BR112015024971A2 - derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1h-indol-5-il)-4-quinazolinamina como inibidores de perk - Google Patents

derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1h-indol-5-il)-4-quinazolinamina como inibidores de perk

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Publication number
BR112015024971A2
BR112015024971A2 BR112015024971A BR112015024971A BR112015024971A2 BR 112015024971 A2 BR112015024971 A2 BR 112015024971A2 BR 112015024971 A BR112015024971 A BR 112015024971A BR 112015024971 A BR112015024971 A BR 112015024971A BR 112015024971 A2 BR112015024971 A2 BR 112015024971A2
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Brazil
Prior art keywords
quinazolinamine
dihydro
pyrrolo
indol
pyridin
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BR112015024971A
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English (en)
Other versions
BR112015024971B1 (pt
Inventor
Stansfield Ian
Luc Aimé Versele Matthias
Claudie Isabelle Amblard Nathalie
Aimé Eddy Ligny Yannick
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Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112015024971A2 publication Critical patent/BR112015024971A2/pt
Publication of BR112015024971B1 publication Critical patent/BR112015024971B1/pt

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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/407Heterocyclic 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Abstract

resumo patente de invenção: "derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1h-indol-5-il)-4-quinazolinamina como inibidores de perk". a presente invenção se relaciona com derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1h-indol-5-il)-4-quinazolinamina da fórmula (i) em que r1, r2, r3, r4, r5, r6 e a têm o significado definido nas reivindicações. os compostos de acordo com a presente invenção são úteis como inibidores de perk. a invenção se relaciona adicionalmente com processos para preparação de tais compostos, composições farmacêuticas compreendendo os referidos compostos como um ingrediente ativo bem como o uso dos referidos compostos como um medicamento.
BR112015024971-0A 2013-04-04 2014-03-31 Derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1hindol-5-il)-4-quinazolinamina como inibidores de perk e composição farmacêutica que os compreende BR112015024971B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13162362.1 2013-04-04
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
BR112015024971A2 true BR112015024971A2 (pt) 2017-07-18
BR112015024971B1 BR112015024971B1 (pt) 2022-09-20

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BR112015024971-0A BR112015024971B1 (pt) 2013-04-04 2014-03-31 Derivados de n-(2,3-di-hidro-1h-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina e n-(2,3-di-hidro-1hindol-5-il)-4-quinazolinamina como inibidores de perk e composição farmacêutica que os compreende

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

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CN104530063B (zh) * 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
AU2016261223A1 (en) * 2015-05-08 2018-01-04 Oklahoma Medical Research Foundation Nitrofuran derivatives that induce apoptosis in breast cancer cells by activating protein expression
WO2017189837A1 (en) 2016-04-29 2017-11-02 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
RU2753520C2 (ru) 2016-06-21 2021-08-17 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Производные n-(замещенный фенил)-сульфонамида в качестве ингибиторов киназы
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US20240122938A1 (en) 2019-10-29 2024-04-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treating uveal melanoma

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JP6268276B2 (ja) 2018-01-24
ES2638317T3 (es) 2017-10-19
IL241808B (en) 2018-04-30
US9688662B2 (en) 2017-06-27
CN105102450B (zh) 2018-03-09
US20160039798A1 (en) 2016-02-11
EP2989091B1 (en) 2017-05-10
EP2989091A1 (en) 2016-03-02
KR102274755B1 (ko) 2021-07-08
EA027811B1 (ru) 2017-09-29
EA201591904A1 (ru) 2016-02-29
AU2014247215B2 (en) 2018-05-10
BR112015024971B1 (pt) 2022-09-20
KR20150138847A (ko) 2015-12-10
CN105102450A (zh) 2015-11-25
WO2014161808A1 (en) 2014-10-09
CA2901267A1 (en) 2014-10-09
HK1215026A1 (zh) 2016-08-12
CA2901267C (en) 2021-01-19
MX367772B (es) 2019-09-05
JP2016517845A (ja) 2016-06-20
AU2014247215A1 (en) 2015-09-03
MX2015014025A (es) 2016-02-10

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