JP7126084B2 - Ｉｒｅ１小分子阻害薬 - Google Patents

Ｉｒｅ１小分子阻害薬 Download PDF

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JP7126084B2
JP7126084B2 JP2019566754A JP2019566754A JP7126084B2 JP 7126084 B2 JP7126084 B2 JP 7126084B2 JP 2019566754 A JP2019566754 A JP 2019566754A JP 2019566754 A JP2019566754 A JP 2019566754A JP 7126084 B2 JP7126084 B2 JP 7126084B2
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amino
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aminocyclohexyl
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JP2020522520A5 (enExample
JP2020522520A (ja
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ジョセフ ピー． ヴァッカ
タンスー リー
サラ ベッティゴール
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Cornell University
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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)
JP2019566754A 2017-06-01 2018-05-31 Ｉｒｅ１小分子阻害薬 Active JP7126084B2 (ja)

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 (3)

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JP2020522520A JP2020522520A (ja) 2020-07-30
JP2020522520A5 JP2020522520A5 (enExample) 2021-02-12
JP7126084B2 true JP7126084B2 (ja) 2022-08-26

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JP2019566754A Active JP7126084B2 (ja) 2017-06-01 2018-05-31 Ｉｒｅ１小分子阻害薬

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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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021502387A (ja) * 2017-11-10 2021-01-28 コーネル・ユニバーシティーＣｏｒｎｅｌｌ Ｕｎｉｖｅｒｓｉｔｙ 低分子ｉｒｅ１阻害剤
US11649224B2 (en) 2017-06-01 2023-05-16 Cornell University IRE1 small molecule inhibitors

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WO2018102751A1 (en) 2016-12-02 2018-06-07 Quentis Therapeutics, Inc. 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
US12071426B2 (en) 2018-12-03 2024-08-27 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.
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
SG11202109194UA (en) * 2019-02-27 2021-09-29 Optikira Llc Pyrazolopyridine compounds for ire1 inhibition
WO2020176761A1 (en) * 2019-02-27 2020-09-03 Optikira, LLC Imidazolopyrazine compounds for ire1 inhibition
WO2020232401A1 (en) * 2019-05-15 2020-11-19 Cornell University Combination therapies with ire1 small molecule inhibitors
US12479818B2 (en) 2019-05-15 2025-11-25 Cornell University Treatment of fibrosis with IRE1 small molecule inhibitors
CN114302877A (zh) * 2019-06-11 2022-04-08 基因泰克公司 喹唑啉基化合物及使用方法
BR112022007981A2 (pt) * 2019-11-01 2022-07-05 Janssen Biotech Inc Quinolina fluorada e derivados de quinoxalina como inibidores da di-hidro-orotato desidrogenase (dhodh) para o tratamento de câncer, doenças autoimunes e inflamatórias
WO2021158516A1 (en) * 2020-02-03 2021-08-12 Nimbus Iaso, Inc. IRE1α 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
EP4192462A4 (en) * 2020-08-07 2024-09-04 Optikira LLC PYRAZOLOPYRIDINE COMPOUNDS AND METHODS OF INHIBITING IRE1 USING THEM
CN116710429A (zh) * 2020-11-13 2023-09-05 加利福尼亚大学董事会 IRE1α抑制剂及其用途
JP2023549540A (ja) 2020-11-18 2023-11-27 デシフェラ・ファーマシューティカルズ，エルエルシー Ｇｃｎ２およびｐｅｒｋキナーゼ阻害剤およびその使用方法
WO2024131893A1 (en) * 2022-12-22 2024-06-27 Shanghai Yi Zhong Xing Biotechnology Co., Ltd. IRE1α SMALL MOLECULE INHIBITORS

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JP2008515812A (ja) 2004-10-01 2008-05-15 アムジエン・インコーポレーテツド アリール窒素含有二環式化合物およびそれのキナーゼ阻害薬としての使用
JP2009514526A (ja) 2005-11-04 2009-04-09 マンカインド コーポレ−ション ＩＲＥ−１α基質
WO2011047384A2 (en) 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
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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US6632608B2 (en) 1999-12-30 2003-10-14 President And Fellows Of Harvard College Methods and compositions relating to modulation of hepatocyte growth, plasma cell differentiation or T cell subset activity by modulation of XBP-1 activity
EP1878727A4 (en) 2005-04-28 2013-11-13 Kyowa Hakko Kirin Co Ltd 2-AMINOQUINAZOLINE DERIVATIVES
US20090291857A1 (en) 2006-02-27 2009-11-26 The Board Of Trustees Of The Leland Stanford Junior University Methods to identify inhibitors of the unfolded protein response
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
EP3799870A1 (en) * 2010-04-05 2021-04-07 Fosun Orinove Pharmatech, Inc. Ire-1a inhibitors
WO2012109238A2 (en) 2011-02-07 2012-08-16 President And Fellows Of Harvard College 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.
WO2014176348A1 (en) 2013-04-23 2014-10-30 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of the ire-1/xbp-1 pathway and methods of using thereof
WO2015048331A1 (en) 2013-09-25 2015-04-02 Cornell University Compounds for inducing anti-tumor immunity and methods thereof
AU2017228405A1 (en) 2016-03-03 2018-10-18 Cornell University Small molecule IRE1-alpha inhibitors
WO2018102751A1 (en) 2016-12-02 2018-06-07 Quentis Therapeutics, Inc. Ire1 small molecule 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
EP3630748B1 (en) 2017-06-01 2023-04-19 Cornell University Ire1 small molecule inhibitors
CN111566089B (zh) * 2017-11-10 2023-11-17 康奈尔大学 Ire1小分子抑制剂

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JP2009514526A (ja) 2005-11-04 2009-04-09 マンカインド コーポレ−ション ＩＲＥ−１α基質
WO2011047384A2 (en) 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
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 (8)

* 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
JP2021502387A (ja) * 2017-11-10 2021-01-28 コーネル・ユニバーシティーＣｏｒｎｅｌｌ Ｕｎｉｖｅｒｓｉｔｙ 低分子ｉｒｅ１阻害剤
US11634403B2 (en) 2017-11-10 2023-04-25 Cornell University IRE1 small molecule 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
JP2023100744A (ja) * 2017-11-10 2023-07-19 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤
JP7535335B2 (ja) 2017-11-10 2024-08-16 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤
US12071424B2 (en) 2017-11-10 2024-08-27 Cornell University IRE1 small molecule inhibitors
JP2024156774A (ja) * 2017-11-10 2024-11-06 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤

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US20210284628A1 (en) 2021-09-16
CA3064837A1 (en) 2018-12-06
EP3630748A4 (en) 2021-01-27
US20180346446A1 (en) 2018-12-06
US11649224B2 (en) 2023-05-16
US11021466B2 (en) 2021-06-01
EP3630748A1 (en) 2020-04-08
WO2018222918A1 (en) 2018-12-06
AU2018278311B2 (en) 2021-10-07
EP3630748B1 (en) 2023-04-19
JP2020522520A (ja) 2020-07-30
AU2018278311A1 (en) 2019-12-12
US20200157079A1 (en) 2020-05-21

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