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1. 发明授权

US5051413A Unsaturated amino acids 失效
标题翻译：不饱和氨基酸
公开(公告)号：US5051413A
公开(公告)日：1991-09-24
申请号：US452995
申请日：1989-12-18
申请人： Christof Angst , Derek E. Brundish , John G. Dingwall , Graham E. Fagg , Hans Allgeier , Guido Bold , Rudolf Duthaler , Roland Heckendorn , Antonio Togni
发明人： Christof Angst , Derek E. Brundish , John G. Dingwall , Graham E. Fagg , Hans Allgeier , Guido Bold , Rudolf Duthaler , Roland Heckendorn , Antonio Togni
IPC分类号： C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/48
CPC分类号： C07F9/4825 , C07F9/302 , C07F9/3217 , C07F9/3826 , C07F9/4015
摘要： The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.
摘要翻译：本发明涉及式I（I）的不饱和氨基酸，其中R 1表示羟基或醚化羟基，R 2表示氢，烷基，羟基或醚化羟基，R 3表示氢，烷基，卤代烷基，羟基烷基，低级烷氧基烷基，芳基烷基，低级烯基，卤素或芳基，R 4表示氢，烷基或芳基，R 5表示氢或烷基，R 6表示羧基或酯化或酰胺化羧基，R 7表示氨基或被烷基或酰基取代的氨基，A表示未取代或烷基取代具有1至3个碳原子的α，ω-亚烷基或表示键，并且B表示亚甲基或键，条件是当B表示键时A不是键，以及其盐。它们可以例如根据Michaelis-Arbuzov反应制造，并且可以用作药理活性物质。

2. 发明授权

US5175344A Unsaturated amino acids 失效
标题翻译：不饱和氨基酸
公开(公告)号：US5175344A
公开(公告)日：1992-12-29
申请号：US731580
申请日：1991-07-17
申请人： Christof Angst , Derek E. Brundish , John G. Dingwall , Graham E. Fagg , Hans Allgeier , Guido Bold , Rudolf Duthaler , Roland Heckendorn , Antonio Togni
发明人： Christof Angst , Derek E. Brundish , John G. Dingwall , Graham E. Fagg , Hans Allgeier , Guido Bold , Rudolf Duthaler , Roland Heckendorn , Antonio Togni
IPC分类号： C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/48
CPC分类号： C07F9/4825 , C07F9/302 , C07F9/3217 , C07F9/3826 , C07F9/4015
摘要： The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.
摘要翻译：本发明涉及式I（I）的不饱和氨基酸，其中R 1表示羟基或醚化羟基，R 2表示氢，烷基，羟基或醚化羟基，R 3表示氢，烷基，卤代烷基，羟基烷基，低级烷氧基烷基，芳基烷基，低级烯基，卤素或芳基，R 4表示氢，烷基或芳基，R 5表示氢或烷基，R 6表示羧基或酯化或酰胺化羧基，R 7表示氨基或被烷基或酰基取代的氨基，A表示未取代或烷基取代具有1至3个碳原子的α，ω-亚烷基或表示键，并且B表示亚甲基或键，条件是当B表示键时A不是键，以及其盐。它们可以例如根据Michaelis-Arbuzov反应制造，并且可以用作药理活性物质。

3. 发明授权

US5294734A 4-substituted 2-aminoalk-3-enoic acids 失效
标题翻译： 4-取代的2-氨基-3-烯酸
公开(公告)号：US5294734A
公开(公告)日：1994-03-15
申请号：US851437
申请日：1992-03-16
申请人： Christof Angst , Hans Allgeier , Roland Heckendorn , Daniel Wallach
发明人： Christof Angst , Hans Allgeier , Roland Heckendorn , Daniel Wallach
IPC分类号： C07F9/38 , C07F9/59 , A61K31/66
CPC分类号： C07F9/592 , C07F9/3826
摘要： Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by optionally acylated or aliphatically or araliphatically etherified hydroxy, by halogen, by optionally acylated and/or aliphatically substituted amino or by an aza-, diaza-, azoxa- or oxa-cycloaliphatic radical, or is an oxacycloaliphatic hydrocarbon radical bonded via a carbon atom, or is an optionally aliphatically N-substituted or N-acylated azacycloaliphatic hydrocarbon radical, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.
摘要翻译：取代的式I的2-氨基-3-烯酸衍生物其中R 1是被任选被酰化或脂族或芳烷基醚化的羟基，被卤素任选被酰化和/或脂族取代的脂族烃基氨基或氮杂 - ，二氮杂 - 氮杂 - 或氧杂 - 脂环族基团，或是通过碳原子键合的氧杂环脂族烃基，或任选地是脂族N-取代或N-酰化氮杂环脂族烃基，R2是游离的或酯化的羧基，它们的盐表现出NMDA-拮抗性质，可用作抗惊厥药物的活性成分。

