EA201591904A1 - НОВЫЕ ПРОИЗВОДНЫЕ N-(2,3-ДИГИДРО-1H-ПИРРОЛО[2,3-b]ПИРИДИН-5-ИЛ)-4-ХИНАЗОЛИНАМИНА И N-(2,3-ДИГИДРО-1H-ИНДОЛ-5-ИЛ)-4-ХИНАЗОЛИНАМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PERK - Google Patents

НОВЫЕ ПРОИЗВОДНЫЕ N-(2,3-ДИГИДРО-1H-ПИРРОЛО[2,3-b]ПИРИДИН-5-ИЛ)-4-ХИНАЗОЛИНАМИНА И N-(2,3-ДИГИДРО-1H-ИНДОЛ-5-ИЛ)-4-ХИНАЗОЛИНАМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PERK

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EA201591904A1
EA201591904A1 EA201591904A EA201591904A EA201591904A1 EA 201591904 A1 EA201591904 A1 EA 201591904A1 EA 201591904 A EA201591904 A EA 201591904A EA 201591904 A EA201591904 A EA 201591904A EA 201591904 A1 EA201591904 A1 EA 201591904A1
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Prior art keywords
dihydro
hinazolinamina
indol
pyridin
pirrolo
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EA201591904A
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English (en)
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EA027811B1 (ru
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Ян Стэнсфилд
Янник Эме Эдди Линьи
Натали Клоди Изабелль Амблар
Маттиас Люк Эме Версель
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Янссен Фармацевтика Нв
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Publication of EA201591904A1 publication Critical patent/EA201591904A1/ru
Publication of EA027811B1 publication Critical patent/EA027811B1/ru

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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

Изобретение относится к производным N-(2,3-дигидро-1H-пирроло[2,3-b]пиридин-5-ил)-4-хиназолинамина и N-(2,3-дигидро-1H-индол-5-ил)-4-хиназолинамина формулы (I)где R, R, R, R, R, Rи А имеют значение, определенное в формуле изобретения. Соединения по настоящему изобретению применяются в качестве ингибиторов PERK. Настоящее изобретение также относится к способам получения таких соединений, фармацевтическим композициям, содержащим указанные соединения в качестве активного ингредиента, а также применению указанных соединений в качестве лекарственного средства.
EA201591904A 2013-04-04 2014-03-31 ПРОИЗВОДНЫЕ N-(2,3-ДИГИДРО-1H-ПИРРОЛО[2,3-b]ПИРИДИН-5-ИЛ)-4-ХИНАЗОЛИНАМИНА И N-(2,3-ДИГИДРО-1H-ИНДОЛ-5-ИЛ)-4-ХИНАЗОЛИНАМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PERK EA027811B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13162362 2013-04-04
PCT/EP2014/056430 WO2014161808A1 (en) 2013-04-04 2014-03-31 Novel n-(2,3-dihydro-1h-pyrrolo[2,3-b]jpyridin-5-yl)-4- quinazolinamine and n-(2,3-dihydro-1h-indol-5-yl)-4- quinazolinamine derivatives as perk inhibitors

Publications (2)

Publication Number Publication Date
EA201591904A1 true EA201591904A1 (ru) 2016-02-29
EA027811B1 EA027811B1 (ru) 2017-09-29

Family

ID=48040101

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EA201591904A EA027811B1 (ru) 2013-04-04 2014-03-31 ПРОИЗВОДНЫЕ N-(2,3-ДИГИДРО-1H-ПИРРОЛО[2,3-b]ПИРИДИН-5-ИЛ)-4-ХИНАЗОЛИНАМИНА И N-(2,3-ДИГИДРО-1H-ИНДОЛ-5-ИЛ)-4-ХИНАЗОЛИНАМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PERK

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US (1) US9688662B2 (ru)
EP (1) EP2989091B1 (ru)
JP (1) JP6268276B2 (ru)
KR (1) KR102274755B1 (ru)
CN (1) CN105102450B (ru)
AU (1) AU2014247215B2 (ru)
BR (1) BR112015024971B1 (ru)
CA (1) CA2901267C (ru)
EA (1) EA027811B1 (ru)
ES (1) ES2638317T3 (ru)
HK (1) HK1215026A1 (ru)
IL (1) IL241808B (ru)
MX (1) MX367772B (ru)
WO (1) WO2014161808A1 (ru)

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US10968203B2 (en) 2017-03-17 2021-04-06 Genentech, Inc. Pyrimidinyl-pyridyloxy-naphthyl compounds and methods of treating IRE1-related diseases and disorders

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CA2989118A1 (en) * 2015-05-08 2016-11-17 Oklahoma Medical Research Foundation Nitrofuran derivatives that induce apoptosis in breast cancer cells by activating protein expression
US11026945B2 (en) 2016-04-29 2021-06-08 The Trustees Of The University Of Pennsylvania Protein kinase RNA-like endoplasmic reticulum kinase (PERK) inhibitors for prevention and/or treatment of lung injury and/or inflammation
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CA3081548A1 (en) * 2017-09-26 2019-04-04 The Regents Of The University Of California Compositions and methods for treating cancer
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EP4051286A1 (en) 2019-10-29 2022-09-07 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods and compositions for treating uveal melanoma

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Publication number Priority date Publication date Assignee Title
US10968203B2 (en) 2017-03-17 2021-04-06 Genentech, Inc. Pyrimidinyl-pyridyloxy-naphthyl compounds and methods of treating IRE1-related diseases and disorders

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KR20150138847A (ko) 2015-12-10
JP6268276B2 (ja) 2018-01-24
CA2901267C (en) 2021-01-19
CA2901267A1 (en) 2014-10-09
EA027811B1 (ru) 2017-09-29
US20160039798A1 (en) 2016-02-11
HK1215026A1 (zh) 2016-08-12
AU2014247215A1 (en) 2015-09-03
JP2016517845A (ja) 2016-06-20
BR112015024971A2 (pt) 2017-07-18
EP2989091A1 (en) 2016-03-02
BR112015024971B1 (pt) 2022-09-20
AU2014247215B2 (en) 2018-05-10
US9688662B2 (en) 2017-06-27
KR102274755B1 (ko) 2021-07-08
CN105102450A (zh) 2015-11-25
EP2989091B1 (en) 2017-05-10
WO2014161808A1 (en) 2014-10-09
MX367772B (es) 2019-09-05
CN105102450B (zh) 2018-03-09
MX2015014025A (es) 2016-02-10
ES2638317T3 (es) 2017-10-19
IL241808B (en) 2018-04-30

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