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1. 发明授权

US4594344A 1-aryloxypropanolamines 失效
标题翻译： 1-芳氧基丙醇胺
公开(公告)号：US4594344A
公开(公告)日：1986-06-10
申请号：US755044
申请日：1985-07-15
申请人： Herbert Koppe , Wolfgang Abele, deceased , Franz Esser , Wolfram Gaida , Wolfgang Hoefke
发明人： Herbert Koppe , Wolfgang Abele, deceased , Franz Esser , Wolfram Gaida , Wolfgang Hoefke
IPC分类号： A61K31/54 , A61P9/12 , C07D285/30 , C07D417/12
CPC分类号： C07D285/30
摘要： Disclosed are novel compounds having the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, a lower alkyl, lower alkoxy, lower alkoxy lower alkyl, lower alkenyl, lower alkenyl oxy, cyano, hydroxy, trifluoromethyl, nitro, amino, aminocarbonylmethyl, lower monoalkylamino, lower dialkylamino group;R.sub.2 is a hydrogen or halogen atom, cyano, lower alkyl or lower alkoxy or acylamino group;R.sub.3 is a hydrogen or halogen atom, a lower alkyl or lower alkoxy group, while R.sub.2 and R.sub.3 together can also be a butadienyl or methylene dioxy group;R.sub.4 is a hydrogen atom or a lower alkyl group;R.sub.5 is a chlorine atom or a trifluoromethyl group;X is an alkylene group;and the non-toxic, pharmaceutically acceptable acid addition salts thereof.The compounds are suitable for treatment and prophylaxis of hypertension.
摘要翻译：公开了具有下式的新化合物：其中R1是氢或卤原子，低级烷基，低级烷氧基，低级烷氧基低级烷基，低级烯基，低级烯基氧基，氰基，羟基，三氟甲基，硝基，氨基，氨基羰基甲基，低级单烷基氨基，低级二烷基氨基; R2是氢或卤素原子，氰基，低级烷基或低级烷氧基或酰氨基; R3是氢或卤素原子，低级烷基或低级烷氧基，R2和R3一起也可以是丁二烯基或亚甲基二氧基; R4是氢原子或低级烷基; R5是氯原子或三氟甲基; X是亚烷基; 和其无毒的药学上可接受的酸加成盐。该化合物适用于治疗和预防高血压。

2. 发明授权

US4259346A Bradycardiac pharmaceutical compositions and method of use 失效
标题翻译：心动过缓药物组合物和使用方法
公开(公告)号：US4259346A
公开(公告)日：1981-03-31
申请号：US103584
申请日：1979-12-14
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
IPC分类号： A61K31/415 , A61P9/06 , A61P9/10 , C07D233/52
CPC分类号： C07D233/52
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, hydroxy-lower alkyl, chloro-hydroxy-propyl, 2,3-epoxy-propyl, alkoxyalkyl, aminoalkyl, N-substituted aminoalkyl, benzyl or phenethyl,R.sub.3 is hydrogen or halogen, andR.sub.4 is halogen or methyl, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as bradycardiacs.
摘要翻译：其中R 1为氢或低级烷基，R 2为氢，低级烷基，羟基 - 低级烷基，氯 - 羟基 - 丙基，2,3-环氧丙基，烷氧基烷基，氨基烷基，N-取代的氨基烷基，苄基或苯乙基，R3是氢或卤素，R4是卤素或甲基，或其无毒的药学上可接受的酸加成盐; 以及使用其作为心动过缓的方法。

