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    1-Aryloxy-3-alkylamino-propan-2-ols
    4.
    发明授权
    1-Aryloxy-3-alkylamino-propan-2-ols 失效
    1-芳氧基-3-烷基氨基 - 丙-2-醇

    公开(公告)号：US4442120A

    公开(公告)日：1984-04-10

    申请号：US398577

    申请日：1982-07-15

    申请人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic ,  Werner Traunecker

    发明人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic ,  Werner Traunecker

    IPC分类号： A61K31/275 ,  A61K20060101 ,  A61K31/135 ,  A61K31/16 ,  A61K31/335 ,  A61K31/357 ,  A61K31/36 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07C20060101 ,  C07C33/00 ,  C07C67/00 ,  C07C253/00 ,  C07C253/30 ,  C07C255/59 ,  C07C255/60 ,  C07D317/60 ,  C07D317/68 ,  C07C121/80

    CPC分类号： C07C255/00 ,  Y10S514/821

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 10 carbon atoms; phenyl; mono- or poly-substituted phenyl, where the substituents are halogen, lower alkyl, lower alkoxy, lower alkenyl, lower alkinyl, lower alkinyloxy, lower cycloalkyl, acyl, acyloxy, lower alkoxycarbonyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl or the ring-forming groups (--CH.dbd.CH--).sub.2 or --O--CH.sub.2 --O-- attached to vicinal carbon atoms of the phenyl ring; aryloxy-lower alkyl; (mono- or poly-substituted aryl)-oxy-lower alkyl, where the substituents are halogen, lower alkyl, lower alkoxy, lower alkenyl, lower alkinyl, lower alkinyloxy, lower cycloalkyl, acyl, acyloxy, lower alkoxycarbonyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl or the ring-forming groups (--CH.dbd.CH--).sub.2 or --O--CH.sub.2 --O-- attached to vicinal carbon atoms of the phenyl ring;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or the ring-forming group (--CH.dbd.CH).sub.2 or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, attached to vicinal carbon atoms of the phenyl ring; andR.sub.3 is straight or branched alkyl of 1 to 10 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of tachycardia, hypertension and coronary diseases.

    摘要翻译： 其中R 1是3至10个碳原子的环烷基的化合物＆lt; IMAGE＆gt; 苯基; 单取代或多取代的苯基，其中取代基为卤素，低级烷基，低级烷氧基，低级烯基，低级炔基，低级烷氧基，低级环烷基，酰基，酰氧基，低级烷氧基羰基，羟基 - 低级烷基，低级烷氧基 - 低级烷基或 连接到苯环的邻位碳原子上的成环基团（-CH = CH-）2或-O-CH2-O-; 芳氧基 - 低级烷基; （单或多取代芳基） - 氧基 - 低级烷基，其中取代基是卤素，低级烷基，低级烷氧基，低级烯基，低级炔基，低级烷氧基，低级环烷基，酰基，酰氧基，低级烷氧基羰基，羟基 - 低级烷基 ，低级烷氧基 - 低级烷基或连接到苯环的邻位碳原子上的成环基团（-CH = CH-）2或-O-CH2-O-; R 2是氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或成环基团（-CH = CH）2或 - （CH 2）n - ，其中n是从3到 5，连接苯环的连位碳原子; 并且R 3是1至10个碳原子的直链或支链烷基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用于治疗心动过速，高血压和冠状动脉疾病。

    1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof
    5.
    发明授权
    1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof 失效
    1-（烷酰基氨基 - 芳氧基）-2-羟基-3-（炔基 - 氨基） - 丙烷及其盐

    公开(公告)号：US4344964A

    公开(公告)日：1982-08-17

    申请号：US241519

    申请日：1981-03-09

    申请人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic ,  Werner Traunecker

    发明人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic ,  Werner Traunecker

    IPC分类号： C07C255/60 ,  A61K31/275 ,  A61K31/505 ,  A61P9/00 ,  C07C67/00 ,  C07C253/00 ,  C07C255/58 ,  C07C255/59 ,  C07C121/78

    CPC分类号： C07C255/00 ,  A61K31/505

    摘要： This invention relates to a compound of the formula ##STR1## wherein R.sub.1 is ethyl or isopropyl;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or a bivalent radical --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, inclusive, and the free bonds of said bivalent radical are attached to adjacent carbon atoms of the phenyl ring; andR.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is alkyl of 1 to 3 carbon atoms; orR.sub.3 and R.sub.4, together with each other, are --(CH.sub.2).sub.p --, where p is an integer from 4 to 6, inclusive,or a non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds of formula I are useful for treatment and prophylaxis of diseases of the coronaries, for treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1是乙基或异丙基; R 2是氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或2价基团-CH = CH-CH = CH-或 - （CH 2）n - ，其中n是从3到 5，其中所述二价基团的游离键连接到苯环的相邻碳原子上; 且R 3为氢或1至3个碳原子的烷基; R4是1〜3个碳原子的烷基; 或R 3和R 4彼此一起为 - （CH 2）p - ，其中p为4至6的整数，或其无毒的药学上可接受的酸加成盐。 式I化合物可用于治疗和预防冠状动脉疾病，治疗高血压和治疗心律失常，特别是心动过速。

    Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid amides
    6.
    发明授权
    Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid amides 失效
    使用新的噻吩并三唑-1,4-二氮杂-2-羧酸酰胺的方法

    公开(公告)号：US5155103A

    公开(公告)日：1992-10-13

    申请号：US774683

    申请日：1991-10-11

    申请人： Karl-Heinz Weber ,  Albrecht Harreus ,  Jorge Casals-Stenzel ,  Gojko Muacevic ,  Wolfgang Troger ,  Gerhard Walther

    发明人： Karl-Heinz Weber ,  Albrecht Harreus ,  Jorge Casals-Stenzel ,  Gojko Muacevic ,  Wolfgang Troger ,  Gerhard Walther

    IPC分类号： A61K31/55 ,  A61K31/5517 ,  A61P7/02 ,  A61P9/02 ,  A61P11/08 ,  A61P29/00 ,  A61P37/00 ,  A61P37/08 ,  C07C235/40 ,  C07D243/00 ,  C07D249/08 ,  C07D333/00 ,  C07D333/36 ,  C07D495/00 ,  C07D495/04 ,  C07D495/14

    CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D495/14

    摘要： The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.

    摘要翻译： 本发明涉及式I的新的噻吩并三唑并-1,4-二氮杂-2-羧酸酰胺其中R 1表示氢，可以任意被C 1 -C 4直链或支链烷基取代的C 1 -C 4直链或支链烷基 卤素，优选Cl或Br，或羟基，环丙基，C 1 -C 3烷氧基，优选甲氧基或卤素，优选氯或溴; R2和R3各自独立地代表氢，C1-C4直链或支链烷基，C1-C4羟基烷基或两个R2和R3与氮原子一起表示5-，6-或7-元环，其中 任选地含有氮，氧或硫原子作为另外的杂原子，第二氮原子任选被C 1 -C 4烷基，优选甲基取代; R4表示α-吡啶基或苯基，其中苯环优选在2-位上被甲基，卤素，优选氯或溴，硝基或三氟甲基取代; n表示数字0,1,2,3,4,5,6,7或8中的一个; 及其新型中间体。 式I化合物可用于治疗涉及血小板活化因子的病理状况和疾病。

    1-Phenoxy-2-hydroxy-3-alkynylamino-propanes and salts thereof
    10.
    发明授权
    1-Phenoxy-2-hydroxy-3-alkynylamino-propanes and salts thereof 失效

    公开(公告)号：US4016202A

    公开(公告)日：1977-04-05

    申请号：US609998

    申请日：1975-09-03

    申请人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic

    发明人： Herbert Koppe ,  Werner Kummer ,  Helmut Stahle ,  Gojko Muacevic

    IPC分类号： C07C275/34 ,  C07C93/06

    CPC分类号： C07C275/34

    摘要： Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; halogen; nitro; alkyl of 1 to 5 carbon atoms; alkoxy of 1 to 4 carbon atoms; alkenyl of 2 to 5 carbon atoms; alkynyl of 2 to 5 carbon atoms; alkylamino of 1 to 5 carbon atoms; dialkylamino of 1 to 5 carbon atoms in each alkyl; alkoxyalkyl of 2 to 6 carbon atoms; alkylamino-alkyl of 2 to 6 carbon atoms; dialkylaminoalkyl of 3 to 12 carbon atoms; --(CH.sub.2).sub.x --NH.sub.2, --(CH.sub.2).sub.x -- OH, all where x is an integer from 0 to 3; --COOH; --COOR.sub.6, where R.sub.6 is alkyl of 1 to 4 carbon atoms; alkynyloxy of 3 to 6 carbon atoms; alkenyloxy of 3 to 6 carbon atoms; --CO--R.sub.9, --OCO--R.sub.9, --NH--CO--R.sub.9, all where R.sub.9 is alkyl of 1 to 6 carbon atoms, phenylalkyl of 7 to 10 carbon atoms or phenyl; cycloalkyl of 3 to 7 carbon atoms; --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; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, cyano and carboxyl; phenoxy; or phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, cyano and carboxyl;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=CH--CH=CH-- or --(CH.sub.2)n--, where n is an integer from 3 to 5;R.sub.4 is hyddrogen 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.