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1. 发明授权

US4924004A 1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4924004A
公开(公告)日：1990-05-08
申请号：US264049
申请日：1988-10-28
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen Magda
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/24 , C07D209/42
CPC分类号： C07D209/42
摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkyl or cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is a alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmacological properties, in particular antiarrhythmic properties. The compounds may be in the form of the free base or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.

2. 发明授权

US4803198A 1-Phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4803198A
公开(公告)日：1989-02-07
申请号：US885684
申请日：1986-07-15
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/24 , C07D209/42 , A61K31/55 , C07D403/12 , C07D403/14
CPC分类号： C07D209/42
摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmaceutical properties, in particular antiarrhythmic properties. The compounds may be in the form of the free bases or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.
摘要翻译：描述了具有通式Ⅰ的新的1-苯基-2-氨基羰基吲哚化合物，其中R 1是氢原子，或低级烷基，烯基，环烷基烷基，R 2是氢原子或低级烷基，R 3 是氢或卤素原子，或低级烷基，羟基或低级烷氧基，R4是氢或卤素原子，或低级烷基，羟基或低级烷氧基，或者如果R3是氢原子，R4可以是硝基或三氟甲基，或R 3和R 4一起表示亚甲二氧基或亚乙二氧基，R 5具有R 3的含义，R 6具有对R 4的定义，R 7是氢原子，或者如果R 5和R 6是低级烷氧基，则R 7 也可以是低级烷氧基，R 8和R 9各自为氢原子或低级烷基，或者与氮原子一起形成杂环基，Z为任选被羟基取代的亚烷基链。这些化合物具有药物性质，特别是抗心律失常性质。化合物可以是游离碱或酸加成盐的形式。含有这些化合物的药物组合物被描述为制备它们的方法。还描述了制备这些化合物的有价值的中间体和制备中间体的方法。

3. 发明授权

US4814345A 1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4814345A
公开(公告)日：1989-03-21
申请号：US123201
申请日：1987-11-20
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/42 , A61K31/405
CPC分类号： C07D209/42
摘要： Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.
摘要翻译：公开了具有通式I的新型1-苯基-2-氨基羰基吲哚化合物，其中R 1是脂族或芳族酰基或任选取代的苄基; R2是氢或低级烷基; R3是氢，卤素，低级烷基或低级烷氧基; R4是氢，卤素，低级烷基或低级烷氧基; R5具有给定R3的意义; R6对R4具有重要意义，或R6是硝基或三氟甲基; R7和R8各自表示氢或低级烷基，或与氮原子一起形成杂环基; Z表示任选被羟基或酰氧基取代的亚烷基链。这些化合物具有药理学，特别是抗心律不齐的特性。

4. 发明授权

US4714709A N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof 失效
标题翻译： N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺衍生物及其医药组合物
公开(公告)号：US4714709A
公开(公告)日：1987-12-22
申请号：US653707
申请日：1984-09-24
申请人： Peter W. Thies , Samuel David , Ulrich Kuehl , Gerd Buschmann , Peter Flecker
发明人： Peter W. Thies , Samuel David , Ulrich Kuehl , Gerd Buschmann , Peter Flecker
IPC分类号： A61K31/35 , A61K31/357 , A61P9/12 , C07D319/00 , C07D493/08 , A61K31/40 , C07D405/12
CPC分类号： C07D493/08
摘要： N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.
摘要翻译：对应于具有降血压效果的式“IMAGE”I的N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺化合物，制备这样的化合物和掺入这种化合物的药物组合物，其中R 1是氢，苄基或低级烷基; R2是低级烷基或低级烷酰基; R3是氢或低级烷基; R4是氢，苄氧基，羟基或低级烷氧基; R5是氢，苄氧基，羟基或低级烷氧基; 并且A和B既可以是氢，也可以一起表示它们各自的碳之间的键。

