RU2002133666A - Производные триазола - Google Patents
Производные триазола Download PDFInfo
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- RU2002133666A RU2002133666A RU2002133666/04A RU2002133666A RU2002133666A RU 2002133666 A RU2002133666 A RU 2002133666A RU 2002133666/04 A RU2002133666/04 A RU 2002133666/04A RU 2002133666 A RU2002133666 A RU 2002133666A RU 2002133666 A RU2002133666 A RU 2002133666A
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Claims (7)
1. Медицинские композиции, обладающие ингибирующей способностью по отношению к переносчику глицина за счет того, что включают производные триазола, которые описываются приведенной ниже общей формулой (I), или их фармакологически приемлемые соли
где символы в формуле принимают следующие значения:
кружок А обозначает (1) ароматическое углеводородное кольцо, которое может быть замещенным,
(2) алифатическое углеводородное кольцо, которое может быть замещенным или конденсированным с бензольным кольцом или гетерокольцом,
(3) пятичленное гетерокольцо, которое может быть замещенным, содержащее один или два атома азота в качестве гетероатомных компонентов кольца, содержащее один атом кислорода или атом серы в качестве другого гетероатома, и которое может быть конденсировано с бензольным кольцом, или
(4) шестичленное гетерокольцо, которое может быть замещенным, содержащее один атом азота в качестве гетероатомного компонента кольца, содержащее один атом кислорода или атом серы в качестве другого гетероатома, и которое может быть конденсировано с бензольным кольцом;
кружок В и кружок D обозначают ароматические углеводородные кольца, которые могут быть замещенными одинаковым или различным образом, алифатические углеводородные кольца, которые могут быть замещенными, или гетерокольца, которые могут быть замещенными;
R обозначает Н, низкомолекулярный галогеноалкил, арил, который может быть замещенным, гетерокольцо, которое может быть замещенным, циклоалкил, который может быть замещенным, или
-[Alk1]m-X-[Alk2]n-Y-R1;
R1 обозначает Н, ОН, циано, арил, который может быть замещенным, гетерокольцо, которое может быть замещенным, циклоалкил, который может быть замещенным, или низкомолекулярную алкоксигруппу;
X обозначает связь, атом кислорода, -S(O)q-, или -N(R2)-;
Y обозначает связь, -С(O)-, -С(O)-N(R3)-, -Z1-Alk3-, или
-N(R3)-Alk3-С(О)-,
где R1 представляет собой группу, отличную от ОН и низкомолекулярных алкоксигрупп в случае, когда Y обозначает связь;
Alk1 и Alk2 могут быть одинаковыми или различными и обозначают низкомолекулярный алкилен, низкомолекулярный алкенилен, или низкомолекулярный алкинилен;
m и n могут быть одинаковыми или различными и равны 0 или 1, причем m+n=1 в случае, когда Х представляет собой связь;
Z1 обозначает -S(O)q-, -N(R3)-, -С(О)- или -С(О)-N(R3)-;
Alk3 обозначает низкомолекулярный алкилен,
R2 и R3 могут быть одинаковыми или различными и обозначают Н или низкомолекулярный алкил, и
q обозначает 0, 1, или 2.
2. Медицинские композиции по п.1, предназначенные для улучшения расстройства обучаемости.
