MX2015014025A - Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk. - Google Patents

Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk.

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Publication number
MX2015014025A
MX2015014025A MX2015014025A MX2015014025A MX2015014025A MX 2015014025 A MX2015014025 A MX 2015014025A MX 2015014025 A MX2015014025 A MX 2015014025A MX 2015014025 A MX2015014025 A MX 2015014025A MX 2015014025 A MX2015014025 A MX 2015014025A
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MX
Mexico
Prior art keywords
dihydro
quinazolinamine
pyrrolo
derivatives
jpyrid
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MX2015014025A
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English (en)
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MX367772B (es
Inventor
Yannick Aimé Eddy Ligny
Ian Stansfield
Nathalie Claudie Isabelle Amblard
Matthias Luc Aimé Versele
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of MX2015014025A publication Critical patent/MX2015014025A/es
Publication of MX367772B publication Critical patent/MX367772B/es

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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
    • 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
    • A61K31/407Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
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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
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

La presente invención se refiere a derivados de N-(2,3-dihidro-1H-pirrolo[2,3-b]piridin-5-iI)-4-quinazolinamina y N(2,3-dihidro-1H-indol-5-il)-4-quinazolinamina de Fórmula (I) (ver Fórmula) donde R1, R2, R3, R4, R5, R6 y A tienen el significado definido en las reivindicaciones. Los compuestos de acuerdo con la presente invención son útiles como inhibidores de PERK; la invención se refiere además a procesos para preparar tales compuestos, a composiciones farmacéuticas que comprenden dichos compuestos como principio activo, así como también al uso de dichos compuestos como un medicamento.
MX2015014025A 2013-04-04 2014-03-31 Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk. MX367772B (es)

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)

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MX2015014025A true MX2015014025A (es) 2016-02-10
MX367772B MX367772B (es) 2019-09-05

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MX2015014025A MX367772B (es) 2013-04-04 2014-03-31 Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk.

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

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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
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
US10561660B2 (en) 2016-06-21 2020-02-18 Nerviano Medical Sciences S.R.L. N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors
TW201838981A (zh) 2017-03-17 2018-11-01 美商建南德克公司 嘧啶基-吡啶氧基-萘基化合物以及治療ire1相關之疾病及病症的方法
WO2019067543A1 (en) * 2017-09-26 2019-04-04 The Regents Of The University Of California COMPOSITIONS AND METHODS OF TREATING CANCER
US20220040183A1 (en) 2018-10-01 2022-02-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of inhibitors of stress granule formation for targeting the regulation of immune responses
WO2021083959A1 (en) 2019-10-29 2021-05-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treating uveal melanoma

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GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
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CN105102450A (zh) 2015-11-25
JP2016517845A (ja) 2016-06-20
CN105102450B (zh) 2018-03-09
EA201591904A1 (ru) 2016-02-29
IL241808B (en) 2018-04-30
MX367772B (es) 2019-09-05
ES2638317T3 (es) 2017-10-19
AU2014247215B2 (en) 2018-05-10
WO2014161808A1 (en) 2014-10-09
JP6268276B2 (ja) 2018-01-24
US20160039798A1 (en) 2016-02-11
CA2901267A1 (en) 2014-10-09
KR20150138847A (ko) 2015-12-10
US9688662B2 (en) 2017-06-27
EP2989091A1 (en) 2016-03-02
KR102274755B1 (ko) 2021-07-08
HK1215026A1 (zh) 2016-08-12
CA2901267C (en) 2021-01-19
AU2014247215A1 (en) 2015-09-03
EP2989091B1 (en) 2017-05-10
EA027811B1 (ru) 2017-09-29
BR112015024971B1 (pt) 2022-09-20
BR112015024971A2 (pt) 2017-07-18

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