3. 发明授权

US4250186A Method of slowing heart rate 失效
标题翻译：减慢心率的方法
公开(公告)号：US4250186A
公开(公告)日：1981-02-10
申请号：US12650
申请日：1979-02-16
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Wolfgang Hoefke , Wolfram Gaida , Ludwig Pichler
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Wolfgang Hoefke , Wolfram Gaida , Ludwig Pichler
IPC分类号： C07D233/44 , A61K31/415 , A61K31/4168 , A61P9/00 , A61P9/06 , A61P9/10 , C07D233/50
CPC分类号： C07D233/50
摘要： Compounds of the formula ##STR1## wherein R is 2-bromo-4,5-dihydroxy-phenyl; 3-chloro-4-hydroxy-phenyl; 4-bromo-2,5-dihydroxy-phenyl; 3,5-dihydroxy-phenyl; 5-chloro-2,4-dihydroxy-phenyl; 3-hydroxy-4-methyl-phenyl; 2,6-dibromo-4-hydroxymethyl-phenyl; 3,5-dibromo-4-amino-phenyl; 3-methylmercapto-phenyl; 3,4,5-trihydroxy-phenyl; or 3-bromo-4-fluoro-phenyl;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是2-溴-4,5-二羟基 - 苯基的式IMAMA的化合物; 3-氯-4-羟基 - 苯基; 4-溴-2,5-二羟基 - 苯基; 3,5-二羟基 - 苯基; 5-氯-2,4-二羟基 - 苯基; 3-羟基-4-甲基 - 苯基; 2,6-二溴-4-羟甲基 - 苯基; 3,5-二溴-4-氨基 - 苯基; 3-甲基巯基 - 苯基; 3,4,5-三羟基 - 苯基; 或3-溴-4-氟 - 苯基; 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。

4. 发明授权

US4454149A Imidazo[1,2-a]imidazoles in the treatment of pain, hypertonia and coronary diseases 失效
标题翻译：咪唑并[1,2-a]咪唑治疗疼痛，高血压和冠心病
公开(公告)号：US4454149A
公开(公告)日：1984-06-12
申请号：US389283
申请日：1982-06-17
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfgang Hoefke , Wolfram Gaida
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfgang Hoefke , Wolfram Gaida
IPC分类号： A61K31/415 , A61K31/4188 , A61P9/06 , A61P9/12 , A61P25/04 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to substituted imidazo[1,2-a]imidazoles and non-toxic, pharmaceutically acceptable salts thereof. These compounds are useful in relieving pain and in treating hypertonia and coronary diseases.
摘要翻译：本发明涉及取代的咪唑并[1,2-a]咪唑及其无毒的药学上可接受的盐。这些化合物可用于缓解疼痛和治疗高血压和冠状动脉疾病。

5. 发明授权

US4361575A Substituted 2-phenylamino-2-imidazolines and salts thereof 失效
标题翻译：取代的2-苯基氨基-2-咪唑啉及其盐
公开(公告)号：US4361575A
公开(公告)日：1982-11-30
申请号：US276703
申请日：1981-06-23
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
IPC分类号： A61K31/415 , A61P9/06 , C07D233/50 , C07D233/52 , C07D233/06
CPC分类号： C07D233/50
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, trifluoromethyl, hydroxyl or amino;R.sub.4 is straight or branched alkyl of 1 to 5 carbon atoms, allyl or benzyl;R.sub.5 is methyl, ethyl or 2-dimethylamino-ethyl; andn is 0 or 1;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，三氟甲基，羟基或氨基; R4是1至5个碳原子的直链或支链烷基，烯丙基或苄基; R5是甲基，乙基或2-二甲基氨基 - 乙基; 并且n为0或1; 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。

6. 发明授权

US4438118A Substituted imidazo[1,2-a]pyrimidines and pharmaceutical compositions containing them 失效
标题翻译：取代的咪唑并[1,2-a]嘧啶和含有它们的药物组合物
公开(公告)号：US4438118A
公开(公告)日：1984-03-20
申请号：US389284
申请日：1982-06-17
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfram Gaida , Wolfgang Hoefke
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfram Gaida , Wolfgang Hoefke
IPC分类号： A61K31/505 , A61P9/06 , A61P9/12 , A61P25/04 , C07D487/04 , C07D487/00
CPC分类号： C07D487/04
摘要： This invention relates to substituted imidazo[1,2-a]pyrimidines and non-toxic, pharmaceutically acceptable salts thereof. These compounds are useful in relieving pain and in treating hypertonia and coronary diseases.
摘要翻译：本发明涉及取代的咪唑并[1,2-a]嘧啶及其无毒的药学上可接受的盐。这些化合物可用于缓解疼痛和治疗高血压和冠状动脉疾病。

7. 发明授权

US4293564A 2-(3,5-Dibromo-4-amino-phenylimino)-imidazolidine, salts and compositions thereof 失效
标题翻译： 2-（3,5-二溴-4-氨基 - 苯基亚氨基） - 咪唑烷，其盐和组合物
公开(公告)号：US4293564A
公开(公告)日：1981-10-06
申请号：US179839
申请日：1980-08-20
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Wolfgang Hoefke , Wolfram Gaida , Ludwig Pichler
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Wolfgang Hoefke , Wolfram Gaida , Ludwig Pichler
IPC分类号： C07D233/44 , A61K31/415 , A61K31/4168 , A61P9/00 , A61P9/06 , A61P9/10 , C07D233/50
CPC分类号： C07D233/50
摘要： The compound of the formula ##STR1## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compound as well as its salts are useful as bradycardiacs.
摘要翻译：式“IMAGE”的化合物及其无毒的药学上可接受的酸加成盐。该化合物及其盐可用作心动过缓。