3. Новые производные триазола, выраженные приведенной ниже общей формулой (1а), и
их соли,
в этой формуле символы принимают следующие значения:
кружок А' обозначает (1) группу, которая описывается следующей формулой:
(2) нафталин, который может быть замещенным одной или двумя группами-заместителями, выбранными из групп, выраженных Rf,
(3) алифатическое углеводородное кольцо, которое может быть замещенным одной или двумя группами-заместителями, выбранными из групп, выраженных Rf, и которое может быть конденсировано с бензольным кольцом, или гетерокольцо,
(4) пятичленное гетерокольцо, которое может быть замещенным одной или двумя группами-заместителями, выбранными из групп, выраженных Rf, содержащее один или два атома азота в качестве гетероатомных компонентов кольца, содержащее один атом кислорода или атом серы в качестве другого гетероатома, и которое может быть конденсировано с бензольным кольцом, или
(5) шестичленное гетерокольцо, которое может быть замещенным одной или двумя группами-заместителями, выбранными из групп, выраженных Rf, содержащее один атом азота в качестве входящего в кольцо гетероатома, содержащее один атом кислорода или атом серы в качестве другого гетероатома, и которое может быть конденсировано с бензольным кольцом;
кружок В' обозначает либо бензол, либо азотсодержащее моноциклическое гетерокольцо;
кружок D' обозначает либо бензол, либо гетерокольцо, причем А', В' и D' не обозначают одновременно бензольные кольца;
Ra обозначает низкомолекулярный галогеноалкил, гетерокольцо, которое может быть замещенным, циклоалкил который может быть замещенным, или -[Alk1]m-X-[Alk2]n-Y-R1;
R1 обозначает Н, ОН, циано, арил, который может быть замещенным, гетерокольцо, которое может быть замещенным, циклоалкил, который может быть замещенным, или низкомолекулярную алкоксигруппу;
X обозначает связь, атом кислорода, -S(O)q-, или -N(R2)-,
Y обозначает связь, -С(О)-, -С(O)-N(R3)-, -Z1-Alk3- или -N(R3)-Alk3-С(О)-,
где в случае, когда Y представляет собой связь, R1 обозначает группу, отличную от ОН и низкомолекулярной алкоксигруппы;
Alk1 и Alk2 могут быть одинаковыми или различными и обозначают низкомолекулярный алкилен, низкомолекулярный алкенилен, или низкомолекулярный алкинилен;
m и n могут быть одинаковыми или различными и равны 0 или 1, при условии, что m+n=1 в случае, когда Х обозначает связь;
Z1 обозначает -S(O)q-, -N(R3)-, -С(О)-, или -С(O)-N(R3)-;
Alk3 обозначает низкомолекулярный алкилен;
R2 и R3 могут быть одинаковыми или различными и обозначают Н или низкомолекулярный алкил;
Rb обозначает атом галогена, низкомолекулярный алкил, который может быть замещенным приведенными ниже группами-заместителями, низкомолекулярный алкинил, низкомолекулярный галогеноалкил, гетерокольцо, гетерокольцо -О-, циано, нитро, низкомолекулярный галогеноалкил -О-, низкомолекулярную алкоксигруппу -О- низкомолекулярный алкилен -N-(R3)- низкомолекулярный алкилен -С(O)O-R6, Z2 - R6, или Z3 - R7, где замещающими группами для низкомолекулярного алкила являются следующие: ОН, циано, низкомолекулярная алкоксигруппа или аминогруппа, которая может быть замещенной низкомолекулярным алкилом;
Z2 -S(O)q-, -N(R3)-, -С(О)-, -С(O)-N(R3)-, -N(R3)-C(О)-, -С(O)-S(O)q-, -N-(R3)-S(O)q-, или -С(О)О-;
Z3 -N(R3) или -N(R3)-C(O)-;
R6 Н, низкомолекулярный алкил или арил;
R7 ОН или низкомолекулярная алкоксигруппа;
p равно 0 или 1;
q равно 0, 1, или 2;
Rc обозначает низкомолекулярный алкил или атом галогена;
Rd и Re могут быть одинаковыми или различными и обозначают Н, атом галогена, низкомолекулярный алкил, низкомолекулярную алкоксигруппу, ОН, галогеноалкил, фенил, низкомолекулярный галогеноалкил-O-, или
-N(R8)-C(О)-R9;
R8 и R9 могут быть одинаковыми или различными и обозначают Н или низкомолекулярный алкил;
Rf обозначает группы, выраженные Rb, оксогруппы, или арил, в котором Rd обозначает группу, отличную от Н, в случае, если кружок В' представляет собой бензол, когда кружок А' обозначает бензол, замещенный низкомолекулярной алкоксигруппой.
