RU2427573C2 - Новые производные бензимидазола в качестве ингибиторов ваниллоидного рецептора 1 (vr1) - Google Patents
Новые производные бензимидазола в качестве ингибиторов ваниллоидного рецептора 1 (vr1) Download PDFInfo
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- RU2427573C2 RU2427573C2 RU2008122404/04A RU2008122404A RU2427573C2 RU 2427573 C2 RU2427573 C2 RU 2427573C2 RU 2008122404/04 A RU2008122404/04 A RU 2008122404/04A RU 2008122404 A RU2008122404 A RU 2008122404A RU 2427573 C2 RU2427573 C2 RU 2427573C2
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- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
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Abstract
Настоящее изобретение относится к соединению, выбранному из N-((1S)-1-{4-[2-фтор-1-(фторметил)этокси]фенил}этил)-2-(7-нитро-1Н-бензимидазол-1-ил)ацетамида, 2-(7-нитро-1Н-бензимидазол-1-ил)-N-{1-[6-(2,2,3,3-тетрафторпропокси)пиридин-3-ил]этил}ацетамида, N-[1-(4-тpeт-бутилфенил)этил]-2-(6,7-дифтор-1H-бензимидазол-1-ил)ацетамида и N-[(1S)-1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамида. Также изобретение относится к применению указанных соединений в изготовлении лекарственного средства. Технический результат: получены новые соединения, полезные для лечения расстройств, опосредованных VR1 (ваниллоидный рецептор 1), и/или для лечения острых и хронических болевых расстройств. 2 н. и 4 з.п. ф-лы, 5 табл.
Description
Claims (6)
1. Соединение, выбранное из:
N-((1S)-1-{4-[2-фтор-1-(фторметил)этокси]фенил}этил)-2-(7-нитро-1Н-бензимидазол-1-ил)ацетамида,
2-(7-нитро-1Н-бензимидазол-1-ил)-N-{1-[6-(2,2,3,3-тетрафторпропокси)пиридин-3-ил]этил}ацетамида,
N-[1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамида и
N-[(1S)-1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамида.
N-((1S)-1-{4-[2-фтор-1-(фторметил)этокси]фенил}этил)-2-(7-нитро-1Н-бензимидазол-1-ил)ацетамида,
2-(7-нитро-1Н-бензимидазол-1-ил)-N-{1-[6-(2,2,3,3-тетрафторпропокси)пиридин-3-ил]этил}ацетамида,
N-[1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамида и
N-[(1S)-1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамида.
2. Соединение по п.1, представляющее собой N-[1-(4-трет-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамид.
3. Соединение по п.1, представляющее собой N-[(1S)-1-(4-тpeт-бутилфенил)этил]-2-(6,7-дифтор-1Н-бензимидазол-1-ил)ацетамид.
4. Соединение по любому из пп.1-3 для ингибирования ваниллоидного рецептора 1 (VR1).
5. Соединение по любому из пп.1-3 для лечения острой и хронической боли.
6. Применение соединений по любому из пп.1-3 в изготовлении лекарственного средства для лечения расстройств, опосредованных VR1 (ваниллоидный рецептор 1), и/или для лечения острых и хронических болевых расстройств, таких как острая или хроническая невропатическая боль, острая или хроническая ноцицептивная боль и острая или хроническая воспалительная боль; и/или респираторных заболеваний; артрита; остеоартрита; ревматоидного артрита; фибромиалгии; поясничной боли; послеоперационной боли; висцеральных болей, таких как хроническая боль в области таза; цистита; синдрома раздраженного кишечника (IBS); панкреатита; ишемии, ишиаса, диабетической невропатии, рассеянного склероза, интерстициального цистита и/или боли, связанной с интерстициальным циститом; невропатии при ВИЧ; астмы; кашля; и/или воспалительного кишечного заболевания (IBD); заболевания гастроэзофагеальный рефлюкс (GERD); боли и других признаков и симптомов, ассоциированных с псориазом; боли и других признаков и симптомов, ассоциированных с раком; ожирения; рвоты; энуреза; и/или гиперактивного мочевого пузыря, включая признаки и/или симптомы, относящиеся к указанным заболеваниям.
