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。

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。

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。

公开(公告)号：US3969512A

公开(公告)日：1976-07-13

申请号：US548366

申请日：1975-02-10

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

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

IPC分类号： C07C275/24 ,  C07C275/34 ,  A61K31/135 ,  C07C93/06

CPC分类号： C07C275/34 ,  C07C275/24

摘要： Compounds of the formula ##EQU1## wherein R.sub.1 is allyl, allyloxy or chlorine, R.sub.2 is hydrogen or methyl,R.sub.3 is hydrogen, alkyl of 1 to 5 carbon atoms or benzyl, andn is an integer from 2 to 6, inclusive,Provided, however, that when R.sub.1 is allyl or allyloxy, R.sub.2 is hydrogen; and their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as .beta.-adrenergic blocking agents and hypotensives.

摘要翻译： 式-OCH2-CHOH-CH2-N-（CH2）nN-CH2 || R3R3 -CHOH-CH2-O-的化合物，其中R1是烯丙基，烯丙氧基或氯，R2是氢或甲基，R3是氢， 1至5个碳原子或苄基，N为2至6的整数，包括但不包括，当R1为烯丙基或烯丙氧基时，R2为氢; 及其无毒，药理学上可接受的酸加成盐; 化合物及其盐可用作β-肾上腺素能阻滞剂和低血糖剂。

公开(公告)号：US3975539A

公开(公告)日：1976-08-17

申请号：US568798

申请日：1975-04-16

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

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

IPC分类号： C07C275/24 ,  A61K31/275

CPC分类号： C07C275/24

摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##EQU1## wherein R.sub.1 is --(CH.sub.2).sub.x --CN, where x is 0,1,2 or 3,R.sub.2 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms or alkenyloxy of 2 to 5 carbon atoms;R.sub.3 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms or alkoxy of 1 to 5 carbon atoms;R.sub.2 and R.sub.3, together with each other and the carbon atoms to which they are attached, form a saturated or unsaturated carbocyclic ring of up to 6 carbon atoms;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms or aralkyl; andn is an integer from 1 to 10, inclusive; or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blockers and hypotensives.

摘要翻译： 含有式-OCH 2 -CHOH-CH 2 -N（CH 2）n - | R N-CH 2 -CHOH-CH 2 -O-R 4的化合物作为活性成分的药物组合物，其中R1为 - （CH2）x-CN 其中x为0,1,2或3，R2为氢，卤素，1至5个碳原子的烷基，1至5个碳原子的烷氧基，2至5个碳原子的链烯基或2至5个碳原子的链烯氧基; R3是氢，卤素，1至5个碳原子的烷基或1至5个碳原子的烷氧基; R2和R3彼此连接并与它们相连的碳原子形成最多6个碳原子的饱和或不饱和碳环; R4是氢，1至5个碳原子的烷基或芳烷基; N是1到10的整数，包含; 或非毒性，药理学上可接受的酸添加盐; 以及使用它们作为β-受体阻断剂阻断剂和HYPTENSIVES的方法。

公开(公告)号：US4442121A

公开(公告)日：1984-04-10

申请号：US398578

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： A61K31/165 ,  A61K20060101 ,  A61K31/045 ,  A61K31/135 ,  A61K31/16 ,  A61K31/275 ,  A61K31/335 ,  A61K31/36 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07C20060101 ,  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 alkenyloxy, lower alkinyl, nitro, trifluoromethyl, hydroxyl, 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, acyl, acyloxy, nitro, trifluoromethyl or the ring-forming groups (--CH.dbd.CH--).sub.2 or --O--CH.sub.2 --O-- attached to vicinal carbon atoms of the aryl 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;R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.4 is alkyl of 1 to 3 carbon atoms or, together with R.sub.3, a ring-forming group --(CH.sub.2).sub.p --, where p is an integer from 4 to 6;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; 低级烷氧基，低级烯基，低级烯氧基，低级炔基，硝基，三氟甲基，羟基，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，酰基，酰氧基，硝基，三氟甲基或成环基团（-CH = CH-）2或-O-CH2-O-连接到芳环的连位碳原子上; 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; R3是氢或1至3个碳原子的烷基; 并且R 4是1至3个碳原子的烷基，或者与R 3一起形成环 - 基团 - （CH 2）p - ，其中p是4至6的整数; 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。

公开(公告)号：US4438143A

公开(公告)日：1984-03-20

申请号：US420796

申请日：1982-09-21

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： C07C253/30 ,  A61K20060101 ,  A61K31/045 ,  A61K31/13 ,  A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61K31/275 ,  A61P9/08 ,  A61P9/12 ,  C07C20060101 ,  C07C33/00 ,  C07C67/00 ,  C07C231/00 ,  C07C253/00 ,  C07C255/59 ,  C07C255/60 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D239/70 ,  C07D251/12 ,  C07D251/46 ,  C07D491/048 ,  C07D491/052 ,  C07C121/80