4. 发明授权

US5488140A 4-substituted 2-aminoalk-3-enoic 失效
标题翻译： 4-取代的2-氨基-3-烯酸
公开(公告)号：US5488140A
公开(公告)日：1996-01-30
申请号：US483628
申请日：1995-06-07
申请人： Christof Angst , Hans Allgeier , Roland Heckendorn , Daniel Wallach
发明人： Christof Angst , Hans Allgeier , Roland Heckendorn , Daniel Wallach
IPC分类号： C07F9/38 , C07F9/59 , C07C229/30 , A61K31/66
CPC分类号： C07F9/592 , C07F9/3826
摘要： Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by hydroxy, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.
摘要翻译：取代的式I的2-氨基-3-烯酸衍生物其中R1是被羟基取代的脂族烃基，R2是游离的或酯化的羧基，它们的盐表现出NMDA-拮抗性质，并且是作为抗惊厥药物的有效成分。

5. 发明授权

US06656957B1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US06656957B1
公开(公告)日：2003-12-02
申请号：US09722803
申请日：2000-11-27
申请人： Hans Allgeier , Yves Auberson , Michel Biollaz , Nicholas David Cosford , Fabrizio Gasparini , Roland Heckendorn , Edwin Carl Johnson , Rainer Kuhn , Mark Andrew Varney , Gönül Veliçelebi
发明人： Hans Allgeier , Yves Auberson , Michel Biollaz , Nicholas David Cosford , Fabrizio Gasparini , Roland Heckendorn , Edwin Carl Johnson , Rainer Kuhn , Mark Andrew Varney , Gönül Veliçelebi
IPC分类号： C07D40112
CPC分类号： C07D213/06 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/53 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/89 , C07D215/12 , C07D401/06 , C07D401/10 , C07D405/06 , C07D409/06 , C07F7/0812
摘要： A compound of formula I wherein X represents an optionally halo-substituted (C2-4)alkynylene group bonded via vicinal unsaturated carbon atoms.
摘要翻译：式I的化合物，其中X表示通过连续不饱和碳原子键合的任选卤素取代的（C 2-4）亚炔基。

6. 发明授权

US3943145A 6-Phenyl-4H-v-triazolo[1,5-a][1,4]benzodiazepines 失效
标题翻译： 6-苯基-4H-哒嗪-3-基）{8,1-a {9 {8 1,4 {9 benzodiazepines
公开(公告)号：US3943145A
公开(公告)日：1976-03-09
申请号：US427167
申请日：1973-12-20
申请人： Andre Gagneux , Roland Heckendorn , Rene Meier
发明人： Andre Gagneux , Roland Heckendorn , Rene Meier
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07C247/00
摘要： Compounds of the class of 6-phenyl-4H-v-triazolo[1,5-a][1,4] benzodiazepines, which in the 3-position are unsubstituted or substituted, particularly by a carbamoyl group or a substituted carbamoyl group, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anticonvulsive and anti-aggressive action. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-v-triazolo [1,5-a][1,4]benzodiazepine-3-carboxamide and N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-v-triazolo [1,5-a][1,4]benzodiazepine-3-carboxamide.
摘要翻译： 6-苯基-4H-v-三唑并[1,5-a] [1,4]苯并二氮杂类化合物，其3-位未被取代或被取代，尤其是氨基甲酰基或取代的氨基甲酰基取代，其5-氧化物及其药学上可接受的酸加成盐具有有价值的药理学性质，并且是治疗组合物的活性成分。特别地，这些新化合物具有抗惊厥和抗侵袭作用。具体实施方案是N，N-二甲基-6-苯基-8-氯-4H-哒嗪并[1,5-a] [1,4]苯并二氮杂-3-甲酰胺和N，N-二甲基-6-（o - 氟苯基）-8-氯-4H-哒嗪并[1,5-a] [1,4]苯并二氮杂-3-甲酰胺。

7. 发明授权

US4209516A Triazole derivatives 失效
公开(公告)号：US4209516A
公开(公告)日：1980-06-24
申请号：US938623
申请日：1978-08-31
申请人： Roland Heckendorn , Rene Meier
发明人： Roland Heckendorn , Rene Meier
IPC分类号： C07D249/08 , A61K31/41 , C07D249/10 , C07D401/06 , C07D413/06
CPC分类号： C07D249/08
摘要： The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl,R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anti-convulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation. Specific embodiments are 1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-(morpholinomethyl)-1H-1,2,4-triazole-3-carboxamide,1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-tariazole-3-carboxamide, N-methyl-1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-(morpholinomethyl)-1H-1,2,4-triazole-3-carboxamide, N-ethyl-1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-(morpholinomethyl)-1H-1,2,4-triazole-3-carboxamide, N-ethyl-1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-triazole-3-carboxamide, N-propyl-1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-triazole-3-carboxamide, N,N-dimethyl-1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-triazole-3-carboxamide, and N,N-dimethyl-1-[2-(o-fluorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-triazole-3-carboxamide.

