CA3064837A1 - Ire1 small molecule inhibitors - Google Patents

Ire1 small molecule inhibitors Download PDF

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Publication number
CA3064837A1
CA3064837A1 CA3064837A CA3064837A CA3064837A1 CA 3064837 A1 CA3064837 A1 CA 3064837A1 CA 3064837 A CA3064837 A CA 3064837A CA 3064837 A CA3064837 A CA 3064837A CA 3064837 A1 CA3064837 A1 CA 3064837A1
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CA
Canada
Prior art keywords
optionally substituted
compound
solvate
pharmaceutically acceptable
acceptable salt
Prior art date
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.)
Pending
Application number
CA3064837A
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English (en)
French (fr)
Inventor
Joseph P. Vacca
Dansu Li
Sarah Bettigole
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cornell University
Original Assignee
Quentis Therapeutics Inc
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 Quentis Therapeutics Inc filed Critical Quentis Therapeutics Inc
Publication of CA3064837A1 publication Critical patent/CA3064837A1/en
Pending legal-status Critical Current

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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CA3064837A 2017-06-01 2018-05-31 Ire1 small molecule inhibitors Pending CA3064837A1 (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 (1)

Publication Number Publication Date
CA3064837A1 true CA3064837A1 (en) 2018-12-06

Family

ID=64455585

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3064837A Pending CA3064837A1 (en) 2017-06-01 2018-05-31 Ire1 small molecule inhibitors

Country Status (6)

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

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EP3548476A4 (en) 2016-12-02 2020-05-20 Quentis Therapeutics, Inc. SMALL MOLECULAR IRE1 INHIBITORS
CA3064837A1 (en) 2017-06-01 2018-12-06 Quentis Therapeutics, Inc. Ire1 small molecule inhibitors
US10745379B2 (en) 2017-11-10 2020-08-18 Cornell University IRE1 small molecule inhibitors
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
JP7539892B2 (ja) * 2019-01-03 2024-08-26 ジェネンテック, インコーポレイテッド 癌疾患の処置のためのエンドリボヌクレアーゼのイノシトール要求酵素i(ireiアルファ)の阻害剤としてのピリド-ピリミジノン化合物及びプテリジノン化合物
CN113795307A (zh) * 2019-02-18 2021-12-14 基因泰克公司 吡啶并嘧啶基化合物及其使用方法
CN113795254B (zh) * 2019-02-27 2024-08-09 奥普提卡拉公司 用于ire1抑制的吡唑并吡啶化合物
US20220194945A1 (en) * 2019-02-27 2022-06-23 Optikira, LLC Imidazolopyridine Compounds For IRE1 Inhibition
WO2020232401A1 (en) * 2019-05-15 2020-11-19 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
WO2020252165A1 (en) * 2019-06-11 2020-12-17 Genentech, Inc. Quinazolinyl compounds and methods of use
JP2023500252A (ja) * 2019-11-01 2023-01-05 ヤンセン バイオテツク,インコーポレーテツド 癌、自己免疫疾患及び炎症性疾患の治療用のジヒドロオロト酸デヒドロゲナーゼ(dhodh)阻害剤としてのフッ素化キノリン及びキノキサリン誘導体
US20240262830A1 (en) * 2020-02-03 2024-08-08 Nimbus Iaso, Inc. Ire1a modulators and uses thereof
BR112022016072A2 (pt) * 2020-02-17 2022-10-04 Alesta Therapeutics BV Compostos moduladores de gcn2, sal farmaceuticamente aceitável, seus usos, e composição farmacêutica
CA3188602A1 (en) * 2020-08-07 2022-02-10 Richard Keenan 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
MX2023005747A (es) 2020-11-18 2023-07-28 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos.
KR20240113496A (ko) 2021-12-03 2024-07-22 데시페라 파마슈티칼스, 엘엘씨. Gcn2 및 perk 키나아제 억제제로서의 헤테로고리 화합물
WO2024131893A1 (en) * 2022-12-22 2024-06-27 Shanghai Yi Zhong Xing Biotechnology Co., Ltd. IRE1α SMALL MOLECULE INHIBITORS

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JP2003518942A (ja) 1999-12-30 2003-06-17 プレジデント・アンド・フェローズ・オブ・ハーバード・カレッジ 肝細胞成長、形質細胞分化、又はt細胞サブセットの活性を、xbp−1活性の変調により変調することに関する方法及び組成物
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
JP5079500B2 (ja) 2005-04-28 2012-11-21 協和発酵キリン株式会社 2−アミノキナゾリン誘導体
US8017331B2 (en) * 2005-11-04 2011-09-13 Mannkind Corporation IRE-1α substrates
AU2007220039A1 (en) 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Inhibitors of the unfolded protein response and methods for their use
WO2009091815A2 (en) 2008-01-14 2009-07-23 President And Fellows Of Harvard College Methods for modulating de novo hepatic lipogenesis by modulating xbp-1 activity
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
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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
US9422298B2 (en) * 2011-03-17 2016-08-23 Cmg Pharmaceutical Co., Ltd. Pyridopyrimidine derivatives and use thereof
US20150018406A1 (en) 2012-03-09 2015-01-15 Cornell University Modulation of breast cancer growth by modulation of xbp1 activity
MX2015003874A (es) 2012-09-26 2015-12-16 Univ California Modulacion de ire1.
US10323013B2 (en) 2013-04-23 2019-06-18 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of the IRE-1/XBP-1 pathway and methods of using thereof
DK3049521T3 (en) 2013-09-25 2019-04-23 Univ Cornell Compounds for inducing antitumor immunity and methods thereof
US9682123B2 (en) * 2013-12-20 2017-06-20 The Trustees Of Columbia University In The City Of New York Methods of treating metabolic disease
CA3016161A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
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
CA3064837A1 (en) 2017-06-01 2018-12-06 Quentis Therapeutics, Inc. Ire1 small molecule inhibitors
US10745379B2 (en) * 2017-11-10 2020-08-18 Cornell University IRE1 small molecule inhibitors

Also Published As

Publication number Publication date
WO2018222918A1 (en) 2018-12-06
JP2020522520A (ja) 2020-07-30
AU2018278311A1 (en) 2019-12-12
US20210284628A1 (en) 2021-09-16
JP7126084B2 (ja) 2022-08-26
US20200157079A1 (en) 2020-05-21
AU2018278311B2 (en) 2021-10-07
EP3630748B1 (en) 2023-04-19
EP3630748A1 (en) 2020-04-08
EP3630748A4 (en) 2021-01-27
US11021466B2 (en) 2021-06-01
US20180346446A1 (en) 2018-12-06
US11649224B2 (en) 2023-05-16

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