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1. 发明授权

US4486433A Fused-ring amino-pyrazines as bradycardiacs 失效
标题翻译：融合环氨基吡嗪作为心动过缓
公开(公告)号：US4486433A
公开(公告)日：1984-12-04
申请号：US501437
申请日：1983-06-06
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。

2. 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。

3. 发明授权

US4575504A Thienothiazole derivatives 失效
标题翻译：噻吩噻唑衍生物
公开(公告)号：US4575504A
公开(公告)日：1986-03-11
申请号：US649898
申请日：1984-09-12
申请人： Robert Sauter , Gerhart Griss, deceased , Wolfgang Grell , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler
发明人： Robert Sauter , Gerhart Griss, deceased , Wolfgang Grell , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/435 , A61K31/55 , A61P9/06 , C07D495/04 , C07D513/14 , A61K31/44
CPC分类号： C07D495/04 , C07D513/14
摘要： Compounds of the formula ##STR1## wherein A is ##STR2## and R is hydrogen, alkyl of 1 to 5 carbon atoms, alkanoyl of 1 to 5 carbon atoms, alkenyl of 3 to 5 carbon atoms, (alkoxy of 1 to 4 carbon atoms)carbonyl, or aralkyl of 7 to 11 carbon atoms optionally halo-substituted,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为X，R为氢，1至5个碳原子的烷基，1至5个碳原子的烷酰基，3至5个碳原子的烯基，（1至4个碳原子的烷氧基））羰基或任选被卤素取代的7至11个碳原子的芳烷基，以及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

US5068325A 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines, their preparation and their use as pharmaceutical compositions 失效
标题翻译： 4,5,7,8-四氢-6H-噻唑（5,4-D）亚胺，其制备及其作为药物组合物的用途
公开(公告)号：US5068325A
公开(公告)日：1991-11-26
申请号：US368753
申请日：1989-06-20
申请人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
发明人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
IPC分类号： A61K31/55 , A61P9/00 , A61P25/00 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to new 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines of general formula II ##STR1## wherein the substituents are defined herein below, which compounds have valuable pharmacological properties, namely selective effects on the dopaminergic system which are achieved by stimulating (predominantly D2) dopamine receptors.
摘要翻译：本发明涉及通式II（II）的新的4,5,7,8-四氢-6H-噻唑并[5,4-d]吖庚因，其中取代基如下文所定义，该化合物具有有价值的药理学性质，即通过刺激（主要是D2）多巴胺受体而实现的对多巴胺能系统的选择性作用。

5. 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。

6. 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.

7. 发明授权

US4735959A Carboxylic acid amides and pharmaceutical compositions containing them 失效
标题翻译：羧酸酰胺和含有它们的药物组合物
公开(公告)号：US4735959A
公开(公告)日：1988-04-05
申请号：US734252
申请日：1985-05-14
申请人： Wolfgang Grell , Gerhart Griss , Robert Sauter , Rudolf Hurnaus , Eckhard Rupprecht , Nikolaus Kaubisch , Joachim Kahling , Bernhard Eisele
发明人： Wolfgang Grell , Gerhart Griss , Robert Sauter , Rudolf Hurnaus , Eckhard Rupprecht , Nikolaus Kaubisch , Joachim Kahling , Bernhard Eisele
IPC分类号： C07D207/26 , C07D207/27 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/70 , C07D211/74 , C07D213/40 , C07D213/80 , C07D217/04 , C07D223/04 , C07D225/02 , C07D295/073 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/192 , C07D317/22 , C07D473/08 , C07D491/10 , A61K31/445 , A61K31/165 , C07C103/82 , C07D295/14
CPC分类号： C07D207/27 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/70 , C07D211/74 , C07D213/40 , C07D213/80 , C07D217/04 , C07D223/04 , C07D225/02 , C07D295/073 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/192 , C07D317/22 , C07D473/08 , C07D491/10 , Y10S514/866
摘要： There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
摘要翻译：描述了式（I）的新型羧酸衍生物和式（Ia）的衍生物及其加成盐，其对中间代谢具有影响。此外，式Ia化合物以及式I化合物具有降血糖特性。

