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1. 发明授权

US4080503A 2-Amino-4-phenyl-2-imidazolines and salts thereof 失效
标题翻译： 2-氨基-4-苯基-2-咪唑啉及其盐
公开(公告)号：US4080503A
公开(公告)日：1978-03-21
申请号：US379750
申请日：1973-07-16
申请人： Werner Kummer , Herbert Koppe , Helmut Stahle , Walter Haarmann
发明人： Werner Kummer , Herbert Koppe , Helmut Stahle , Walter Haarmann
IPC分类号： C07D233/46 , C07D233/48 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04
CPC分类号： C07D233/46 , C07D233/48 , Y10S514/821 , Y10S514/822
摘要： 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,R.sub.3 is hydrogen, furfuryl, hydroxyethyl, .beta.-hydroxy-phenethyl, monochlorophenyl-ethyl, dichlorophenyl-ethyl, N-ethyl-piperidyl or --A--NR.sub.6 R.sub.7,whereA is alkylene of 1 to 5 carbon atoms, andR.sub.6 and R.sub.7 are alkyl of 1 to 2 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, morpholino, piperazino or N'-dimethylphenyl-piperazino,R.sub.4 is hydrogen or, together with R.sub.3 and the nitrogen to which they are attached, forms a heterocycle selected from the group consisting of piperidino, morpholino, dimethyl-morpholino or N'-methyl-piperazino,R.sub.5 is hydrogen, alkyl of 1 to 3 carbon atoms, hydroxy-ethyl, 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 that R.sub.3 and R.sub.5 are other than both hydrogen at the same time, or a non-toxic, pharmacologically acceptable acid addition salt thereof; the compounds as well as the salt are useful as hypotensives, platelet aggregation inhibitors and antiarrhythmics.
摘要翻译：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，R3是氢，糠基，羟乙基，β-羟基 - 苯乙基，一氯苯基 - 乙基，二氯苯基 - 乙基，N-乙基 - 哌啶基或-A-NR 6 R 7，其中A为1至5个碳原子的亚烷基，R 6和R 7为1至2个碳原子的烷基，形成选自吡咯烷子基，吗啉代，哌嗪子基或N'-二甲基苯基 - 哌嗪子基的杂环，R 4为氢，或者与R 3和它们所连接的氮一起，形成选自哌啶子基，吗啉代，二甲基吗啉代或N'-甲基 - 哌嗪子基的杂环，R 5为氢，1至3个碳原子的烷基，羟基 - 乙基，二乙基氨基 - 乙基或糠基，提供，其中R 1和R 2不是氢或两个烷基同时，R3和R5不仅同时为氢，也可以是其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。

2. 发明授权

US4105765A 2-(N-(1,3-diamino-isopropyl)-amino)-4-phenyl-2-imidazolines and salts thereof 失效
标题翻译： 2-（N-（1,3-二氨基 - 异丙基） - 氨基）-4-苯基-2-咪唑啉及其盐
公开(公告)号：US4105765A
公开(公告)日：1978-08-08
申请号：US837692
申请日：1977-09-29
申请人： Werner Kummer , Helmut Stahle , Herbert Koppe , Walter Haarmann , Richard Reichl
发明人： Werner Kummer , Helmut Stahle , Herbert Koppe , Walter Haarmann , Richard Reichl
IPC分类号： C07D233/48 , C07D413/14 , A61K31/415 , A61K31/495 , A61K31/535
CPC分类号： C07D233/48
摘要： A compound of the formula ##STR1## wherein R.sub.1 is chlorine, bromine, fluorine or methyl;R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, chlorine or methyl;R.sub.4 is hydrogen, methyl or ethyl; andR.sub.5 and R.sub.6, together with each other and the nitrogen atom to which they are attached, are morpholino, piperazino or N-methylpiperazino;And non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as the salts are useful as antithrombotics.
摘要翻译：其中R 1是氯，溴，氟或甲基的式（Ⅰ）化合物; R2和R3可以相同或不同，分别为氢，氯或甲基; R4是氢，甲基或乙基; 并且R 5和R 6彼此连接并与它们相连的氮原子是吗啉代，哌嗪基或N-甲基哌嗪基; 和非毒性药用植物酸加药盐; 化合物作为抗菌药物有用的方法。

3. 发明授权

US4073905A 2-Amino-4-phenyl-2-imidazolines and salts thereof 失效
标题翻译： 2-氨基-4-苯基-2-咪唑啉及其盐
公开(公告)号：US4073905A
公开(公告)日：1978-02-14
申请号：US775736
申请日：1977-03-09
申请人： Werner Kummer , Herbert Koppe , Helmut Stahle , Walter Haarmann
发明人： Werner Kummer , Herbert Koppe , Helmut Stahle , Walter Haarmann
IPC分类号： C07D233/46 , C07D233/48
CPC分类号： C07D233/46 , C07D233/48 , Y10S514/821
摘要： 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.
摘要翻译：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。

