atoms, phenyl (alkyl of 1 to 4 carbon atoms) or phenyl; --Q--CO--NR.sub.7 R.sub.8, where Q is a single bond, oxygen, --NH--, --CH2-- or --CH.sub.2 --NH--, and R.sub.7 and R.sub.8, taken together with the nitrogen, are pyrrolidino, piperidino or morpholino; cyano-phenyl; carboxyl-phenyl; cyano-phenoxy; or carboxyl-phenoxy;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkanoyl of 2 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, amino, nitro or, together with R.sub.1, 3,4-methylenedioxy;R.sub.3 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or, together with R.sub.2 in the ortho-position, --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n -- where n is an integer from 3 to 5;R.sub.4 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.5 is alkyl of 1 to 3 carbon atoms or, together with R.sub.4, --(CH.sub.2).sub.p --, where p is an integer from 4 to 6; and physiologically compatible acid addition salts thereof. The compounds as well as their salts are useful as adrenolytics and hypotensives.
    • 其中R 1为-COOR 6,其中R 6为氢或1至4个碳原子的烷基的外消旋和旋光活性化合物。 -OCO-R 9,其中R 9是具有1至6个碳原子的烷基,苯基(1至4个碳原子的烷基)或苯基; -Q-CO-NR7R8,其中Q是单键,氧,-NH-,-CH 2 - 或-CH 2 -NH-,并且R 7和R 8与氮一起是吡咯烷子基,哌啶子基或吗啉代; 氰基 - 苯基; 羧基 - 苯基; 氰基 - 苯氧基; 或羧基 - 苯氧基; R 2是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,2至4个碳原子的烷酰基,2至4个碳原子的链烯基,氨基,硝基或与R 1, 亚甲二氧基 R 3是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,或与邻位的R 2一起-CH = CH-CH = CH-或 - (CH 2)n,其中n 是3到5的整数; R4是氢或1〜3个碳原子的烷基; 和R 5为1至3个碳原子的烷基,或与R 4一起为 - (CH 2)p - ,其中p为4至6的整数; 和其生理上相容的酸加成盐。 化合物及其盐可用作肾上腺素和低血糖。
    • 47. 发明授权
    • 1-Phenoxy-2-hydroxy-3-alkynylamino-propanes and salts thereof and
treatment of coronary diseases therewith
    • 1-苯氧基-2-羟基-3-炔基氨基 - 丙烷及其盐与冠心病的治疗
    • US4119728A
    • 1978-10-10
    • US742782
    • 1976-11-18
    • Herbert KoppeWerner KummerHelmut StahleGojko Muacevic
    • Herbert KoppeWerner KummerHelmut StahleGojko Muacevic
    • C07C275/34A61K31/165C07C103/10
    • C07C275/34
    • Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is --COOR.sub.6, where R.sub.6 is hydrogen or alkyl of 1 to 4 carbon atoms; --OCO--R.sub.9 or --NH--CO--R.sub.9, where R.sub.9 is alkyl of 1 to 6 carbon atoms, phenyl (alkyl of 1 to 4 carbon atoms) or phenyl; --Q--CO--NR.sub.7 R.sub.8, where Q is a single bond, oxygen, --NH--, --CH.sub.2 -- or --CH.sub.2 --NH--, and R.sub.7 and R.sub.8 are hydrogen, lower alkyl or, taken together with the nitrogen, pyrrolidino, piperidino or morpholino; cyano-phenyl; carboxylphenyl; cyano-phenoxy; or carboxyl-phenoxy;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkanoyl of 2 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, amino, nitro or, together with R.sub.1, 3,4-methylenedioxy;R.sub.3 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or, together with R.sub.2 in the ortho-position, --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2)n-- where n is an integer from 3 to 5;R.sub.4 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.5 is alkyl of 1 to 3 carbon atoms or, together with R.sub.4, --(CH.sub.2).sub.p --, where p is an integer from 4 to 6;And physiologically compatible acid addition salts thereof. The compounds as well as their salts are useful as adrenolytics and hypotensives.
    • 其中R 1为-COOR 6,其中R 6为氢或1至4个碳原子的烷基的外消旋和旋光活性化合物。 -OCO-R 9或-NH-CO-R 9,其中R 9是具有1至6个碳原子的烷基,苯基(1至4个碳原子的烷基)或苯基; -Q-CO-NR7R8,其中Q是单键,氧,-NH-,-CH2-或-CH2-NH-,并且R7和R8是氢,低级烷基或与氮一起,吡咯烷子基,哌啶子基 或吗啉代; 氰基 - 苯基; 羧基苯基; 氰基 - 苯氧基; 或羧基 - 苯氧基; R 2是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,2至4个碳原子的烷酰基,2至4个碳原子的链烯基,氨基,硝基或与R 1, 亚甲二氧基 R 3是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,或与邻位的R 2一起-CH = CH-CH = CH-或 - (CH 2)n,其中n 是3到5的整数; R4是氢或1〜3个碳原子的烷基; 和R 5为1至3个碳原子的烷基,或与R 4一起为 - (CH 2)p - ,其中p为4至6的整数; 和生理上相容的酸添加剂。 化合物及其盐可用作肾上腺素和低血糖。
    • 49. 发明授权
    • 2-Amino-4-phenyl-2-imidazolines and salts thereof
    • 2-氨基-4-苯基-2-咪唑啉及其盐
    • US4073905A
    • 1978-02-14
    • US775736
    • 1977-03-09
    • Werner KummerHerbert KoppeHelmut StahleWalter Haarmann
    • Werner KummerHerbert KoppeHelmut StahleWalter Haarmann
    • C07D233/46C07D233/48
    • C07D233/46C07D233/48Y10S514/821
    • Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, chlorine, bromine or alkyl of 1 to 3 carbon atoms,A is alkylene of 1 to 5 carbon atoms, andR.sub.6 and R.sub.7, together with each other and the nitrogen atom to which they are attached, form a heterocycle selected from the group consisting of morpholino, piperazino or N'-dimethylphenyl-piperazino, andR.sub.5 is hydrogen, alkyl of 1 to 3 carbon atoms, hydroxyethyl, diethylamino-ethyl or furfuryl,Provided, however, that R.sub.1 and R.sub.2 are other than both hydrogen or both alkyl at the same time, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as hypotensives, platelet aggregation inhibitors and antiarrhythmics.
    • 其中R 1和R 2可以相同或不同,可以是氢,氯,溴或1-3个碳原子的烷基,A是1至5个碳原子的亚烷基,和 R6和R7以及它们所连接的氮原子一起形成选自吗啉代,哌嗪子基或N'-二甲基苯基 - 哌嗪子基的杂环,R 5为氢,1至3个碳原子的烷基 ,羟乙基,二乙基氨基 - 乙基或糠基,提供,但是R 1和R 2不同于氢或两个烷基,同时也是无毒的,药学上可接受的酸加成盐; 化合物以及盐可用作低血压,血小板聚集抑制剂和抗心律失常药。