JP7126084B2 - Ｉｒｅ１小分子阻害薬 - Google Patents

Ｉｒｅ１小分子阻害薬 Download PDF

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Publication number
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
compound
alkyl
aminocyclohexyl
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JP2020522520A (ja
JP2020522520A5 (enExample
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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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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 Expired - Fee Related 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 Expired - Fee Related 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
JP7546299B2 (ja) 2018-12-03 2024-09-06 コーネル・ユニバーシティー Ｉｒｅ１小分子阻害物質
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.
TWI756636B (zh) * 2019-02-18 2022-03-01 美商建南德克公司 嘧啶并嘧啶化合物及使用方法
SG11202109194UA (en) * 2019-02-27 2021-09-29 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
US12479818B2 (en) 2019-05-15 2025-11-25 Cornell University Treatment of fibrosis with IRE1 small molecule inhibitors
EP3983400B1 (en) * 2019-06-11 2025-05-28 Genentech, Inc. Quinazolinyl compounds and methods of use
KR20220097438A (ko) * 2019-11-01 2022-07-07 얀센 바이오테크 인코포레이티드 암, 자가면역, 및 염증성 질환의 치료를 위한 다이하이드로오로테이트 데하이드로게나제(dhodh) 억제제로서의 플루오르화 퀴놀린 및 퀴녹살린 유도체
US20240262830A1 (en) * 2020-02-03 2024-08-08 Nimbus Iaso, Inc. Ire1a modulators and uses thereof
EP4107146A1 (en) * 2020-02-17 2022-12-28 Alesta Therapeutics BV Gcn2 modulator compounds
CA3188602A1 (en) * 2020-08-07 2022-02-10 Richard Keenan Pyrazolopyridine compounds and methods of inhibiting ire1 using same
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
PE20231311A1 (es) 2020-11-18 2023-08-24 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos
MX2024006627A (es) 2021-12-03 2024-08-22 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos.
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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EP1626056B1 (en) 1999-12-30 2012-03-28 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
WO2007101225A2 (en) 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Methods to identify inhibitors of the unfolded protein response
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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).
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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

Also Published As

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

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