4. 发明授权

US4058616A 2-[N-(1,3-diamino-isopropyl)-amino]-4-phenyl-2-imidazolines and salts thereof 失效
标题翻译： 2- {8 N-（1,3-二氨基 - 异丙基） - 氨基} -9-苯基-2-咪唑啉及其盐
公开(公告)号：US4058616A
公开(公告)日：1977-11-15
申请号：US692325
申请日：1976-06-03
申请人： Werner Kummer , Helmut Stahle , Herbert Koppe , Walter Haarmann , Richard Reichl
发明人： Werner Kummer , Helmut Stahle , Herbert Koppe , Walter Haarmann , Richard Reichl
IPC分类号： A61K31/415 , A61P7/02 , C07D233/48 , A61K31/445 , C07D401/14
CPC分类号： C07D233/48 , Y10S514/822
摘要： A compound of the formula ##STR1## wherein R.sub.1 is chlorine, bromine, fluorine or methyl;R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, chlorine or methyl;R.sub.4 is hydrogen, methyl or ethyl; andR.sub.5 and R.sub.6, which may be identical to or different from each other, are each methyl, ethyl or alkoxy-alkyl of 2 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocycle which may contain an additional heteroatom, such as pyrrolidino, piperidino, morpholino, piperazino or hexamethyleneimino;And non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as the salts are useful as antithrombotics.
摘要翻译：其中R 1是氯，溴，氟或甲基的式（Ⅰ）化合物; R2和R3可以相同或不同，分别为氢，氯或甲基; R4是氢，甲基或乙基; 和可以相同或不同的R 5和R 6各自是2至4个碳原子的甲基，乙基或烷氧基 - 烷基，或彼此连接并与它们相连的氮原子形成5 - 可含有另外的杂原子的6-或7-元杂环，例如吡咯烷子基，哌啶子基，吗啉代，哌嗪基或六亚甲基亚氨基; 和非毒性药用植物酸加药盐; 化合物作为抗菌药物有用的方法。

5. 发明授权

US4442120A 1-Aryloxy-3-alkylamino-propan-2-ols 失效
标题翻译： 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。

6. 发明授权

US4344964A 1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof 失效
标题翻译： 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。

7. 发明授权

US4210659A Substituted 7-phenyl-2,3-dihydro-imidazo[1,2-.alpha.]imidazoles and salts thereof 失效
标题翻译：取代的7-苯基-2,3-二氢 - 咪唑并[1,2-a]咪唑及其盐
公开(公告)号：US4210659A
公开(公告)日：1980-07-01
申请号：US52566
申请日：1979-06-27
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
IPC分类号： A61K31/415 , A61P9/06 , C07D487/04
CPC分类号： C07D487/04 , Y10S514/96
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, methyl, methoxy or trifluoromethyl, provided that one of them is other than hydrogen; andR.sub.4 and R.sub.5, which may be identical to or different from each other, are each hydrogen or methyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中R 1，R 2和R 3可以相同或不同，可以是氢，氟，氯，溴，甲基，甲氧基或三氟甲基，其中一个不是氢 ; 和可以相同或不同的R 4和R 5各自为氢或甲基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

8. 发明授权

US4036972A 2-(N-thienylmethyl-phenylamino)-imidazolines-(2) and salts thereof 失效
标题翻译： 2-（N-噻吩基甲基 - 苯基氨基） - 咪唑啉 - （2）及其盐
公开(公告)号：US4036972A
公开(公告)日：1977-07-19
申请号：US607258
申请日：1975-08-25
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus
IPC分类号： A61K31/415 , G03G15/08 , C07D409/12
CPC分类号： A61K31/415 , G03G15/08
摘要： Compounds of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are each hydrogen, fluorine, chlorine, bromine, methoxy or trifluoromethyl, but other than all hydrogen at the same time, andR.sub.3 is hydrogen, methyl or ethyl,And non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics and hypotensives.
摘要翻译：其中R，R 1和R 2各自为氢，氟，氯，溴，甲氧基或三氟甲基，但不是全部为氢，而R3为氢，甲基或乙基，和非毒性的化合物，其药用添加剂; 化合物作为它们的有效的有效的化学和低分子化合物。

9. 发明授权

US4021576A Pharmaceutical compositions containing a 1-(2'-ethynyl-phenoxy)-2-hydroxy-3-(cycloalkyl-amino)-propane and method of use 失效
标题翻译：含有1-（2（40-乙炔基 - 苯氧基）-2-羟基-3-（环烷基 - 氨基） - 丙烷的药物组合物及其使用方法
公开(公告)号：US4021576A
公开(公告)日：1977-05-03
申请号：US639342
申请日：1975-12-10
申请人： Herbert Koppe , Werner Kummer , Helmut Stahle , Karl Zeile , Albrecht Engelhardt , Werner Taunecker
发明人： Herbert Koppe , Werner Kummer , Helmut Stahle , Karl Zeile , Albrecht Engelhardt , Werner Taunecker
IPC分类号： A61K31/13 , A61K31/135 , A61K31/275 , A61K31/505 , C07C233/00 , C07C255/53 , E04H13/00
CPC分类号： A61K31/13 , A61K31/135 , A61K31/275 , A61K31/505 , C07C233/00 , C07C255/53
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein n is 4 or 5, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blockers.
摘要翻译：作为活性成分含有下式的化合物的药物组合物，其中n为4或5，或其无毒的药学上可接受的酸加成盐; 以及使用β-肾上腺素能受体阻断剂的方法。

10. 发明授权

US4609672A 1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof 失效
标题翻译： 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：US4609672A
公开(公告)日：1986-09-02
申请号：US623960
申请日：1984-06-25
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 , A61K31/505 , A61P9/00 , C07C67/00 , C07C253/00 , C07C255/59 , C07C255/60
CPC分类号： C07C255/00 , A61K31/505
摘要： The invention relates to a compound of the formula ##STR1## wherein R.sub.1 is a linear or branched alkyl of 4 to 20 carbon atoms;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 the treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.
摘要翻译：本发明涉及式IMA的化合物，其中R 1是4至20个碳原子的直链或支链烷基; 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。

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