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RU95114449A - Derivatives of 4-aryl- or heteroaryl-6-amino-nicotinic acid, a mixture of their isomers or separate isomers, and also a pharmaceutical composition with a modulatory cali num ate ia i'm i'm i'm i'm i'm going - Google Patents

Derivatives of 4-aryl- or heteroaryl-6-amino-nicotinic acid, a mixture of their isomers or separate isomers, and also a pharmaceutical composition with a modulatory cali num ate ia i'm i'm i'm i'm i'm going

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Publication number
RU95114449A
RU95114449A RU95114449/04A RU95114449A RU95114449A RU 95114449 A RU95114449 A RU 95114449A RU 95114449/04 A RU95114449/04 A RU 95114449/04A RU 95114449 A RU95114449 A RU 95114449A RU 95114449 A RU95114449 A RU 95114449A
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RU
Russia
Prior art keywords
carbon atoms
unbranched
cyano
isomers
branched
Prior art date
Application number
RU95114449/04A
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Russian (ru)
Other versions
RU2154635C2 (en
Inventor
Урбанс Клаус
Гольдманн Зигфрид
Хейне Ханс-Георг
Юнге Бодо
Шохе-Лооп Рудольф
ЗОММЕРМЕЙЕР Хеннинг
Глазер Томас
ВИТТКА Рейлинде
де Ври Жан-Мари-Виктор
Original Assignee
Байер Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE4430638A external-priority patent/DE4430638A1/en
Application filed by Байер Аг filed Critical Байер Аг
Publication of RU95114449A publication Critical patent/RU95114449A/en
Application granted granted Critical
Publication of RU2154635C2 publication Critical patent/RU2154635C2/en

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Claims (4)

1. Производные 4-арил- или гетероарил-6-амино-никотиновой кислоты общей формулы I
Figure 00000001

где А - арил с 6-10 атомами углерода и пиридил, незамещенные или замещенные 1 - 3 одинаковыми или различными остатками из группы, включающей нитро, циано, фенил, галоген и трифторметил, или неразветвленной или разветвленной алкилтио-группой с 1 - 6 атомами углерода или неразветвленным или разветвленным алкоксилом с 1 - 6 атомами углерода,
D - циано или нитро;
R1 - водород или неразветвленный или разветвленный алкил с 1 - 8 атомами углерода,
R2 и R3 одинаковы или различны и означают водород или неразветвленный или разветвленный алкил с 1-6 атомами углерода или неразветвленный или разветвленный ацил с 1 - 6 атомами углерода,
при этом, если А означает фенил, незамещенный или замещенный в положении 4 хлором, метоксилом или нитро-группой, D - циано и R2 и R3 одинаковы и означают водород, то радикал R1 не означает этил,
смесь изомеров или отдельные изомеры и их соли.
1. Derivatives of 4-aryl or heteroaryl-6-amino-nicotinic acid of general formula I
Figure 00000001

where A is aryl with 6-10 carbon atoms and pyridyl, unsubstituted or substituted by 1 to 3 identical or different residues from the group including nitro, cyano, phenyl, halogen and trifluoromethyl, or an unbranched or branched alkylthio group with 1 to 6 carbon atoms or unbranched or branched alkoxy with 1 to 6 carbon atoms,
D - cyano or nitro;
R 1 is hydrogen or unbranched or branched alkyl with 1 to 8 carbon atoms,
R 2 and R 3 are the same or different and denote hydrogen or unbranched or branched alkyl with 1-6 carbon atoms or a unbranched or branched acyl with 1 to 6 carbon atoms,
moreover, if A means phenyl unsubstituted or substituted in position 4 with chlorine, methoxy or a nitro group, D means cyano and R 2 and R 3 are the same and mean hydrogen, then the radical R 1 does not mean ethyl,
a mixture of isomers or individual isomers and their salts.
2. Производные 4-арил- или гетероарил-6-амино-никотиновой кислоты общей формулы I по п. 1,
где А - фенил и нафтил, незамещенные или замещенные 1 - 3 одинаковыми или различными остатками из группы, включающей нитро, циано, фтор, хлор, бром, йод, фенил и трифторметил, или неразветвленной или разветвленной алкилтио-группой с 1 - 4 атомами углерода или неразветвленным или разветвленным алкоксилом с 1 - 4 атомами углерода,
D - циано или нитро;
R1 - водород или неразветвленный или разветвленный алкил с 1 - 6 атомами углерода;
R2 и R3 одинаковы или различны и означают водород или неразветвленный или разветвленный алкил с 1 - 4 атомами углерода или неразветвленный или разветвленный ацил с 1-4 атомами углерода,
при этом, если А означает фенил, незамещенный или замещенный в положении 4 хлором, метоксилом или нитро-группой, D - циано и R2 и R3 одинаковы и означают водород, то радикал R1 не означает этил,
смесь их изомеров или отдельные изомеры и их соли.
2. Derivatives of 4-aryl or heteroaryl-6-amino-nicotinic acid of general formula I according to claim 1,
where A is phenyl and naphthyl, unsubstituted or substituted by 1 to 3 identical or different residues from the group including nitro, cyano, fluorine, chlorine, bromine, iodine, phenyl and trifluoromethyl, or a straight or branched alkylthio group with 1 to 4 carbon atoms or unbranched or branched alkoxy with 1-4 carbon atoms,
D - cyano or nitro;
R 1 is hydrogen or unbranched or branched alkyl with 1 to 6 carbon atoms;
R 2 and R 3 are the same or different and denote hydrogen or unbranched or branched alkyl with 1 to 4 carbon atoms or a unbranched or branched acyl with 1-4 carbon atoms,
moreover, if A means phenyl unsubstituted or substituted in position 4 with chlorine, methoxy or a nitro group, D means cyano and R 2 and R 3 are the same and mean hydrogen, then the radical R 1 does not mean ethyl,
a mixture of their isomers or individual isomers and their salts.
3. Производные 4-арил- или гетероарил-6-амино-никотиновой кислоты общей формулы I по п. 1,
где А - фенил, незамещенный или замещенный 1 - 2 одинаковыми или различными остатками из группы, включающей нитро, циано, фтор, хлор, бром, йод, фенил, трифторметил, метокси и метилтио,
D - циано или нитро;
R1 - водород или неразветвленный или разветвленный алкил с 1 - 4 атомами углерода;
R2 и R3 одинаковы или различны и означают водород или неразветвленный или разветвленный алкил с 1-3 атомами углерода или неразветвленный или разветвленный ацил с 1 - 3 атомами углерода,
при этом, если А означает фенил, незамещенный или замещенный в положении 4 хлором, метоксилом или нитро-группой, D - циано и R2 и R3 одинаковы и означают водород, то радикал R1 не означает этил,
смесь их изомеров или отдельные изомеры и их соли.
3. 4-aryl- or heteroaryl-6-amino-nicotinic acid derivatives of general formula I according to claim 1,
where A is phenyl, unsubstituted or substituted by 1 to 2 identical or different residues from the group including nitro, cyano, fluorine, chlorine, bromine, iodine, phenyl, trifluoromethyl, methoxy and methylthio,
D - cyano or nitro;
R 1 is hydrogen or unbranched or branched alkyl with 1 to 4 carbon atoms;
R 2 and R 3 are the same or different and mean hydrogen or a straight or branched alkyl with 1 to 3 carbon atoms or a straight or branched acyl with 1 to 3 carbon atoms,
moreover, if A means phenyl unsubstituted or substituted in position 4 with chlorine, methoxy or a nitro group, D means cyano and R 2 and R 3 are the same and mean hydrogen, then the radical R 1 does not mean ethyl,
a mixture of their isomers or individual isomers and their salts.
4. Фармацевтическая композиция с модулирующим калиевые канальцы действием, содержащая активное начало и по крайней мере один фармацевтически приемлемый, нетоксичный инертный носитель, отличающаяся тем, что она содержит в качестве активного начала соединение вышеуказанной общей формулы I,
Figure 00000002