8. 发明授权

US3987047A Tetrahydro-azepinoquinolines 失效
标题翻译：四氮唑腈
公开(公告)号：US3987047A
公开(公告)日：1976-10-19
申请号：US520965
申请日：1974-11-05
申请人： Gerhart Griss , Rudolf Hurnaus , Wolfgang Grell , Robert Sauter , Richard Reichl
发明人： Gerhart Griss , Rudolf Hurnaus , Wolfgang Grell , Robert Sauter , Richard Reichl
IPC分类号： C07D471/04 , C07D491/14 , C07D491/147
CPC分类号： C07D471/04 , C07D491/14 , Y10S514/96 , Y10S514/966
摘要： Compounds of the formula ##SPC1##Wherein ##EQU1## where R.sub.1 is hydrogen, straight or branched aliphatic acyl of 1 to 12 carbon atoms, methoxy-substituted straight or branched aliphatic acyl of 1 to 12 carbon atoms, benzoyl, halo-benzoyl, carbalkoxy of 2 to 7 carbon atoms, carbcycloalkoxy of 4 to 7 carbon atoms, benzyl, methylbenzyl, phenylsulfonyl, halo-phenylsulfonyl, tolylsulfonyl, alkenyl of 2 to 6 carbon atoms, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl, methylsulfonyl or--B -- XwhereB is straight or branched alkylene of 1 to 6 carbon atoms, andX is hydrogen, hydroxyl, methoxy, carboxyl, cyano, dimethylaminocarbonyl, morpholino-carbonyl or carbalkoxy of 2 to 6 carbon atoms,R.sub.2 is hydrogen, hydroxyl, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkanoyloxy of 1 to 3 carbon atoms, alkoxycarbonyloxy of 2 to 4 carbon atoms, amino, dimethylamino, morpholino or halogen,R.sub.3 is hydrogen, halogen, hydroxyl, carboxyl, straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms, phenyl-alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms -- alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms, hydroxymethyl, phenyl, phenoxy, amino, pyrrolidino or morpholino,R.sub.4, r.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen, halogen, methyl, hydroxyl, methoxy, cyano, amino, nitro, trifluoromethyl, carboxyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, or any two of R.sub.4, R.sub.5 and R.sub.6 together are methylenedioxy, andX.sub.1 and X.sub.2 are hydrogen or together form a double bond,6-N-oxides thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anoretics.

9. 再颁专利

USRE37035E1 Phenylacetic acid benzylamides 失效
标题翻译：苯乙酸苄基酰胺
公开(公告)号：USRE37035E1
公开(公告)日：2001-01-30
申请号：US08946602
申请日：1997-10-07
申请人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
发明人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
IPC分类号： A61K3140
CPC分类号： C07D307/14 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D295/135 , C07D295/155 , C07D309/04
摘要： Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
摘要翻译：公开了具有取代基中的以下一般结构的苯乙酸苄基酰胺，其中该化合物是低血糖剂。

10. 发明授权

US5312924A Phenylacetic acid benzylamides 失效
标题翻译：苯乙酸苄基酰胺
公开(公告)号：US5312924A
公开(公告)日：1994-05-17
申请号：US919820
申请日：1992-07-24
申请人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Ruprecht
发明人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Ruprecht
IPC分类号： C07D295/135 , C07D295/155 , C07D307/14 , C07D309/04 , C07D211/32 , A61K31/40 , A61K31/445
CPC分类号： C07D307/14 , C07D295/135 , C07D295/155 , C07D309/04 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： The present application relates to the uses of phenylacetic acid benzylamides and new (S)(+)-2-ethoxy-4-[N-[1-2-piperidino-phenyl)-3-methyl-1-butyl]-aminocarbonylmethyl]benzoic acid and the salts thereof, which have valuable pharmacological properties, namely an effect on the intermediate metabolism, but particularly the effect of lowering blood sugar.
摘要翻译：本申请涉及苯乙酸苄基酰胺和新的（S）（+） - 2-乙氧基-4- [N- [2-哌啶子基 - 苯基）-3-甲基-1-丁基] - 氨基羰基甲基] 苯甲酸及其盐具有有价值的药理学性质，即对中间代谢的作用，特别是降低血糖的作用。

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