8. 发明授权

US4045570A Heterocyclic S-imino-S-oxides 失效
标题翻译：杂环S-亚氨基-S-氧化物
公开(公告)号：US4045570A
公开(公告)日：1977-08-30
申请号：US575319
申请日：1975-05-07
申请人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
发明人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
IPC分类号： C07D337/14 , C07D495/04
CPC分类号： C07D495/04 , C07D337/14
摘要： The invention relates to new heterocyclic S-imino-S-oxides of the formula I ##STR1## in which one of the symbols X.sub.1 and X.sub.2 denotes a direct bond and the other denotes the vinylene group --CH=CH-- or the epithio radical --S--, Y.sub.1 and Y.sub.2 conjointly denote an additional bond or one of the symbols denotes hydrogen and the other denotes hydrogen or, conjointly with the symbol R.sub.1 or R.sub.2, which is present on the same carbon atom, denotes the oxo radical, one of the symbols R.sub.1 and R.sub.2 denotes hydrogen or lower alkyl and the other denotes hydrogen or lower alkyl or, conjointly with the symbol Y.sub.1 or Y.sub.2, which is present on the same carbon atom, denotes the oxo radical, or, if Y.sub.1 and Y.sub.2 conjointly denote an additional bond, also denotes lower alkoxy, and R.sub.3 and R.sub.4 independently of one another denote hydrogen, halogen up to atomic number 35, lower alkyl, lower alkoxy or trifluoromethyl and R.sub.5 denotes hydrogen or lower alkyl, and to their acid addition salts in particular the pharmaceutically with inorganic and organic acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anticonvulsive activity and are useful for the treatment of epilepsy and of states of tension and states of agitation.
摘要翻译：本发明涉及式I（I）的新的杂环S-亚氨基-S-氧化物，其中符号X1和X2之一表示直接键，而另一个表示亚乙烯基-CH = CH-或环氧基-S-，Y1和Y2共同表示另外的键，或者一个符号表示氢，另一个表示氢，或与存在于同一碳原子上的符号R 1或R 2结合表示氧代基，符号R1和R2中的一个表示氢或低级烷基，另一个表示氢或低级烷基，或与存在于同一碳原子上的符号Y1或Y2结合表示氧代基，或者如果Y1和Y2 并且表示低级烷氧基，R3和R4彼此独立地表示氢，卤素直至原子数为35，低级烷基，低级烷氧基或三氟甲基，R5表示氢或低级烷基，并且表示其酸加成盐特别是药物中含有的有机和有机可接受的酸加成盐。这些新化合物具有宝贵的药理学特性。特别是它们具有抗惊厥活性，并且可用于治疗癫痫和张力状态和搅动状态。

9. 发明授权

US4027029A Diazepine derivatives 失效
标题翻译：二氮杂衍生物
公开(公告)号：US4027029A
公开(公告)日：1977-05-31
申请号：US535480
申请日：1974-12-23
申请人： Andre Gagneux , Roland Heckendorn , Rene Meier
发明人： Andre Gagneux , Roland Heckendorn , Rene Meier
IPC分类号： A61K31/55 , A61K31/41 , A61K31/445 , A61K31/495 , A61K31/535
CPC分类号： A61K31/55
摘要： Compounds of the class of 6-phenyl-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamides, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anti-convulsive and anti-aggressive action and inhibit somatic reflexes. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide, 6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide, N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide and N,N-dimethyl-6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide.
摘要翻译： 6-苯基-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂-2-甲酰胺类化合物，其5-氧化物及其药学上可接受的酸加成盐具有有价值的药理学性质并且是活性的治疗组合物的成分。特别地，这些新化合物具有抗惊厥和抗侵袭作用并抑制体细胞反射。具体实施方案是N，N-二甲基-6-苯基-8-氯-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂-2-甲酰胺，6-（邻氟苯基）-8- 5-氯-4H-三唑并[1,5-a] [1,4]苯并二氮杂-2-甲酰胺，N，N-二甲基-6-（邻氟苯基）-8-氯-4H-三唑并[1 ，5-a] [1,4]苯并二氮杂-2-甲酰胺和N，N-二甲基-6-（邻氯苯基）-8-氯-4H-三唑并[1,5-a] 4]苯并二氮杂-2-甲酰胺。

10. 发明授权

US3988467A Aminoacyl compounds 失效
标题翻译：氨酰基化合物
公开(公告)号：US3988467A
公开(公告)日：1976-10-26
申请号：US575320
申请日：1975-05-07
申请人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
发明人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
IPC分类号： C07D333/80 , C07C67/00 , C07C325/00 , C07C381/10 , C07D337/14 , C07D495/04
CPC分类号： C07D495/04 , C07D337/14
摘要： The invention relates to new aminoacyl compounds of the formula I, ##SPC1##
摘要翻译：本发明涉及式I，+ Q，10的新的氨酰基化合物

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