AU2018278311B2 - IRE1 small molecule inhibitors - Google Patents

IRE1 small molecule inhibitors Download PDF

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Publication number
AU2018278311B2
AU2018278311B2 AU2018278311A AU2018278311A AU2018278311B2 AU 2018278311 B2 AU2018278311 B2 AU 2018278311B2 AU 2018278311 A AU2018278311 A AU 2018278311A AU 2018278311 A AU2018278311 A AU 2018278311A AU 2018278311 B2 AU2018278311 B2 AU 2018278311B2
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AU
Australia
Prior art keywords
optionally substituted
amino
aminocyclohexyl
compound
chlorobenzenesulfonamide
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Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2018278311A
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English (en)
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AU2018278311A1 (en
Inventor
Sarah Bettigole
Dansu Li
Joseph P. Vacca
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Cornell University
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Cornell University
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Publication of AU2018278311A1 publication Critical patent/AU2018278311A1/en
Assigned to CORNELL UNIVERSITY reassignment CORNELL UNIVERSITY Request for Assignment Assignors: QUENTIS THERAPEUTICS, INC.
Application granted granted Critical
Publication of AU2018278311B2 publication Critical patent/AU2018278311B2/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/04Heterocyclic 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
    • 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
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • 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
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2018278311A 2017-06-01 2018-05-31 IRE1 small molecule inhibitors Ceased AU2018278311B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762513929P 2017-06-01 2017-06-01
US62/513,929 2017-06-01
PCT/US2018/035465 WO2018222918A1 (en) 2017-06-01 2018-05-31 Ire1 small molecule inhibitors

Publications (2)

Publication Number Publication Date
AU2018278311A1 AU2018278311A1 (en) 2019-12-12
AU2018278311B2 true AU2018278311B2 (en) 2021-10-07

Family

ID=64455585

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018278311A Ceased AU2018278311B2 (en) 2017-06-01 2018-05-31 IRE1 small molecule inhibitors

Country Status (6)

Country Link
US (3) US20180346446A1 (enExample)
EP (1) EP3630748B1 (enExample)
JP (1) JP7126084B2 (enExample)
AU (1) AU2018278311B2 (enExample)
CA (1) CA3064837A1 (enExample)
WO (1) WO2018222918A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11649224B2 (en) 2017-06-01 2023-05-16 Cornell University IRE1 small molecule inhibitors

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EP3548476A4 (en) 2016-12-02 2020-05-20 Quentis Therapeutics, Inc. SMALL MOLECULAR IRE1 INHIBITORS
JP7271538B2 (ja) * 2017-11-10 2023-05-11 コーネル・ユニバーシティー 低分子ire1阻害剤
TWI831829B (zh) 2018-09-12 2024-02-11 美商建南德克公司 苯氧基-吡啶基-嘧啶化合物及使用方法
EP3891137B1 (en) 2018-12-03 2024-10-09 Cornell University Ire1 small molecule inhibitors
WO2020142612A1 (en) * 2019-01-03 2020-07-09 Genentech, Inc. Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases.
AR118119A1 (es) * 2019-02-18 2021-09-22 Genentech Inc Compuestos de pirido-pirimidinilo y métodos de uso
EP3930718A4 (en) * 2019-02-27 2022-10-05 Optikira LLC Pyrazolopyridine compounds for ire1 inhibition
US20220194945A1 (en) * 2019-02-27 2022-06-23 Optikira, LLC Imidazolopyridine Compounds For IRE1 Inhibition
US20220265656A1 (en) * 2019-05-15 2022-08-25 Cornell University Combination therapies with ire1 small molecule inhibitors
WO2020232403A1 (en) * 2019-05-15 2020-11-19 Cornell University Treatment of fibrosis with ire1 small molecule inhibitors
JP7765972B2 (ja) * 2019-06-11 2025-11-07 ジェネンテック, インコーポレイテッド キナゾリニル化合物及び使用方法
MX2022005270A (es) * 2019-11-01 2022-06-09 Janssen Biotech Inc Derivados de quinolina y quinoxalina fluoradas como inhibidores de dihidroorotato deshidrogenasa (dhodh) para el tratamiento del cancer, enfermedades autoinmunes e inflamatorias.
WO2021158516A1 (en) * 2020-02-03 2021-08-12 Nimbus Iaso, Inc. IRE1α MODULATORS AND USES THEREOF
JP2023514328A (ja) * 2020-02-17 2023-04-05 アレスタ・セラピューティクス・ベスローテン・フェンノートシャップ Gcn2モジュレーター化合物
US20230331719A1 (en) * 2020-08-07 2023-10-19 Optikira, LLC Pyrazolopyridine Compounds and Methods of Inhibiting IRE1 Using Same
US11840523B2 (en) * 2020-11-13 2023-12-12 The Regents Of The University Of California IRE1α inhibitors and uses thereof
IL302807A (en) 2020-11-18 2023-07-01 Deciphera Pharmaceuticals Llc Gcn2 and perk kinase inhibitors and methods of use thereof
WO2024131893A1 (en) * 2022-12-22 2024-06-27 Shanghai Yi Zhong Xing Biotechnology Co., Ltd. IRE1α SMALL MOLECULE INHIBITORS