4. Производные триазола выраженные приведенной ниже общей формулой (1b), и их соли
где символы в формуле принимают следующие значения:
Ra, Re, и p соответствуют определениям, приведенным для соединения формулы (1а), описанного в п.3;
Rb' обозначает атом галогена, низкомолекулярный алкил, который может быть замещенным указанными ниже группами-заместителями, низкомолекулярный галогеноалкил, гетерокольцо, гетерокольцо-O-, циано, нитро, низкомолекулярный галогеноалкил -О-, низкомолекулярную алкоксигруппу, -О- низкомолекулярный алкилен -N(R3)- низкомолекулярный алкилен -С(O)O-R6, -N(R3)-R7, Z2 - R6, или Z3 - R7, где замещающими группами для низкомолекулярного алкила являются следующие: ОН, циано, низкомолекулярная алкоксигруппа, или аминогруппа, которая может быть замещенной низкомолекулярным алкилом;
R, Z3, R6, R7 и q соответствуют определениям, приведенным для соединения формулы (1а), описанного в п.3;
Rd' обозначает Н, низкомолекулярную алкоксигруппу, ОН, или низкомолекулярный алкил,
Re' обозначает Н, атом галогена, низкомолекулярную алкоксигруппу, низкомолекулярный галогеноалкил, низкомолекулярный галогеноалкил-O-, или -N(R8)C(О)-R9;
R8 и R9 обозначают те же группы, которые определены для соединения (1а), описанного в п.3;
где
(1) если Ra обозначает низкомолекулярный алкил, р=0, и Rb' представляет собой низкомолекулярный алкил, низкомолекулярную алкоксигруппу, либо атом галогена, по крайней мере одно из Rd' и Re' обозначает группу, отличную от Н, и Rd' обозначает группу, отличную от низкомолекулярного алкила в случае, когда Re' представляет собой Н,
(2) если Ra обозначает α-стирил, Rd' и Re' обозначают Н, и р=0, Rb' представляет собой группу, отличную от низкомолекулярного алкила и низкомолекулярной алкоксигруппы, и
(3) если Ra обозначает 2-фурил, Rd' и Re' обозначают Н, и р=0, то Rb' представляет собой группу, отличную от низкомолекулярного алкила.
5. Производные триазола по п.3 или их соли, в которых производные триазола, выраженные общей формулой (1а), содержат: азотсодержащее моноциклическое гетерокольцо в качестве кружка В', бензольное кольцо в качестве кружка D', и атом галогена, низкомолекулярный алкил, низкомолекулярную алкоксигруппу, арил, циано, карбамоил или оксогруппу, в качестве Rf.
6. Следующие соединения и их соли: 5-[4-(2,6-дифторфенил)-5-изопропил-4H-1,2,4-триазол-3-ил]-2-фенилпиридин; 4-[3-изопропил-5-(6-фенилпиридин-3-ил)-4H-1,2,4-триазол-4-ил]-2,1,3-бензоксадиазол; 3-[3-(3-метоксипропил)-5-(6-фенилпиридин-3-ил)-4Н-1,2,4-триазол-4-ил]-2 метилбензонитрил; 3-[3-этил-5-(6-фенилпиридин-3-ил)-4Н-1,2,4-триазол-4-ил]-2-метилбензонитрил; 2-{3-[N-(2-метоксиэтил)-N-метиламино]-5-(6-фенилпиридин-3-ил)-4H-1,2,4-триазол-4-ил}бензонитрил; и 4-(2,1,3-бензоксадиазол-4-ил)-N-(2-метоксиэтил)-N-метил-5-(6-фенилпиридин-3-ил)-4Н-1,2,4-триазол-3-ил-амин.