8. 发明授权

US4296117A 1-Aryloxy-2-hydroxy-3-[(Benzimidazolinone-substituted alkyl)-amino]propanes and salts thereof 失效
标题翻译： 1-芳氧基-2-羟基-3 - [（苯并咪唑啉酮取代的烷基） - 氨基]丙烷及其盐
公开(公告)号：US4296117A
公开(公告)日：1981-10-20
申请号：US112640
申请日：1980-01-16
申请人： Herbert Koppe , Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Gojko Muacevic
发明人： Herbert Koppe , Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Gojko Muacevic
IPC分类号： C07D233/36 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/435 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/538 , A61P9/00 , A61P25/24 , A61P25/26 , C07D205/04 , C07D209/34 , C07D215/22 , C07D215/227 , C07D233/32 , C07D235/26 , C07D265/18 , C07D265/28 , C07D265/30
CPC分类号： C07D215/227 , C07D209/34 , C07D233/32 , C07D235/26 , C07D265/18 , C07D265/28
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen; alkyl of 1 to 5 carbon atoms; or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要翻译：其中R 1，R 2和R 3为氢或各种取代基的式IMAMA的化合物; R4是氢; 1至5个碳原子的烷基; 或任选取代的具有7-14个碳原子的芳烷基; R5是杂环; D是1至12个碳原子的亚烷基; A是氢或酰基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作α-和β-肾上腺素能受体阻断剂和抗抑郁药。

9. 发明授权

US4212877A 1-Aryloxy-2-hydroxy-3-[(benzimidazolin-one-substituted alkyl)-amino]-propanes and salts thereof 失效
标题翻译： 1-芳氧基-2-羟基-3 - [（苯并咪唑啉-1-取代的烷基） - 氨基] - 丙烷及其盐
公开(公告)号：US4212877A
公开(公告)日：1980-07-15
申请号：US4280
申请日：1979-01-17
申请人： Herbert Koppe , Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Gojko Muacevic
发明人： Herbert Koppe , Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Gojko Muacevic
IPC分类号： C07D233/36 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/435 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/538 , A61P9/00 , A61P25/24 , A61P25/26 , C07D205/04 , C07D209/34 , C07D215/22 , C07D215/227 , C07D233/32 , C07D235/26 , C07D265/18 , C07D265/28 , C07D265/30
CPC分类号： C07D215/227 , C07D209/34 , C07D233/32 , C07D235/26 , C07D265/18 , C07D265/28
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms, or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
摘要翻译：其中R 1，R 2和R 3为氢或各种取代基的式IMAMA的化合物; R4是氢，1至5个碳原子的烷基或任选取代的具有7-14个碳原子的芳烷基; R5是杂环; D是1至12个碳原子的亚烷基; A是氢或酰基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作α-和β-肾上腺素能受体阻断剂和抗抑郁药。

10. 发明授权

US4025607A Propargyl-substituted 2-phenylamino-2-imidazolines and salts thereof 失效
标题翻译：炔丙基取代的2-苯基氨基-2-咪唑啉及其盐
公开(公告)号：US4025607A
公开(公告)日：1977-05-24
申请号：US687250
申请日：1976-05-17
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfgang Hoefke , Franz Josef Kuhn
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus , Wolfgang Hoefke , Franz Josef Kuhn
IPC分类号： C07D233/44 , A61K31/415 , A61K31/4168 , A61P9/12 , A61P25/04 , C07D233/50
CPC分类号： C07D233/50
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, ethyl, methoxy or trifluoromethyl, andR.sub.4 and R.sub.5 are each hydrogen or propargyl, but other than both hydrogen or both propargyl at the same time,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as analgesics and hypotensives.
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，乙基，甲氧基或三氟甲基，R 4和R 5各自为氢或炔丙基，但不包括氢或炔丙炔，同时和非毒性，药理学上可接受的酸添加量; 该化合物作为盐作为有用的分析和低温。

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