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1. 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。

2. 发明授权

US3937706A 1-(2'Ethynyl-phenoxy)-2-hydroxy-3-(cycloalkyl-amino)-propanes and salts thereof 失效
标题翻译： 1-（2'-羟基 - 苯氧基）-2-羟基-3-（环丙基氨基）丙酸酯及其盐
公开(公告)号：US3937706A
公开(公告)日：1976-02-10
申请号：US310638
申请日：1972-11-29
申请人： Herbert Koppe , Werner Kummer , Helmut Stahle , Karl Zeile , Albrecht Engelhardt , Werner Traunecker
发明人： Herbert Koppe , Werner Kummer , Helmut Stahle , Karl Zeile , Albrecht Engelhardt , Werner Traunecker
IPC分类号： A61K31/13 , A61K31/135 , A61K31/275 , C07C233/00 , C07C255/53 , E04H13/00 , C07C93/06 , C07D473/00
CPC分类号： A61K31/13 , A61K31/135 , A61K31/275 , C07C233/00 , C07C255/53
摘要： Compounds of the formula ##EQU1## wherein n is 4 or 5, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as .beta.-adrenergic receptor blocking agents.

3. 发明授权

US4010158A 1-(2'-Ethynyl-phenoxy)-2-hydroxy-3-butylamino-propanes and salts 失效
标题翻译： 1-（2 {40-乙炔基 - 苯氧基）-2-羟基-3-丁基氨基 - 丙烷和盐
公开(公告)号：US4010158A
公开(公告)日：1977-03-01
申请号：US324844
申请日：1973-01-18
申请人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Albrecht Engelhardt
发明人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Albrecht Engelhardt
IPC分类号： A61K31/135 , C07C93/06 , C07D473/00
CPC分类号： A61K31/135 , Y10S514/821
摘要： Compounds of the formula ##STR1## wherein R is secondary butyl or tertiary butyl, and their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as .beta.-adrenergic receptor blocking agents and hypotensives.
摘要翻译：其中R是仲丁基或叔丁基的式“IMAGE”的化合物及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作β-肾上腺素能受体阻断剂和低血糖剂。

4. 发明授权

US4031244A Pharmaceutical compositions containing a 1-(2,6-dimethyl-phenoxy)-2-amino-alkane and method of use 失效
标题翻译：含有1-（2,6-二甲基 - 苯氧基）-2-氨基 - 烷烃的药物组合物及其使用方法
公开(公告)号：US4031244A
公开(公告)日：1977-06-21
申请号：US653296
申请日：1976-01-29
申请人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
发明人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
IPC分类号： A61K31/135 , A61K31/55 , F41J11/02
CPC分类号： F41J11/02 , A61K31/135 , A61K31/55
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, and R.sub.1 is hydrogen or methyl, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as anticonvulsives and antiarrhythmics.
摘要翻译：其中R为氢或1〜3个碳原子的烷基，R1为氢或甲基，或其无毒的药理学上可接受的酸加成盐作为活性成分含有下式化合物的药物组合物：以及使用其作为抗惊厥药和抗心律失常药的方法。

5. 发明授权

US3954872A 1-(2',6'-Dimethyl-phenoxy)-2-amino-alkanes and salts thereof 失效
标题翻译： 1-（2 {40,6（40-二甲基 - 苯氧基）-2-氨基 - 烷烃及其盐
公开(公告)号：US3954872A
公开(公告)日：1976-05-04
申请号：US511063
申请日：1974-10-01
申请人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
发明人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
IPC分类号： A61K31/135 , F41J11/02 , C07C93/06
CPC分类号： F41J11/02 , A61K31/135 , Y10S514/821
摘要： Compounds of the formula ##EQU1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, andR.sub.1 is hydrogen or methyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anticonvulsives and antiarrhythmics in warmblooded animals.

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US4039685A 1-Phenoxy-2-hydroxy-3-tert.-butylamino propane antiarrhythmic compounds 失效
标题翻译： 1-苯氧基-2-羟基-3-叔丁基 - 丁酰胺丙醛抗坏血酸化合物
公开(公告)号：US4039685A
公开(公告)日：1977-08-02
申请号：US571790
申请日：1975-04-25
申请人： Herbert Koppe , Albrecht Engelhardt , Karl Zeile
发明人： Herbert Koppe , Albrecht Engelhardt , Karl Zeile
IPC分类号： A61K31/00 , A61K31/135 , A61K31/14 , A61K31/275 , A61K31/505 , C07D309/12 , C07C93/06
CPC分类号： C07D309/12 , A61K31/00 , A61K31/135 , A61K31/14 , A61K31/275 , A61K31/505
摘要： A compound selected from the group consisting of racemates of 1-phenoxy-2-hydroxy-3-tert.-butylamino propanes of the formula ##STR1## wherein R is selected from the group consisting of alkynyloxy of 2 to 4 carbon atoms, and R.sub.1 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 4 carbon atoms, their optically active isomers and their non-toxic, pharmaceutically acceptable acid addition salts of said racemates and said optically active isomers which compounds possess bradycardia activity and isoproterenol antagonistic activity and also antiarrhythmic activity.

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