CPC分类号： C07C255/00 ,  Y10S514/821

摘要： This invention relates to compounds of the formula ##STR1## wherein R.sub.1 represents a linear or branched alkyl of from 1 to 20 carbon atoms;R.sub.2 represents a hydrogen or halogen atom, a linear or branched alkyl or alkoxy of from 1 to 4 carbon atoms, or a divalent group --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n --, in which n is an integer of from 3 to 5, with the free valences bonded in the o-position relative to one another; andR.sub.3 represents a linear or branched alkyl of from 3 to 10 carbon atoms, with the provisos that R.sub.3 is not tert.butyl when R.sub.1 is ethyl or propyl and R.sub.2 is a hydrogen atom and that R.sub.3 is not isopropyl when R.sub.1 is propyl and R.sub.2 is a hydrogen atom,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（I）的化合物，其中R 1表示1至20个碳原子的直链或支链烷基; R 2表示氢或卤素原子，1至4个碳原子的直链或支链烷基或烷氧基，或二价基团-CH = CH-CH = CH-或 - （CH 2）n - ，其中n是整数 3至5，其中自由价键合在相对于彼此的o位置上; 并且R 3表示3至10个碳原子的直链或支链烷基，条件是当R 1是乙基或丙基时，R 3不是叔丁基，R 2是氢原子，当R 1是丙基且R 3不是异丙基时，R 2是R 2 是氢原子或其无毒的药学上可接受的酸加成盐。 式I的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。

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.

公开(公告)号：US4084002A

公开(公告)日：1978-04-11

申请号：US742639

申请日：1976-11-17

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 ,  A61K31/135

CPC分类号： C07C275/34

摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a 1-aryloxy-2-hydroxy-3-alkynylamino-propane selected from the group consisting of racemic or optically active compounds of the formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of hydrogen; halogen; nitro; alkyl having from 1 to 5 carbon atoms; alkoxy having from 1 to 4 carbon atoms; alkenyl having from 2 to 5 carbon atoms; alkynyl having from 2 to 5 carbon atoms; alkylamino having from 1 to 5 carbon atoms; dialkylamino having from 1 to 5 carbon atoms in each alkyl; alkoxyalkyl having from 2 to 6 carbon atoms; alkylaminoalkyl having from 2 to 6 carbon atoms; dialkylaminoalkyl having from 3 to 12 carbon atoms; --(CH.sub.2).sub.x -NH.sub.2 or --(CH.sub.2).sub.x -OH, where x is an integer from 0 to 3; alkynyloxy having from 3 to 6 carbon atoms; alkenyloxy having from 3 to 6 carbon atoms; --CO-R.sub.9, where R.sub.9 is a member selected from the group consisting of alkyl having 1 to 6 carbon atoms, phenylalkyl having 7 to 10 carbon atoms and phenyl; cycloalkyl having from 3 to 7 carbon atoms; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro; phenoxy; and phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro;R.sub.2 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms, alkanoyl having from 2 to 4 carbon atoms, alkenyl having from 2 to 4 carbon atoms, amino and nitro;R.sub.3 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms and, 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 a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms; andR.sub.5 is a member selected from the group consisting of alkyl having from 1 to 3 carbon atoms, and, 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; and a method of using the same as adrenolytics and hypotensives.

公开(公告)号：US4016286A

公开(公告)日：1977-04-05

申请号：US615913

申请日：1975-09-23

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 ,  A61K31/135

CPC分类号： C07C275/34

摘要： Pharmaceutical compositions containing as an active ingredient a racemic or optically active compound of the formula ##STR1## wherein R.sub.1 is --(CH.sub.2).sub.X --CN, where X is 0, 1, 2 or 3,R.sub.2 is hydrogen, halogen or --NH--CO--NHR, where R is lower alkyl,R.sub.4 is 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 4, 5 or 6,Or a physiologically compatible acid addition salt thereof; and a method of using the same as adrenolytics and hypotensives.

摘要翻译： 含有下式的外消旋或光学活性化合物作为活性成分的药物组合物，其中R1是 - （CH2）X-CN，其中X是0,1,2或3，R2是氢，卤素或-NH- CO-NHR，其中R是低级烷基，R 4是1至3个碳原子的烷基，R 5是1至3个碳原子的烷基，或者与R 4， - （CH 2）p - ，其中p是4,5或6 ，或其生理水溶性酸添加盐; 和使用它们作为ADRENOLYTICS和HYPTENSIVES的方法。