WO2015056180A8 - Dérivés d'indoline utilisés comme inhibiteurs de perk - Google Patents

Dérivés d'indoline utilisés comme inhibiteurs de perk Download PDF

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Publication number
WO2015056180A8
WO2015056180A8 PCT/IB2014/065310 IB2014065310W WO2015056180A8 WO 2015056180 A8 WO2015056180 A8 WO 2015056180A8 IB 2014065310 W IB2014065310 W IB 2014065310W WO 2015056180 A8 WO2015056180 A8 WO 2015056180A8
Authority
WO
WIPO (PCT)
Prior art keywords
disease
compound
perk
directed
inhibitors
Prior art date
Application number
PCT/IB2014/065310
Other languages
English (en)
Other versions
WO2015056180A1 (fr
Inventor
Jesus Raul Medina
Adam Kenneth Charnley
Stuart Paul Romeril
Original Assignee
Glaxosmithkline Intellectual Property (No.2) Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Intellectual Property (No.2) Limited filed Critical Glaxosmithkline Intellectual Property (No.2) Limited
Publication of WO2015056180A1 publication Critical patent/WO2015056180A1/fr
Publication of WO2015056180A8 publication Critical patent/WO2015056180A8/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des dérivés substitués d'indoline. Spécifiquement, l'invention concerne des composés répondant à la Formule I : (I) dans laquelle R1, R2 et R3 sont définis dans la description. Les composés de l'invention sont des inhibiteurs de PERK et peuvent être utiles dans le traitement du cancer et de maladies associées à des voies de réponse de protéine dépliée activée, telles que la maladie d'Alzheimer, un accident vasculaire cérébral, le diabète de Type 1, la maladie de Parkinson, la maladie de Huntington, la sclérose latérale amyotrophique, un infarctus du myocarde, une maladie cardiovasculaire, l'athérosclérose et les arythmies, et plus spécifiquement les cancers du sein, du côlon, du pancréas et du poumon. Ainsi, l'invention concerne en outre des compositions pharmaceutiques comprenant un composé de l'invention. L'invention concerne en outre également des procédés d'inhibition de l'activité de PERK et le traitement de troubles associés à celle-ci au moyen d'un composé de l'invention ou d'une composition pharmaceutique comprenant un composé de l'invention.
PCT/IB2014/065310 2013-10-15 2014-10-14 Dérivés d'indoline utilisés comme inhibiteurs de perk WO2015056180A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361891019P 2013-10-15 2013-10-15
US61/891,019 2013-10-15

Publications (2)

Publication Number Publication Date
WO2015056180A1 WO2015056180A1 (fr) 2015-04-23
WO2015056180A8 true WO2015056180A8 (fr) 2015-12-03

Family

ID=51982658

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2014/065310 WO2015056180A1 (fr) 2013-10-15 2014-10-14 Dérivés d'indoline utilisés comme inhibiteurs de perk

Country Status (1)

Country Link
WO (1) WO2015056180A1 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US10918650B2 (en) 2016-06-02 2021-02-16 University Of South Florida Method of treating melanoma using an inhibitor of an atypical protein kinase C
WO2018164113A1 (fr) * 2017-03-06 2018-09-13 学校法人 慶應義塾 Modèle murin d'induction de la myopie et inhibiteur de stress du réticulum endoplasmique pour prévenir ou supprimer la myopie
CA3060564A1 (fr) 2017-04-18 2018-10-25 Eli Lilly And Company Composes de phenyl-2-hydroxy-acetylamino-2-methyl-phenyle
ES2935722T3 (es) 2017-07-28 2023-03-09 Novartis Ag Derivados de indol y usos de los mismos
EP3681883B1 (fr) 2017-09-13 2024-02-21 Novartis AG Dérivés de diphenyle et utilisations associées
CN107898793B (zh) * 2017-12-01 2019-12-24 温州医科大学 一种抑制近视的方法及制备药物的应用
EP3860578A1 (fr) 2018-10-01 2021-08-11 Institut National de la Santé et de la Recherche Médicale (INSERM) Utilisation d'inhibiteurs de formation de granules de stress pour cibler la régulation de réponses immunitaires
US20220348584A1 (en) * 2019-08-29 2022-11-03 Hibercell, Inc. Perk inhibiting indolinyl compounds
EP4051286A1 (fr) 2019-10-29 2022-09-07 Institut National de la Santé et de la Recherche Médicale (INSERM) Procédés et compositions pour le traitement d'un mélanome uvéal

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
SI1343782T1 (sl) 2000-12-21 2009-10-31 Smithkline Beecham Corp Pirimidinamini kot modulatorji angiogeneze
PL1761528T3 (pl) 2004-06-11 2008-05-30 Japan Tobacco Inc Pochodne 5-amino-2,4,7-triokso-3,4,7,8-tetrahydro-2H-pirydo[2,3-D]pirymidyny i związki pokrewne do leczenia raka
US7378423B2 (en) 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
WO2007026920A2 (fr) * 2005-09-02 2007-03-08 Astellas Pharma Inc. Nouveaux composes
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
UY33288A (es) * 2010-03-25 2011-10-31 Glaxosmithkline Llc Derivados de indolina inhibidores de la proteina quinasa r del reticulo endoplasmatico

Also Published As

Publication number Publication date
WO2015056180A1 (fr) 2015-04-23

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