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31. 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。

32. 发明授权

US06949541B2 Substituted piperidines, medicaments containing these compounds, and methods for the production thereof 有权
标题翻译：取代的哌啶，含有这些化合物的药物及其制备方法
公开(公告)号：US06949541B2
公开(公告)日：2005-09-27
申请号：US10169009
申请日：2000-12-22
申请人： Klaus Rudolf , Henri Doods , Eckhart Bauer , Rudolf Hurnaus , Wolfgang Eberlein , Alexander Dreyer , Stephan Georg Mueller
发明人： Klaus Rudolf , Henri Doods , Eckhart Bauer , Rudolf Hurnaus , Wolfgang Eberlein , Alexander Dreyer , Stephan Georg Mueller
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/5513 , A61P11/06 , A61P15/12 , A61P17/00 , A61P25/04 , A61P25/36 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04 , A61K31/445 , A61K38/04 , A61P25/06
CPC分类号： C07D401/14 , C07D401/04
摘要： The present invention relates to substituted piperidines of general formula wherein A1, A2, R, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the 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, their use and processes for preparing them.
摘要翻译：本发明涉及以下通式的取代哌啶：其中A 1，A 2，R 2，R 1和R 2， SUP>如权利要求1中所定义，其互变异构体，非对映异构体，对映异构体，其混合物及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的药理学性质，特别是CGRP拮抗剂性质，含有这些化合物的药物组合物，其用途和制备方法。

33. 发明授权

US06908926B1 Substituted imidazoles, their preparation and use 失效
标题翻译：取代的咪唑，其制备和用途
公开(公告)号：US06908926B1
公开(公告)日：2005-06-21
申请号：US09548081
申请日：2000-04-12
申请人： Florencio Zaragoza Dörwald , Knud Erik Andersen , Tine Krogh Jørgensen , Bernd Peschke , Birgitte Schjellerup Wulff , Ingrid Pettersson , Klaus Rudolf , Dirk Stenkamp , Rudolf Hurnaus , Stephan Georg Müller , Bernd Krist
发明人： Florencio Zaragoza Dörwald , Knud Erik Andersen , Tine Krogh Jørgensen , Bernd Peschke , Birgitte Schjellerup Wulff , Ingrid Pettersson , Klaus Rudolf , Dirk Stenkamp , Rudolf Hurnaus , Stephan Georg Müller , Bernd Krist
IPC分类号： A61K31/437 , C07D235/06 , C07D471/04 , C07D471/10 , C07D487/04
CPC分类号： C07D235/06 , C07D471/04 , C07D471/10 , C07D487/04
摘要： Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.
摘要翻译：公开了一类新颖的取代的咪唑化合物，含有它们的药物组合物和这些化合物在治疗和/或预防与组胺H3受体相关的疾病和病症中的用途。更具体地说，这些化合物可用于治疗和/或预防与组胺H3受体相互作用有益的疾病和病症。这些咪唑化合物具有式I，其中R 1，R 2，R 3，R 4，R 4， SUP> 5，R 6，A，X，Y和Z如说明书中所定义。

34. 发明授权

US06437147B1 Imidazole compounds 失效
标题翻译：咪唑化合物
公开(公告)号：US06437147B1
公开(公告)日：2002-08-20
申请号：US09810237
申请日：2001-03-16
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： A61K3142
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。