Citations (3)

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WO2011047384A2 (en) * 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
US20150158874A1 (en) * 2011-03-17 2015-06-11 Cmg Pharmaceutical Co., Ltd. Novel pyridopyrimidine derivatives and use thereof
US20150190466A1 (en) * 2013-12-20 2015-07-09 The Trustees Of Columbia University In The City Of New York Methods of treating metabolic disease

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US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
US7906522B2 (en) 2005-04-28 2011-03-15 Kyowa Hakko Kirin Co., Ltd 2-aminoquinazoline derivatives
US8017331B2 (en) * 2005-11-04 2011-09-13 Mannkind Corporation IRE-1α substrates
US8372861B2 (en) 2006-02-27 2013-02-12 The Board Of Trustees Of The Leland Stanford Junior University Inhibitors of the unfolded protein response and methods for their use
US8227184B2 (en) 2008-01-14 2012-07-24 President And Fellows Of Harvard College Methods for modulating de novo hepatic lipogenesis by modulating XBP-1 activity
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
MX2012011504A (es) * 2010-04-05 2013-01-18 Mannkind Corp Inhibidores de enzima 1 dependiente de inositol (ire-1 alfa).
US9956236B2 (en) 2011-02-07 2018-05-01 Cornell University Methods for increasing immune responses using agents that directly bind to and activate IRE-1
US20150018406A1 (en) 2012-03-09 2015-01-15 Cornell University Modulation of breast cancer growth by modulation of xbp1 activity
RU2015115631A (ru) 2012-09-26 2016-11-20 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Модулирование ire1
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EP3521431A1 (en) 2013-09-25 2019-08-07 Cornell University Compounds for inducing anti-tumor immunity and methods thereof
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EP3548476A4 (en) 2016-12-02 2020-05-20 Quentis Therapeutics, Inc. SMALL MOLECULAR IRE1 INHIBITORS
WO2018161033A1 (en) 2017-03-02 2018-09-07 Wright, Adrian Small molecule ire1-alpha inhibitors
AR111281A1 (es) 2017-03-17 2019-06-26 Genentech Inc Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1
JP7126084B2 (ja) 2017-06-01 2022-08-26 コーネル ユニバーシティー Ire1小分子阻害薬
JP7271538B2 (ja) * 2017-11-10 2023-05-11 コーネル・ユニバーシティー 低分子ire1阻害剤

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WO2011047384A2 (en) * 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
US20150158874A1 (en) * 2011-03-17 2015-06-11 Cmg Pharmaceutical Co., Ltd. Novel pyridopyrimidine derivatives and use thereof
US20150190466A1 (en) * 2013-12-20 2015-07-09 The Trustees Of Columbia University In The City Of New York Methods of treating metabolic disease

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11649224B2 (en) 2017-06-01 2023-05-16 Cornell University IRE1 small molecule inhibitors

Also Published As

Publication number Publication date
JP2020522520A (ja) 2020-07-30
JP7126084B2 (ja) 2022-08-26
EP3630748A1 (en) 2020-04-08
AU2018278311A1 (en) 2019-12-12
US20200157079A1 (en) 2020-05-21
WO2018222918A1 (en) 2018-12-06
US11649224B2 (en) 2023-05-16
CA3064837A1 (en) 2018-12-06
EP3630748B1 (en) 2023-04-19
EP3630748A4 (en) 2021-01-27
US20180346446A1 (en) 2018-12-06
US11021466B2 (en) 2021-06-01
US20210284628A1 (en) 2021-09-16

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Owner name: CORNELL UNIVERSITY

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