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US75360405P | 2005-12-23 | 2005-12-23 | |
US60/753,604 | 2005-12-23 |
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RU2008122404A RU2008122404A (ru) | 2010-01-27 |
RU2427573C2 true RU2427573C2 (ru) | 2011-08-27 |
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RU2008122404/04A RU2427573C2 (ru) | 2005-12-23 | 2006-12-21 | Новые производные бензимидазола в качестве ингибиторов ваниллоидного рецептора 1 (vr1) |
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US (2) | US7618993B2 (ru) |
EP (1) | EP1966156B1 (ru) |
JP (1) | JP2009521431A (ru) |
KR (1) | KR20080080212A (ru) |
CN (1) | CN101389610B (ru) |
AR (1) | AR058705A1 (ru) |
AT (1) | ATE538101T1 (ru) |
AU (1) | AU2006327320B2 (ru) |
BR (1) | BRPI0620410A2 (ru) |
CA (1) | CA2634804A1 (ru) |
EC (1) | ECSP088584A (ru) |
ES (1) | ES2377661T3 (ru) |
HK (1) | HK1121755A1 (ru) |
IL (1) | IL191753A0 (ru) |
NO (1) | NO20083246L (ru) |
NZ (1) | NZ569923A (ru) |
RU (1) | RU2427573C2 (ru) |
TW (1) | TW200736227A (ru) |
UA (1) | UA96277C2 (ru) |
UY (1) | UY30048A1 (ru) |
WO (1) | WO2007073303A2 (ru) |
ZA (1) | ZA200805162B (ru) |
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DE112011102008B4 (de) | 2010-06-15 | 2022-04-21 | Merck Patent Gmbh | Metallkomplexe |
KR101293384B1 (ko) | 2010-10-13 | 2013-08-05 | 주식회사 대웅제약 | 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도 |
AU2015329955A1 (en) * | 2014-10-08 | 2017-05-11 | Thomas Helledays Stiftelse For Medicinsk Forskning | Heterocyclic compounds as DCTPP1 modulators |
JO3719B1 (ar) | 2014-11-20 | 2021-01-31 | Takeda Pharmaceuticals Co | 4- أوكسو-4،3- داي هيدرو-3،2،1- بنزوترايازينات كمواد ضابطة لأجل gpr139 |
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WO2004024710A1 (en) | 2002-09-13 | 2004-03-25 | Glaxo Group Limited | Urea compounds active as vanilloid receptor antagonists for the treatment of pain |
EP1551811A1 (en) | 2002-10-17 | 2005-07-13 | Amgen Inc. | Benzimidazole derivatives and their use as vanilloid receptor ligands |
SE0301446D0 (sv) | 2003-05-16 | 2003-05-16 | Astrazeneca Ab | New Compounds |
SE0301701D0 (sv) | 2003-06-10 | 2003-06-10 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
BRPI0414105B8 (pt) * | 2003-09-03 | 2021-05-25 | Askat Inc | compostos de benzimidazolona com atividade agonista do receptor 5-ht4 |
WO2005095327A1 (ja) | 2004-03-31 | 2005-10-13 | Ajinomoto Co., Inc. | アニリン誘導体 |
SE0402284D0 (sv) * | 2004-09-21 | 2004-09-21 | Astrazeneca Ab | New heterocyclic amides |
AR058705A1 (es) * | 2005-12-23 | 2008-02-20 | Astrazeneca Ab | Compuestos de bencimidazol como inhibidores del receptor vaniloide 1 (vr1) |
CN101479249B (zh) * | 2006-06-29 | 2012-10-10 | 霍夫曼-拉罗奇有限公司 | 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂 |
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- 2006-12-21 US US11/614,346 patent/US7618993B2/en active Active
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Also Published As
Publication number | Publication date |
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ECSP088584A (es) | 2008-07-30 |
CA2634804A1 (en) | 2007-06-28 |
UY30048A1 (es) | 2007-07-31 |
AU2006327320A1 (en) | 2007-06-28 |
CN101389610A (zh) | 2009-03-18 |
EP1966156A2 (en) | 2008-09-10 |
NO20083246L (no) | 2008-09-11 |
UA96277C2 (en) | 2011-10-25 |
RU2008122404A (ru) | 2010-01-27 |
IL191753A0 (en) | 2008-12-29 |
US20080171770A1 (en) | 2008-07-17 |
US20100286202A1 (en) | 2010-11-11 |
WO2007073303A3 (en) | 2007-08-30 |
HK1121755A1 (en) | 2009-04-30 |
CN101389610B (zh) | 2011-12-07 |
EP1966156B1 (en) | 2011-12-21 |
KR20080080212A (ko) | 2008-09-02 |
AR058705A1 (es) | 2008-02-20 |
US7618993B2 (en) | 2009-11-17 |
US8168668B2 (en) | 2012-05-01 |
ZA200805162B (en) | 2009-11-25 |
TW200736227A (en) | 2007-10-01 |
AU2006327320B2 (en) | 2009-12-10 |
JP2009521431A (ja) | 2009-06-04 |
ATE538101T1 (de) | 2012-01-15 |
BRPI0620410A2 (pt) | 2011-11-08 |
WO2007073303A2 (en) | 2007-06-28 |
NZ569923A (en) | 2011-04-29 |
ES2377661T3 (es) | 2012-03-29 |
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