RU2008152761A - Антагонисты vri ванилоидного рецептора на основе ионона - Google Patents

Антагонисты vri ванилоидного рецептора на основе ионона Download PDF

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RU2008152761A
RU2008152761A RU2008152761/04A RU2008152761A RU2008152761A RU 2008152761 A RU2008152761 A RU 2008152761A RU 2008152761/04 A RU2008152761/04 A RU 2008152761/04A RU 2008152761 A RU2008152761 A RU 2008152761A RU 2008152761 A RU2008152761 A RU 2008152761A
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Пьер Джовани БАРАЛДИ (IT)
Пьер Джовани БАРАЛДИ
Пьер Андреа БОРЕА (IT)
Пьер Андреа Бореа
Пьеранджело ДЖЕППЕТТИ (IT)
Пьеранджело Джеппетти
Мария Джованна ПАВАНИ (IT)
Мария Джованна Павани
Франческа ФРУТТАРОЛО (IT)
Франческа Фруттароло
Марчелло ТРЕВИЗАНИ (IT)
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    • C07C233/28—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated

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Abstract

1. Соединение формулы (I): ! ! где Y представляет собой группу формулы: ! ! в которой: ! R' выбирают из атомов водорода, галогена, гидрокси, (С1-С6)алкила, (С2-С6)алкенила, (С3-С6)алкинила, (С1-С6)алкокси, (С1-С6)алкиламино, фенила, нафтила, фенокси, нафтокси или фениламино, ароматические циклы которых необязательно замещены одним или более атомом галогена, гидрокси, (С1-С4)алкильной, (С1-С4)алкокси и трифторметильной группами; ! R представляет собой метил или атом водорода; ! n представляет собой 0 или 1; !X выбирают из фенила, пиридинила, нафтила, хинолинила и изохинолинила, необязательно замещенных одним или более группами, выбранными из атома галогена, гидрокси, (С1-С4)алкила, (С1-С4)алкокси и трифторметила; ! за исключением следующих соединений: ! ! 2. Соединение по п.1, где n равен 0 и Х представляет собой 5-изохинолинил. ! 3. Соединение по п.2, где R представляет собой атом водорода и Y представляет собой группу формулы: ! ! где R' соответствует вышеуказанному определению в п.1. ! 4. Соединение по п.3, где R' выбирают из группы, состоящей из атома водорода, метокси или фенокси, необязательно замещенных как указано в п.1. ! 5. Соединения по любому из пп.1-4 для применения в качестве лекарственного средства. ! 6. Фармацевтическая композиция, включающая соединение по любому из пп.1-4 в сочетании с одним или более носителем и/или эксципиентом. ! 7. Применение соединений по любому из пп.1-5 для приготовления анальгезирующих и/или противовоспалительных лекарственных средств.

Claims (7)

1. Соединение формулы (I):
Figure 00000001
где Y представляет собой группу формулы:
Figure 00000002
в которой:
R' выбирают из атомов водорода, галогена, гидрокси, (С1-С6)алкила, (С2-С6)алкенила, (С3-С6)алкинила, (С1-С6)алкокси, (С1-С6)алкиламино, фенила, нафтила, фенокси, нафтокси или фениламино, ароматические циклы которых необязательно замещены одним или более атомом галогена, гидрокси, (С1-С4)алкильной, (С1-С4)алкокси и трифторметильной группами;
R представляет собой метил или атом водорода;
n представляет собой 0 или 1;
X выбирают из фенила, пиридинила, нафтила, хинолинила и изохинолинила, необязательно замещенных одним или более группами, выбранными из атома галогена, гидрокси, (С1-С4)алкила, (С1-С4)алкокси и трифторметила;
за исключением следующих соединений:
Figure 00000003
2. Соединение по п.1, где n равен 0 и Х представляет собой 5-изохинолинил.
3. Соединение по п.2, где R представляет собой атом водорода и Y представляет собой группу формулы:
Figure 00000004
где R' соответствует вышеуказанному определению в п.1.
4. Соединение по п.3, где R' выбирают из группы, состоящей из атома водорода, метокси или фенокси, необязательно замещенных как указано в п.1.
5. Соединения по любому из пп.1-4 для применения в качестве лекарственного средства.
6. Фармацевтическая композиция, включающая соединение по любому из пп.1-4 в сочетании с одним или более носителем и/или эксципиентом.
7. Применение соединений по любому из пп.1-5 для приготовления анальгезирующих и/или противовоспалительных лекарственных средств.
RU2008152761/04A 2006-07-10 2007-07-02 Антагонисты vri ванилоидного рецептора на основе ионона RU2447064C2 (ru)

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EP1889830A1 (en) * 2006-07-10 2008-02-20 Pharmeste S.r.l. Biarylcarboxyarylamides as vanilloid-1 receptor modulators
NZ587771A (en) 2008-04-18 2011-05-27 Dae Woong Pharma Novel benzoxazine benzimidazole derivatives, pharmaceutical composition comprising same, and a use thereof
KR101293384B1 (ko) 2010-10-13 2013-08-05 주식회사 대웅제약 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도
US20130315843A1 (en) * 2012-05-25 2013-11-28 The Procter & Gamble Company Composition for reduction of trpa1 and trpv1 sensations
WO2018081189A1 (en) 2016-10-25 2018-05-03 The Procter & Gamble Company Fibrous structures
WO2018081191A1 (en) 2016-10-25 2018-05-03 The Procter & Gamble Company Differential pillow height fibrous structures
CN107522668B (zh) * 2017-08-24 2019-12-03 重庆医科大学 Trpv1拮抗剂及其制备方法和用途
CN107522669B (zh) * 2017-08-24 2019-12-03 重庆美莱德生物医药有限公司 瞬时受体电位香草酸亚型1拮抗剂及其制备方法和用途
RU2755206C1 (ru) 2020-05-20 2021-09-14 Федеральное государственное бюджетное учреждение науки Тихоокеанский институт биоорганической химии им. Г.Б. Елякова Дальневосточного отделения Российской академии наук (ТИБОХ ДВО РАН) Средство пролонгированного анальгетического действия и лекарственный препарат на его основе

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CA2468544A1 (en) * 2001-12-10 2003-06-19 Amgen Inc. Vanilloid receptor ligands
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