EA201391094A1 - Антагонисты рецепторов trpm8 - Google Patents

Антагонисты рецепторов trpm8

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Publication number
EA201391094A1
EA201391094A1 EA201391094A EA201391094A EA201391094A1 EA 201391094 A1 EA201391094 A1 EA 201391094A1 EA 201391094 A EA201391094 A EA 201391094A EA 201391094 A EA201391094 A EA 201391094A EA 201391094 A1 EA201391094 A1 EA 201391094A1
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Eurasian Patent Office
Prior art keywords
6alkyl
branched
substituted
linear
unsubstituted
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EA201391094A
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English (en)
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EA022943B1 (ru
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Алессио Морикони
Джанлука Бьянкини
Лаура Брандолини
Андреа Арамини
Кьяра Либерати
Сильвия Боволента
Андреа Беккари
Симоне Лоренци
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Домпе' С.П.А.
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Publication of EA201391094A1 publication Critical patent/EA201391094A1/ru
Publication of EA022943B1 publication Critical patent/EA022943B1/ru

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    • C07D213/04Heterocyclic 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
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Abstract

Соединения, действующие в качестве селективных антагонистов катионного канала транзиторного рецепторного потенциала, подсемейство М, член 8 (здесь и далее обозначен как TRPM8), имеющие формулу (I), где R выбран из Н, Br, CN, NO, SONH, SONHR' и SONR', где R' выбран из линейного или разветвленного С-Салкила; X выбран из F, Cl, C-Cалкила, NHи ОН; Y выбран из О, СН, NH и SO; R1 и R2, независимо друг от друга, выбраны из Н, F и линейного или разветвленного C-Салкила; R3 и R4, независимо друг от друга, выбраны из Н и линейного или разветвленного С-Салкила; Z выбран из NR6 и R6R7N, где R6 и R7, независимо друг от друга, выбраны из Н и линейного или разветвленного С-Салкила; R5 обозначает остаток, выбранный из Н и линейного или разветвленного С-Салкила; Het обозначает гетероарильную группу, выбранную из замещенного или незамещенного пирролила, замещенного или незамещенного N-метилпирролила, замещенного или незамещенного тиофенила, замещенного или незамещенного фурила и замещенного или незамещенного пиридинила. Указанные соединения пригодны для предупреждения и лечения патологий, зависящих от активности TRPM8, таких как боль, воспаление, ишемия, нейродегенерация, инсульт, психиатрические расстройства, воспалительные состояния и урологические расстройства.
EA201391094A 2011-01-28 2012-01-27 Антагонисты рецепторов trpm8 EA022943B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11425021A EP2481727A1 (en) 2011-01-28 2011-01-28 TRPM8 receptor antagonists
PCT/EP2012/051292 WO2012101244A1 (en) 2011-01-28 2012-01-27 Trpm8 receptor antagonists

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EA201391094A1 true EA201391094A1 (ru) 2014-01-30
EA022943B1 EA022943B1 (ru) 2016-03-31

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US (1) US8906946B2 (ru)
EP (2) EP2481727A1 (ru)
JP (1) JP6043298B2 (ru)
KR (1) KR101872553B1 (ru)
CN (1) CN103443077B (ru)
AU (1) AU2012210472B2 (ru)
CY (1) CY1116896T1 (ru)
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SI (1) SI2668160T1 (ru)
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MY182666A (en) 2010-11-05 2021-01-28 Senomyx Inc Compounds useful as modulators of trpm8
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WO2023217989A1 (en) 2022-05-12 2023-11-16 Syngenta Crop Protection Ag Alkoxy heteroaryl- carboxamide or thioamide compounds
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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WO2012101244A1 (en) 2012-08-02
AU2012210472B2 (en) 2016-06-23
SI2668160T1 (sl) 2016-01-29
EP2668160B1 (en) 2015-08-12
JP2014512336A (ja) 2014-05-22
AU2012210472A1 (en) 2013-08-15
EP2481727A1 (en) 2012-08-01
ES2552533T3 (es) 2015-11-30
DK2668160T3 (en) 2015-11-23
RS54337B1 (en) 2016-02-29
US8906946B2 (en) 2014-12-09
PT2668160E (pt) 2015-11-24
PL2668160T3 (pl) 2016-01-29
JP6043298B2 (ja) 2016-12-14
SMT201500296B (it) 2016-01-08
US20140031398A1 (en) 2014-01-30
KR20140019336A (ko) 2014-02-14
EP2668160A1 (en) 2013-12-04
ZA201305576B (en) 2014-10-29
ME02290B (me) 2016-02-20
EA022943B1 (ru) 2016-03-31
CN103443077A (zh) 2013-12-11
HRP20151163T1 (hr) 2015-12-04
HUE026587T2 (hu) 2016-06-28
CN103443077B (zh) 2016-05-18
KR101872553B1 (ko) 2018-06-28
HK1192228A1 (zh) 2014-08-15
CY1116896T1 (el) 2017-04-05

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