5. 发明授权

US4552877A N.sub.b -Quaternary derivatives of sandwicine and isosandwicine methods and intermediate products in the manufacture of their derivatives and methods of using same and pharmaceutical compositions thereof 失效
标题翻译：萜品四烯衍生物及其衍生物及其使用方法的中间产物及其药物组合物
公开(公告)号：US4552877A
公开(公告)日：1985-11-12
申请号：US615756
申请日：1984-05-31
申请人： Wolfgang Kehrbach , Joachim Wegener , Ulrich Kuehl , Renke Budden , Gerd Buschmann
发明人： Wolfgang Kehrbach , Joachim Wegener , Ulrich Kuehl , Renke Budden , Gerd Buschmann
IPC分类号： C07D229/00 , A61K31/435 , A61K31/437 , A61K31/4375 , A61K31/475 , A61P9/06 , C07D461/00 , C07D471/22 , C07D455/00 , C07D471/08
CPC分类号： C07D471/22
摘要： New N.sub.b -quaternary 10-bromosandwicine and 10-bromoisosandwicine derivatives are disclosed which exhibit antiarrhythmic properties and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup..crclbar. represents an acid anion, as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.
摘要翻译：公开了新的Nb-季10-溴和三羟基衍生物，其表现出抗心律失常性质和肾上腺素能性质，并且具有式I其中R表示含有1-10个碳原子的碳连接的有机基团，A（ - ）代表酸性阴离子，以及其药物制剂及其制备方法和中间体。

6. 发明授权

US4742172A Intermediates for synthesizing pharmaceutically active 3,7-diazabicyclo-(3,3,1)-nonane compounds 失效
标题翻译：用于合成药学活性3,7-二氮杂双环（3,3,1） - 壬烷化合物的中间体
公开(公告)号：US4742172A
公开(公告)日：1988-05-03
申请号：US54868
申请日：1987-05-27
申请人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
发明人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
IPC分类号： A61K31/435 , A61P9/06 , A61P9/10 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10
摘要： 3,7-diaza bicyclo-(3,3,1)-nonane compounds of the formula ##STR1## in which substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4, Z.sub.1, and Z.sub.2 indicate the substituents as they are given in the description of the invention, can be employed to produce certain pharmaceutically useful compounds.
摘要翻译：其中取代基R 1，R 2，R 3，R 4，Z 1和Z 2的3,7-二氮杂双环 - （3,3,1） - 壬烷化合物表示取代基，如在其描述本发明可用于生产某些药学上有用的化合物。

7. 发明授权

US4550112A 3,7-Diazabicyclo(3,3,1)nonane compounds and their use in treating heart disease 失效
标题翻译： 3,7-二氮杂双环（3,3,1）壬烷化合物及其在治疗心脏病中的应用
公开(公告)号：US4550112A
公开(公告)日：1985-10-29
申请号：US532762
申请日：1983-09-16
申请人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
发明人： Uwe Schoen , Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
IPC分类号： A61K31/435 , A61P9/06 , A61P9/10 , C07D471/08 , C07D471/10 , A61K31/445
CPC分类号： C07D471/08 , C07D471/10
摘要： Novel 3,7-diaza bicyclo-(3,3,1)-nonane compounds are described which are represented by the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 each denotes hydrogen,R.sub.1 and R.sub.2 each denotes (A) a substituent which contains up to 12 carbon atoms and which is selected from the group consisting of alkyl, alkenyl, and alkinyl, or (B) a cycloalkyl group containing 3 to 6 carbon atoms which is attached to the nitrogen atom directly or by an alkylene group containing 1 to 3 carbon atoms, andR.sub.3 and R.sub.4 each denotes an alkyl group with up to 7 carbon atoms, or both together form an alkylene chain represented by the formula --(CH.sub.2).sub.n --, wherein n is an integer ranging between about 3 and 6, such that the substituents R.sub.1, R.sub.2, R.sub.3, and R.sub.4 together contain at least 5 carbon atoms. Also described are processes of producing said compounds, pharmaceutical compositions containing compounds of Formula I, and methods of preparing and using said compositions.
摘要翻译：描述了由下式表示的新颖的3,7-二氮杂双环（3,3,1） - 壬烷化合物：其中Z1和Z2各自表示氢，R1和R2各自表示（A）含有至多12个碳原子，并且其选自烷基，烯基和炔基，或（B）含有3至6个碳原子的环烷基，其直接连接到氮原子上或通过含有1至 3个碳原子，并且R 3和R 4各自表示具有至多7个碳原子的烷基，或两者一起形成由式 - （CH 2）n - 表示的亚烷基链，其中n为约3至6的整数，使得取代基R 1，R 2，R 3和R 4一起含有至少5个碳原子。还描述了生产所述化合物的方法，含有式I化合物的药物组合物，以及制备和使用所述组合物的方法。

