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21. 发明授权

US5232946A Phenylethanolamines, their use as pharmaceuticals and as performance enhancers in animals 失效
标题翻译：苯乙醇胺，它们用作药物和作为动物中的性能增强剂
公开(公告)号：US5232946A
公开(公告)日：1993-08-03
申请号：US572969
申请日：1990-08-20
申请人： Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Wolfgang Grell , Eckhard Rupprecht
发明人： Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Wolfgang Grell , Eckhard Rupprecht
IPC分类号： A61K31/13 , A61K31/135 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/40 , A61P3/00 , A61P43/00 , C07C213/00 , C07C215/30 , C07C215/32 , C07C215/48 , C07C215/54 , C07C215/68 , C07C217/56 , C07C217/62 , C07C221/00 , C07C225/16 , C07C227/00 , C07C229/38 , C07C233/43 , C07C237/30 , C07C253/30 , C07C255/53 , C07C255/59
CPC分类号： C07C255/00 , C07C229/38
摘要： The invention relates to new phenylethanolamines of general formula ##STR1## wherein A represents a straight-chained or branched alkylene group,B represents a bond, an alkylene group, a carbonyl or hydroxymethylene group,R.sub.1 represents a hydrogen atom, a halogen atom or a trifluoromethyl group,R.sub.2 represents a hydrogen atom or an amino group,R.sub.3 represents a cyano group, a hydrogen, chlorine or bromine atom andR.sub.4 represents a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl group or an alkoxy group substituted in the end position by a carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, pyrrolidino, piperidino or hexamethyleneimino group,the optical isomers and diastereoisomers and acid addition salts thereof.The new compounds of formula I, the optical isomers and diastereoisomers and acid addition salts thereof, particularly the physiologically acceptable acid addition salts thereof with inorganic or organic acids, have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat and they may also be used as performance enhancers in animals.The new compounds of general formula I above may be prepared by methods known per se.
摘要翻译： PCT No.PCT / EP88 / 01083 Sec。 371日期1990年8月20日 102（e）1990年8月20日日期PCT提交1988年11月29日PCT公布。 WO90 / 06299 PCT出版物日本1990年6月14日。本发明涉及通式为（I）的新型苯乙醇胺，其中A表示直链或支链亚烷基，B表示键，亚烷基，羰基或羟基亚甲基，R1 表示氢原子，卤原子或三氟甲基，R 2表示氢原子或氨基，R 3表示氰基，氢，氯或溴原子，R 4表示氢或卤素原子，烷基，羟基，烷氧基羰基，烷氧基羰基，氨基羰基，烷基氨基羰基或二烷基氨基羰基或由羧基，烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，羟基，烷氧基，氨基，烷基氨基，二烷基氨基，吡咯烷子基，哌啶子基或六亚甲基亚氨基取代的烷氧基。光学异构体和非对映异构体及其酸加成盐。式I的新化合物，其光学异构体和非对映异构体及其酸加成盐，特别是其与无机或有机酸的生理上可接受的酸加成盐具有有价值的药理学性质，即对代谢的影响，优选降低血液的作用糖和减少身体脂肪，并且它们也可以用作动物中的性能增强剂。上述通式I的新化合物可以通过本身已知的方法制备。

22. 发明授权

US3992536A Pharmaceutical compositions containing a 1-phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-phenyl of pyridyl)-piperazino]-cyclobutanol-(1) and method of use 失效
标题翻译：含有1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8-吡啶基]苯基） - 哌嗪基{9-环丁醇 - （1 ）和使用方法
公开(公告)号：US3992536A
公开(公告)日：1976-11-16
申请号：US641337
申请日：1975-12-16
申请人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
发明人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
IPC分类号： A61K31/495
CPC分类号： A61K31/495 , Y10S514/906
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbaloxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms,Or a salt thereof with a physiologically compatible inorganic or organic acid or base; and a method of using the same as sedatives and muscle relaxants.
摘要翻译：含有式+ q，10的化合物作为活性成分的药物剂量单位组合物可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，烷基与 1至6个碳原子，具有1至3个碳原子的烷氧基，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5 表示氢原子或具有1至3个碳原子的烷基，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基单 - 或二取代的苯基， 3个碳原子，1〜3个碳原子的烷氧基或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的碳酰氧基，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基，或其与生理上相容的无机或有机酸或碱的盐; 以及将其用作SEDATIVES和MUSCLE RELAXANTS的方法。