где А - арил с 6-10 атомами углерода и пиридил, незамещенные или замещенные 1 - 3 одинаковыми или различными остатками из группы, включающей нитро, циано, фенил, галоген и трифторметил, или неразветвленной или разветвленной алкилтио-группой с 1-6 атомами углерода или неразветвленным или разветвленным алкоксилом с 1 - 6 атомами углерода,
D - циано или нитро;
R1 - водород или неразветвленный или разветвленный алкил с 1 - 8 атомами углерода;
R2 и R3 одинаковы или различны и означают водород или неразветвленный или разветвленный алкил с 1-6 атомами углерода или неразветвленный или разветвленный ацил с 1 - 6 атомами углерода,
смесь его изомеров или отдельный изомер или его соль в эффективном количестве.
4. Pharmaceutical composition with modulating potassium tubules action, containing the active principle and at least one pharmaceutically acceptable, non-toxic inert carrier, characterized in that it contains as active principle a compound of the aforementioned general formula I,
Figure 00000002

where A is aryl with 6-10 carbon atoms and pyridyl, unsubstituted or substituted by 1 to 3 identical or different residues from the group including nitro, cyano, phenyl, halogen and trifluoromethyl, or a straight or branched alkylthio group with 1-6 carbon atoms or unbranched or branched alkoxy with 1 to 6 carbon atoms,
D - cyano or nitro;
R 1 is hydrogen or unbranched or branched alkyl with 1 to 8 carbon atoms;
R 2 and R 3 are the same or different and denote hydrogen or unbranched or branched alkyl with 1-6 carbon atoms or a unbranched or branched acyl with 1 to 6 carbon atoms,
a mixture of its isomers or a single isomer or its salt in an effective amount.
RU95114449/04A 1994-08-29 1995-08-28 Derivatives of 4-aryl-6-aminonicotinic acid and their salts RU2154635C2 (en)

Applications Claiming Priority (2)

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DEP4430638.5 1994-08-29
DE4430638A DE4430638A1 (en) 1994-08-29 1994-08-29 Use of substituted 4-phenyl-6-amino-nicotinic acid derivatives as a medicament

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DE102006056740A1 (en) * 2006-12-01 2008-06-05 Bayer Healthcare Ag Cyclic substituted 3,5-dicyano-2-thiopyridines and their use
DE102006056739A1 (en) * 2006-12-01 2008-06-05 Bayer Healthcare Ag Substituted 4-amino-3,5-dicyano-2-thiopyridines and their use
DE102007035367A1 (en) * 2007-07-27 2009-01-29 Bayer Healthcare Ag Substituted aryloxazoles and their use
DE102007036076A1 (en) 2007-08-01 2009-02-05 Bayer Healthcare Aktiengesellschaft Dipeptoid Produgs and their use
DE102007061764A1 (en) * 2007-12-20 2009-06-25 Bayer Healthcare Ag Anellated cyanopyridines and their use
DE102007061763A1 (en) * 2007-12-20 2009-06-25 Bayer Healthcare Ag Substituted azabicyclic compounds and their use
DE102008013587A1 (en) * 2008-03-11 2009-09-17 Bayer Schering Pharma Aktiengesellschaft Heteroaryl-substituted dicyanopyridines and their use
CA2726020C (en) * 2008-05-29 2016-08-16 Bayer Schering Pharma Aktiengesellschaft 2-alkoxy-substituted dicyanopyridines and use thereof
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