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1. 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。

2. 发明授权

US4343811A 2[3-(4-Chlorophenyl)-1,2-dimethyl-1H-indol-5-yloxy]-2-methyl propanoic acid and hyperlipidemic or atheosclerotic use thereof 失效
标题翻译： 2 [3-（4-氯苯基）-1,2-二甲基-1H-吲哚-5-基氧基] -2-甲基丙酸和其高脂血症或动脉粥样硬化用途
公开(公告)号：US4343811A
公开(公告)日：1982-08-10
申请号：US126006
申请日：1980-02-29
申请人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
发明人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
IPC分类号： C07D401/04 , A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61P3/06 , A61P9/10 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/43 , C07D401/06 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D487/04 , Y10S514/824
摘要： This invention relates to novel indole derivatives of formula ##STR1## and the non-toxic, pharmacologically acceptable salts thereof. These compounds exhibit desirable pharmacological properties, especially lipid-level lowering and anti-atherosclerotic activity. The compounds of the invention may be prepared by, for example, alkylation of a corresponding hydroxy indole.
摘要翻译：本发明涉及式IMA的新型吲哚衍生物及其无毒的药理学上可接受的盐。这些化合物显示出所需的药理学性质，特别是脂质降低和抗动脉粥样硬化活性。本发明的化合物可以通过例如相应的羟基吲哚的烷基化来制备。

3. 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.

4. 发明授权

US4042711A Derivatives of biphenyloxy-lower alkanoic acids, salts thereof and their use as antihyperlipidemics 失效
标题翻译：联苯氧基 - 低级链烷酸的衍生物，其盐及其作为抗高脂血症的用途
公开(公告)号：US4042711A
公开(公告)日：1977-08-16
申请号：US740829
申请日：1976-11-11
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： C07C217/62 , C07D209/48 , C07D213/82 , C07C103/46 , C07C103/737 , 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,A is --CO--NH-- or --NH--CO--, andn is 1, 2 or 3,And non-toxic salts thereof formed with an inorganic or organic base; the compounds as well as the salts are useful as antihyperlipidemics.
摘要翻译：其中R 1为1至6个碳原子的直链或支链烷基，3至6个碳原子的环烷基，苯基烷基，苯基烯基，吡啶基或者其中X，Y和Z各自为氢，卤素， 1至3个碳原子的烷基或1至3个碳原子的烷氧基，R 2是氢或1至4个碳原子的烷基，A是-CO-NH-或-NH-CO-，N IS 1,2或3 ，以及与无机或有机基体形成的非毒性盐; 化合物作为抗生素可用作销售。

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. 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。

7. 发明授权

US6143769A Phenylacetic acid benzylamides 失效
标题翻译：苯乙酸苄基酰胺
公开(公告)号：US6143769A
公开(公告)日：2000-11-07
申请号：US180587
申请日：1994-05-09
申请人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
发明人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
IPC分类号： C07D295/135 , C07D295/155 , C07D307/14 , C07D309/04 , A61K31/445 , C07D211/08
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。

8. 发明授权

US5216167A Phenylacetic acid benzylamides 失效
标题翻译：苯乙酸苄基酰胺
公开(公告)号：US5216167A
公开(公告)日：1993-06-01
申请号：US495820
申请日：1990-06-21
申请人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
发明人： Wolfgang Grell , Rudolf Hurnaus , Gerhart Griss, deceased , Robert Sauter , Manfred Reiffen , Eckhard Rupprecht
IPC分类号： C07D295/135 , C07D295/155 , C07D307/14 , C07D309/04
CPC分类号： C07D295/135 , C07D295/155 , C07D307/14 , C07D309/04 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
摘要翻译：公开了具有以下通式结构的苯乙酸苄基酰胺，其中取代基在本文中定义，哪些化合物是低血糖剂。

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

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。

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