23. 发明授权

US3931185A 1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1) 失效
标题翻译： 1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8 4-（苯基或吡啶基） - 哌嗪基{9-环丁烷醇 - （1）
公开(公告)号：US3931185A
公开(公告)日：1976-01-06
申请号：US413233
申请日：1973-11-06
申请人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
发明人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
IPC分类号： C07D295/08 , A61K31/495 , A61K31/496 , C07D213/74 , C07D213/79 , C07D295/00 , C07D295/04 , C07D295/096 , C07D295/135 , C07D405/08 , C07D295/12
CPC分类号： C07D295/096 , A61K31/495 , C07D295/135 , Y10S514/906
摘要： This invention relates to cyclobutane derivatives having the formula ##SPC1##Wherein R.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbalkoxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms;To salts thereof with physiologically compatible inorganic or organic acids or bases as well as to processes for their preparation.The cyclobutane compounds of the above general formula show valuable pharmacological properties, especially a sedative and muscle relaxing activity.
摘要翻译：本发明涉及具有式WHEREIN R 1至R 3的环丁烷衍生物，其可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，具有1-6个碳原子的烷基， 1至3个碳原子，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5表示氢原子或 1至3个碳原子，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基，具有1至3个碳原子的烷基，1至3个碳原子的烷基， 3个碳原子或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的烷氧基，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; 与生理学兼容的有机酸或有机酸或基础同样适用于其制备方法。

24. 发明授权

US5455273A N,N-disubstituted arylcycloalkylamines, the salts thereof, pharmaceutical compositions containing these compounds and the use thereof and processes for preparing them 失效
标题翻译： N，N-二取代的芳基环烷基胺，其盐，含有这些化合物的药物组合物及其用途及其制备方法
公开(公告)号：US5455273A
公开(公告)日：1995-10-03
申请号：US154644
申请日：1993-11-19
申请人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： A61K31/18 , A61K31/27 , A61P1/16 , A61P3/06 , C07C211/27 , C07C211/35 , C07C233/41 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07C311/20 , C07D333/38 , A61K31/165
CPC分类号： C07C311/20 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07D333/38 , C07C2101/02 , C07C2101/14 , C07C2102/04 , C07C2102/10
摘要： The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
摘要翻译：本发明涉及通式为（I）的N，N-二取代的芳基环烷基胺，其中n，m，A，X和R 1至R 7如权利要求1所定义，其异构体，异构体混合物和盐具有有价值的特性，特别是对胆固醇生物合成的抑制作用。

25. 发明授权

US06756384B2 Imidazole compounds 失效
标题翻译：咪唑化合物
公开(公告)号：US06756384B2
公开(公告)日：2004-06-29
申请号：US10201865
申请日：2002-07-23
申请人： Knud Erik Andersen , Florencio Zaragoza Dorwald , Bernd Peschke , Ulla Grove Sidelmann , Klaus Rudolf , Dirk Stenkamp , Rudolf Hurnaus , Stephan Georg Muller , Bernd Krist , Birgitte Eriksen
发明人： Knud Erik Andersen , Florencio Zaragoza Dorwald , Bernd Peschke , Ulla Grove Sidelmann , Klaus Rudolf , Dirk Stenkamp , Rudolf Hurnaus , Stephan Georg Muller , Bernd Krist , Birgitte Eriksen
IPC分类号： A61K3144
CPC分类号： C07D235/04
摘要： A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
摘要翻译：一类新颖的咪唑并杂环化合物，包含它们的药物组合物及其用于治疗和/或预防与组胺H3受体有关的疾病和病症的用途。更具体地，这些化合物可用于治疗和/或预防与组胺H3受体的相互作用有益的疾病和病症。

26. 发明授权

US06346545B1 Urethanes, thio and dithio analogues and their use as inhibitors of cholesterol biosynthesis 有权
标题翻译：聚氨酯，硫代和二硫代类似物及其作为胆固醇生物合成抑制剂的用途
公开(公告)号：US06346545B1
公开(公告)日：2002-02-12
申请号：US09275318
申请日：1999-03-24
申请人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Adelgoss , Gebhard Schilcher
发明人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Adelgoss , Gebhard Schilcher
IPC分类号： A61K3127
CPC分类号： C07D295/135 , C07C271/24 , C07C271/56 , C07C333/06 , C07C333/24 , C07C2601/14 , Y02P20/55
摘要： The present invention relates to urethanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译：本发明涉及聚氨酯，其一般形式的n，A，X，Y和R 1至R 8的硫代和二硫类似物如权利要求1中所定义，其对映异构体，非对映异构体及其盐，特别是生理上可接受的酸加成其具有有价值的性质，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途和制备方法。