8. 发明授权

US4415577A Bis-sparteine derivatives and method of using same in therapy 失效
标题翻译：双膦酸衍生物及其在治疗中的应用方法
公开(公告)号：US4415577A
公开(公告)日：1983-11-15
申请号：US294207
申请日：1981-08-19
申请人： Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
发明人： Bernd Hachmeister , Wolfgang Kehrbach , Ulrich Kuehl , Gerd Buschmann
IPC分类号： A61K31/435 , A61P9/06 , C07D471/00 , C07D471/22 , C07D519/00
CPC分类号： C07D471/22 , C07D519/00 , Y10S514/821
摘要： Disclosed are a novel dimeric sparteine derivative, the 17S,17'S-bissparteine, and its physiologically compatible acid addition salts. Said compounds are produced by dimerization of 17-hydroxy sparteine or 17-dehydrosparteine salts by means of activated magnesium or an alkali metal. Pharmaceutical compositions containing said novel dimeric sparteine derivatives and their preparation are also described.
摘要翻译：公开了一种新型二聚斯巴汀衍生物，即17S，17'S-双酚A及其生理相容的酸加成盐。所述化合物是通过活化的镁或碱金属使17-羟基阿片或17-脱氢山梨醇盐进行二聚而产生的。还描述了含有所述新型二聚斯巴汀衍生物的药物组合物及其制备方法。

9. 发明授权

US5164401A Method of diuretic treatment with 3,7-diazabicyclo[3,3,1]nonane compounds 失效
标题翻译：用3,7-二氮杂双环（3,3,1）非络合物进行净化处理的方法
公开(公告)号：US5164401A
公开(公告)日：1992-11-17
申请号：US714886
申请日：1991-06-17
申请人： Kurt Burow , Gerd Buschmann , Arman Farjam , Ulrich Kuehl , Gerda Varchmin , Deiter Ziegler , Uwe Schoen
发明人： Kurt Burow , Gerd Buschmann , Arman Farjam , Ulrich Kuehl , Gerda Varchmin , Deiter Ziegler , Uwe Schoen
IPC分类号： A61K31/435 , A61K31/439 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/12 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , Y10S514/869
摘要： A method of treating a mammal in need of diruetic treatment by administering an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound, diuretic pharmaceutical compositions containing an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound; and previously unknown diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compounds containing an optionally substituted phenylalkyl group in the 3-position.
摘要翻译：通过施用有效的利尿剂量的利尿剂活性的3,7,9,9-四取代的3,7-二氮杂双环[3,3,1]壬烷化合物来治疗需要diruetic治疗的哺乳动物的方法，所述利尿药物组合物含有有利的利尿剂量的利尿剂活性的3,7,9,9-四取代的3,7-二氮杂双环[3,3,1]壬烷化合物; 和在3-位含有任选取代的苯基烷基的以前未知的具有利尿作用的3,7,9,9-四取代3,7-二氮杂双环[3,3,1]壬烷化合物。

10. 发明授权

US4554274A N.sub.b Quaternary derivatives of ajmaline and isoajmaline, methods and intermediate products in the manufacture of their derivatives and method of using same and pharmaceutical compositions thereof 失效
标题翻译： Nb氧化锰和异亚氨酸的季铵盐衍生物，制备其衍生物的方法和中间产物及其使用方法及其药物组合物
公开(公告)号：US4554274A
公开(公告)日：1985-11-19
申请号：US615757
申请日：1984-05-31
申请人： Wolfgang Kehrbach , Joachim Wegener , Ulrich Kuehl , Renke Budden , Gerd Buschmann
发明人： Wolfgang Kehrbach , Joachim Wegener , Ulrich Kuehl , Renke Budden , Gerd Buschmann
IPC分类号： C07D461/00 , A61K31/435 , A61K31/437 , A61K31/4375 , A61P9/06 , C07D471/22 , C07D455/00 , C07D471/08
CPC分类号： C07D471/22
摘要： New quaternary derivatives of 10-bromoajmaline and 10-bromoisoajmaline are disclosed which exhibit antiarrhythmic and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup.- represents an acid anion as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.
摘要翻译：公开了10-溴代马焦氨酸和10-溴异马来酸的新季衍生物，其表现出抗心律失常和肾上腺分离性质，并且具有式I（I）其中R表示含有1-10个碳原子的碳连接的有机基团，A-代表酸性阴离子及其药物制剂及其制备方法和中间体。

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