7. Фармацевтические композиции, которые включают производные триазола, описанные в п.3 или 4, в качестве действующего вещества.
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3808283A1 (de) * | 1988-03-12 | 1989-09-21 | Boehringer Ingelheim Kg | Neue 3,4,5-substituierte 4h-1,2,4-triazole, ihre herstellung und verwendung |
DE4302051A1 (de) * | 1993-01-26 | 1994-07-28 | Thomae Gmbh Dr K | 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
GB9605027D0 (en) * | 1996-03-09 | 1996-05-08 | Pfizer Ltd | Quinoxalinediones |
AP982A (en) * | 1997-02-27 | 2001-07-16 | Pfizer | Quinoxalinediones. |
JP2000063363A (ja) * | 1998-08-12 | 2000-02-29 | Yamanouchi Pharmaceut Co Ltd | 新規なトリアゾール誘導体 |
AU2000223275A1 (en) | 2000-02-08 | 2001-08-20 | Yamanouchi Pharmaceutical Co..Ltd. | Novel triazole derivatives |
-
2001
- 2001-05-17 RU RU2002133666/04A patent/RU2002133666A/ru unknown
- 2001-05-17 EP EP01930192A patent/EP1293503A4/en not_active Withdrawn
- 2001-05-17 WO PCT/JP2001/004128 patent/WO2001087855A1/ja not_active Application Discontinuation
- 2001-05-17 SK SK1624-2002A patent/SK16242002A3/sk unknown
- 2001-05-17 MX MXPA02011373A patent/MXPA02011373A/es unknown
- 2001-05-17 BR BR0110961-8A patent/BR0110961A/pt not_active Application Discontinuation
- 2001-05-17 PL PL01359340A patent/PL359340A1/xx unknown
- 2001-05-17 KR KR1020027015529A patent/KR100776119B1/ko not_active IP Right Cessation
- 2001-05-17 CA CA002409819A patent/CA2409819C/en not_active Expired - Fee Related
- 2001-05-17 HU HU0302415A patent/HUP0302415A2/hu unknown
- 2001-05-17 CZ CZ20023763A patent/CZ20023763A3/cs unknown
- 2001-05-17 JP JP2001584251A patent/JP3873746B2/ja not_active Expired - Fee Related
- 2001-05-17 AU AU2001256769A patent/AU2001256769A1/en not_active Abandoned
- 2001-05-17 CN CNB018096166A patent/CN1237055C/zh not_active Expired - Fee Related
- 2001-05-18 AR ARP010102360A patent/AR030933A1/es unknown
-
2002
- 2002-11-18 NO NO20025517A patent/NO20025517D0/no not_active Application Discontinuation
-
2005
- 2005-09-22 US US11/232,011 patent/US7084164B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
AU2001256769A1 (en) | 2001-11-26 |
NO20025517L (no) | 2002-11-18 |
BR0110961A (pt) | 2004-06-29 |
CA2409819C (en) | 2009-09-15 |
US7084164B2 (en) | 2006-08-01 |
EP1293503A1 (en) | 2003-03-19 |
KR100776119B1 (ko) | 2007-11-16 |
CN1237055C (zh) | 2006-01-18 |
PL359340A1 (en) | 2004-08-23 |
MXPA02011373A (es) | 2003-06-26 |
AR030933A1 (es) | 2003-09-03 |
NO20025517D0 (no) | 2002-11-18 |
US20060025461A1 (en) | 2006-02-02 |
KR20030019386A (ko) | 2003-03-06 |
SK16242002A3 (sk) | 2003-04-01 |
CZ20023763A3 (cs) | 2003-03-12 |
CA2409819A1 (en) | 2002-11-18 |
CN1429215A (zh) | 2003-07-09 |
JP3873746B2 (ja) | 2007-01-24 |
WO2001087855A1 (fr) | 2001-11-22 |
EP1293503A4 (en) | 2008-04-02 |
HUP0302415A2 (hu) | 2003-11-28 |
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