27. 发明授权

US07538115B2 Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof 有权
标题翻译：取代的哌啶，含有这些化合物的药物组合物，其用途和制备方法
公开(公告)号：US07538115B2
公开(公告)日：2009-05-26
申请号：US11138868
申请日：2005-05-26
申请人： Rudolf Hurnaus , Klaus Rudolf , Stephan Georg Mueller , Dirk Stenkamp , Philipp Lustenberger , Alexander Dreyer , Kai Gerlach , Marcus Schindler , Kirsten Arndt , Eckhart Bauer
发明人： Rudolf Hurnaus , Klaus Rudolf , Stephan Georg Mueller , Dirk Stenkamp , Philipp Lustenberger , Alexander Dreyer , Kai Gerlach , Marcus Schindler , Kirsten Arndt , Eckhart Bauer
IPC分类号： A61K31/517 , C07D239/72
CPC分类号： C07D471/04 , C07D401/14
摘要： The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
摘要翻译：本发明涉及通式的取代哌啶，其中R，R 2至R 5，A，X，Z和n如权利要求1中所定义，互变异构体，非对映体，对映体，其混合物和盐，特别是其生理上可接受的盐与具有有价值的药理学性质，特别是CGRP拮抗性的无机或有机酸或碱，含有这些化合物的药物组合物，其用途及其制备方法。

28. 发明授权

US5466687A Arylidene-1-azacycloalkanes and arylalkyl-1-azacyclo-alkanes, their salts, medicaments containing these compounds and their use, and processes for their preparation 失效
标题翻译：亚芳基-1-氮杂环烷烃和芳基烷基-1-氮杂环烷烃，其盐，含有这些化合物的药物及其用途及其制备方法
公开(公告)号：US5466687A
公开(公告)日：1995-11-14
申请号：US218092
申请日：1994-03-25
申请人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , A61K31/55 , A61K31/54 , C07D279/06 , C07D405/10
CPC分类号： C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10
摘要： The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.
摘要翻译：本发明涉及通式为（I）（其中n，m，p，A，W 1，W 2，X，Y和R 1至R 11如所定义的亚芳基-1-氮杂环烷烃和芳基烷基-1-氮杂环烷烃权利要求1）及其异构体，异构体混合物和盐，其具有有用的特性，特别是对胆固醇生物合成的抑制作用。

29. 发明授权

US4264771A Alkylation of substituted oxazolinone-(5) compounds 失效
标题翻译：取代的恶唑啉酮 - （5）化合物的烷基化
公开(公告)号：US4264771A
公开(公告)日：1981-04-28
申请号：US891456
申请日：1978-03-29
申请人： Wolfgang Steglich , Rudolf Hurnaus , Peter Gruber , Boerries Kuebel
发明人： Wolfgang Steglich , Rudolf Hurnaus , Peter Gruber , Boerries Kuebel
IPC分类号： C07D263/42 , C07D265/10
CPC分类号： C07D263/42
摘要： Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for .alpha.-substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxozolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.
摘要翻译：通过在非质子传递溶剂中在叔胺存在下将2-取代或3,4-二取代的氧代唑啉酮（5）化合物烷基化制备4-取代的恶唑啉酮 - （5）化合物，它们是α-取代的氨基酸的中间体。

30. 发明授权

US07026312B2 Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof 有权
标题翻译：取代的哌啶，含有这些化合物的药物组合物，其用途和制备方法
公开(公告)号：US07026312B2
公开(公告)日：2006-04-11
申请号：US10388273
申请日：2003-03-13
申请人： Rudolf Hurnaus , Klaus Rudolf , Stephan Georg Mueller , Dirk Stenkamp , Philipp Lustenberger , Alexander Dreyer , Kai Gerlach , Marcus Schindler , Kirsten Arndt , Eckhart Bauer
发明人： Rudolf Hurnaus , Klaus Rudolf , Stephan Georg Mueller , Dirk Stenkamp , Philipp Lustenberger , Alexander Dreyer , Kai Gerlach , Marcus Schindler , Kirsten Arndt , Eckhart Bauer
IPC分类号： A61K31/55 , C07D401/14
CPC分类号： C07D471/04 , C07D401/14
摘要： The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
摘要翻译：本发明涉及通式如下的取代的哌啶：其中R，R 2至R 5，A，X，Z和n如权利要求1所定义，互变异构体，非对映异构体，对映异构体，其混合物和盐，特别是其与具有有价值的药理学特性，特别是CGRP拮抗性质的无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法。

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