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1. 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。

2. 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。

3. 发明授权

US4843086A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4843086A
公开(公告)日：1989-06-27
申请号：US124197
申请日：1987-11-23
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms.R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核可各自被1或2个卤素原子取代。 R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而苯基核可以被氟取代，氯或溴原子，R4表示氢原子，烷基，烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，对映体和酸加成的盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

4. 发明授权

US4414225A Azepine derivatives and their anti-thrombotic compositions and methods 失效
标题翻译： Azepine衍生物及其抗血栓形成和方法
公开(公告)号：US4414225A
公开(公告)日：1983-11-08
申请号：US348496
申请日：1982-02-12
申请人： Robert Sauter , Gerhart Griss , Wolfgang Grell , Rudolf Hurnaus , Bernhard Eisele , Walter Haarmann , Eckhard Rupprecht
发明人： Robert Sauter , Gerhart Griss , Wolfgang Grell , Rudolf Hurnaus , Bernhard Eisele , Walter Haarmann , Eckhard Rupprecht
IPC分类号： C07D487/02 , A61K31/55 , A61P3/06 , A61P7/02 , C07D223/06 , C07D487/04 , C07D491/02 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/40
CPC分类号： C07D487/04 , C07D223/06 , C07D491/04 , C07D495/04
摘要： Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.
摘要翻译：其中n和m各自为1,2或3，并且n + m的和为4; R1是烷基; 烯基; 未取代的，单或二取代的芳烷基; 未取代的，单或二取代的苯甲酰基; 烷氧基羰基芳烷氧羰基; 或者当m和n各自为2和/或R 2和R 3不同时为氢时，也为氢; R2和R3之一是氢或氨基，另一个是羧基或烷氧基羰基; 或当R3为氢时，R2为氢; 氨基; 烷氧基羰基 - 氨基; （未取代或单取代的苯基） - 氨基羰基 - ; （未取代或单取代的苯基）乙基氨基羰基; 叠氮羰基; 或肼基羰基; X是氧，硫或者其中R 4是氢; 烷基; 苯基 - 烷基; 或苯基; 无毒，药理学上可接受的酸加成盐; 并且当R 2或R 3为羧基时，与无机或有机碱形成的无毒的药学上可接受的盐。化合物及其盐可用作抗血栓形成剂。

5. 发明授权

US4010279A Biphenyloxy derivatives and antihyperlipidemic use 失效
标题翻译：苯二酚衍生物和抗血小板药物使用
公开(公告)号：US4010279A
公开(公告)日：1977-03-01
申请号：US643700
申请日：1975-12-23
申请人： Gerhart Griss , Wolfgang Grell , Rudolf Hurnaus , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Matyas Leitold
发明人： Gerhart Griss , Wolfgang Grell , Rudolf Hurnaus , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Matyas Leitold
IPC分类号： A61K31/165 , A61K31/19 , A61K31/22 , C07C67/00 , C07C217/62 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/17 , C07C233/18 , C07C233/60 , C07C233/68 , C07C235/34 , C07C235/38 , C07D209/48 , C07D213/82 , A61K31/24 , C07C103/84
CPC分类号： C07D209/48 , C07C217/62 , C07D213/82
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, phenylalkyl, phenylalkenyl, pyridyl or ##STR2## where X, Y and Z are each hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms,R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms,R.sub.3 is hydroxymethyl, carboxyl, alkoxycarbonyl of 2 to 7 carbon atoms or cycloalkoxycarbonyl or 4 to 8 carbon atoms,A is --CO--NH-- or --NH--CO--, andn is 1, 2 or 3,And, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base; the compounds as well as the salts are useful as antihyperlipidemics.

6. 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。

7. 发明授权

US4886812A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4886812A
公开(公告)日：1989-12-12
申请号：US256671
申请日：1988-10-12
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核酸可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基基团可以被氟，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

8. 发明授权

US4731374A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4731374A
公开(公告)日：1988-03-15
申请号：US810947
申请日：1985-12-19
申请人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基基团可以被氟里酰，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

9. 发明授权

US4409220A Fused-ring amino-pyrazines as bradycardiac agents 失效
标题翻译：稠环氨基吡嗪作为心动过缓剂
公开(公告)号：US4409220A
公开(公告)日：1983-10-11
申请号：US297024
申请日：1981-08-27
申请人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
发明人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/495 , A61K31/55 , A61P9/02 , A61P9/06 , A61P9/12 , A61P25/02 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;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A和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基，苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 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。

10. 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。

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