35. 发明授权

US5962507A O-acyl-4-phenyl-cyclohexanols, their salts, medicaments containing such compounds, and their use, as well as a method of preparing them 失效
标题翻译： O-酰基-4-苯基 - 环己醇，其盐，含有这些化合物的药物及其用途，以及制备它们的方法
公开(公告)号：US5962507A
公开(公告)日：1999-10-05
申请号：US986101
申请日：1997-12-05
申请人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： C07C219/24 , C07C237/06 , C07D295/096 , A01N43/36 , C07D207/04 , C07D211/18 , C07D211/34
CPC分类号： C07D295/096 , C07C219/24 , C07C237/06 , C07C2101/14
摘要： Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl having up to 17 carbon atoms.
摘要翻译：抑制酶-2,3-环氧喹喔啉 - 羊毛甾醇环化酶和胆固醇生物合成的化合物，其中n表示数字0或1，m表示数字1或2，p表示数字0或1，R1和R2 各自表示氢，低级烷基，烯基或炔基，其也可任选地被取代，或与表示5-或7-元饱和的单环或杂环之间的氮原子一起，其也可任选地被氧或硫中断原子或亚氨基，R3，R4，R5和R6表示氢或低级烷基，R5另外表示低级烷氧基，R7表示氢，环烷基，苯基或取代的苯基，萘基，四氢萘基，噻吩基，呋喃基或吡啶基，A表示化学键或烷基，具有至多17个碳原子的烯基。

36. 发明授权

US5726205A O-acyl-4-phenyl-cyclohexanols, their salts, medicaments containing such compounds and their use, as well as a method of preparing them 失效
标题翻译： O-酰基-4-苯基 - 环己醇，其盐，含有这些化合物的药物及其用途，以及制备它们的方法
公开(公告)号：US5726205A
公开(公告)日：1998-03-10
申请号：US718364
申请日：1997-01-17
申请人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： A23K1/18 , A23K1/16 , A61K31/215 , A61K31/22 , A61K31/24 , A61K31/335 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/4465 , A61K31/455 , A61K31/495 , A61K31/53 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P3/06 , A61P3/10 , A61P9/10 , A61P13/02 , A61P15/00 , A61P31/04 , A61P43/00 , C07C219/24 , C07C219/32 , C07C229/06 , C07C229/08 , C07C237/06 , C07C255/24 , C07C311/06 , C07C311/11 , C07D20060101 , C07D207/08 , C07D213/80 , C07D295/08 , C07D295/096 , C07D307/68 , C07D317/54 , C07D333/40 , A61K31/135
CPC分类号： C07D295/096 , C07C219/24 , C07C237/06 , C07C2101/14
摘要： This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis. The antihypercholesterolaemic substances can be used for the treatment and prophylaxis of atherosclerosis; they inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase.
摘要翻译： PCT No.PCT / EP94 / 01276 Sec。 371日期1997年1月17日 102（e）日期1997年1月17日PCT 1994年4月25日PCT PCT。公开号WO95 / 29148 日期：1995年11月2日本文件描述了通式I（I）的O-酰基-4-苯基 - 环烷醇，其中n表示数字0或1，m表示数字1或2，p表示数字0或 1，R 1和R 2各自表示氢，低级烷基，烯基或炔基，其可以任选地被取代，或者与它们之间的氮原子一起表示可以任选地被中断的5-至7-元饱和的单环杂环通过氧或硫原子或亚氨基，R3，R4，R5和R6表示氢或低级烷基，R5另外表示低级烷氧基，R7表示氢，环烷基，苯基或取代的苯基，萘基，四氢萘基，噻吩基，呋喃基或吡啶基和A表示化学键或具有至多17个碳原子的烷基，烯基或炔基，以及其制备方法，含有这些化合物的药物组合物以及介入胆固醇生物合成的这些药物组合物的用途。抗高胆固醇血症物质可用于治疗和预防动脉粥样硬化; 它们抑制酶2,3-环氧喹喔啉 - 羊毛甾醇环化酶。

37. 发明授权

US4339589A Preparation of 4-substituted oxazolidin-5-ones 失效
标题翻译： 4-取代的恶唑烷-5-酮的制备
公开(公告)号：US4339589A
公开(公告)日：1982-07-13
申请号：US175593
申请日：1980-08-05
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 substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxazolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.
摘要翻译：通过在非质子溶剂中在叔胺存在下，通过2-取代或3,4-二取代的恶唑啉酮 - （5）化合物的烷基化制备4-取代的恶唑啉酮 - （5）化合物，它们是取代的氨基酸的中间体。

38. 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。

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