EA201391341A1 - Производные гетероциклических аминов - Google Patents

Производные гетероциклических аминов

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EA201391341A1
EA201391341A1 EA201391341A EA201391341A EA201391341A1 EA 201391341 A1 EA201391341 A1 EA 201391341A1 EA 201391341 A EA201391341 A EA 201391341A EA 201391341 A EA201391341 A EA 201391341A EA 201391341 A1 EA201391341 A1 EA 201391341A1
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Prior art keywords
halogen
lower alkyl
hydrogen
substituted
cycloalkyl
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EA201391341A
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English (en)
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EA023237B1 (ru
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Гуидо Галлей
Роджер Норкросс
Филипп Пфлигер
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Ф.Хоффманн-Ля Рош Аг
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Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA201391341A1 publication Critical patent/EA201391341A1/ru
Publication of EA023237B1 publication Critical patent/EA023237B1/ru

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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I)где Rпредставляет собой водород, низший алкил, галоген, низший алкил, замещенный галогеном, низший алкокси, низший алкокси, замещенный галогеном, циано, нитро, С-циклоалкил, -СН-С-циклоалкил, -О-СН-С-циклоалкил, -О-(СН)-О-низший алкил, S(O)CH, SF, -С(О)NH-низший алкил, фенил, -О-пиримидинил, возможно замещенный низшим алкокси, замещенным галогеном, или представляет собой бензил, оксетанил или фуранил; m представляет собой 1 или 2; Ar представляет собой арил или гетероарил, выбранный из группы, состоящей из фенила, нафтила, пиримидинила, пиридинила, бензотиазолила, хинолинила, хиназолинила, бензо[d][1.3]диоксолила, 5,6,7,8-тетрагидрохиназолинила, пиразолила, пиразинила, пиридазинила или 1,3,4-оксадиазолила; Y представляет собой связь, -СН-, -СНСН-, -CH(CF)- или -СН(СН)-; Rпредставляет собой водород или низший алкил; А представляет собой CR или N и R представляет собой водород, циано, галоген или низший алкил; R' представляет собой водород или галоген; при условии, что, когда R' представляет собой галоген, тогда А представляет собой СН; В представляет собой СН или N; n представляет собой 0, 1 или 2; X представляет собой связь, -СН- или -О-; или к их фармацевтическим активным кислотно-аддитивным солям. Установлено, что соединения формулы I обладают хорошим сродством к рецепторам, ассоциированным со следовыми аминами (TAARs), особенно к TAAR1. Соединения могут быть использованы для лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома дефицита внимания с гиперактивностью (СДВГ), расстройств, обусловленных стрессом, психотических расстройств, таких как шизофрения, неврологических заболеваний, таких как болезнь Паркинсона, нейродегенеративных расстройств, таких
EA201391341A 2011-03-24 2012-03-21 Производные гетероциклических аминов EA023237B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11159566 2011-03-24
PCT/EP2012/054939 WO2012126922A1 (en) 2011-03-24 2012-03-21 Heterocyclic amine derivatives

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EA201391341A1 true EA201391341A1 (ru) 2014-06-30
EA023237B1 EA023237B1 (ru) 2016-05-31

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US (1) US8802673B2 (ru)
EP (1) EP2688870B1 (ru)
JP (1) JP5716128B2 (ru)
KR (1) KR101518660B1 (ru)
CN (1) CN103443074B (ru)
AR (1) AR085478A1 (ru)
AU (1) AU2012230378B2 (ru)
BR (1) BR112013024312A2 (ru)
CA (1) CA2828283A1 (ru)
CL (1) CL2013002664A1 (ru)
CO (1) CO6801736A2 (ru)
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HK (1) HK1190703A1 (ru)
IL (1) IL228246A (ru)
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PE (1) PE20140425A1 (ru)
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ECSP13012896A (es) 2013-11-29
EP2688870B1 (en) 2017-02-01
JP2014508790A (ja) 2014-04-10
CL2013002664A1 (es) 2014-05-09
AU2012230378A1 (en) 2013-09-12
CN103443074B (zh) 2016-04-13
CR20130419A (es) 2013-10-09
JP5716128B2 (ja) 2015-05-13
BR112013024312A2 (pt) 2016-07-19
KR101518660B1 (ko) 2015-05-07
NZ616150A (en) 2014-09-26
SG193556A1 (en) 2013-11-29
AU2012230378B2 (en) 2016-09-15
PE20140425A1 (es) 2014-03-28
CN103443074A (zh) 2013-12-11
ZA201306757B (en) 2015-04-29
KR20130132656A (ko) 2013-12-04
MX351918B (es) 2017-11-03
CA2828283A1 (en) 2012-09-27
EP2688870A1 (en) 2014-01-29
MA35062B1 (fr) 2014-04-03
AR085478A1 (es) 2013-10-02
HK1190703A1 (zh) 2014-07-11
EA023237B1 (ru) 2016-05-31
UA113167C2 (xx) 2016-12-26
IL228246A (en) 2017-10-31
WO2012126922A1 (en) 2012-09-27
US8802673B2 (en) 2014-08-12
CO6801736A2 (es) 2013-11-29
US20120245172A1 (en) 2012-09-27

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