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 (https=
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)
  • 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)
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 (https=) 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 (https=)
EP (1) EP3630748B1 (https=)
JP (1) JP7126084B2 (https=)
AU (1) AU2018278311B2 (https=)
CA (1) CA3064837A1 (https=)
WO (1) WO2018222918A1 (https=)

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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EP3548476A4 (en) 2016-12-02 2020-05-20 Quentis Therapeutics, Inc. SMALL MOLECULAR IRE1 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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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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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
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
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
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
EP2555768B1 (en) * 2010-04-05 2018-08-29 Fosun Orinove Pharmatech, Inc. Ire-1 inhibitors
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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)

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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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WO2018222918A1 (en) 2018-12-06
JP2020522520A (ja) 2020-07-30
AU2018278311A1 (en) 2019-12-12
US20210284628A1 (en) 2021-09-16
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
CA3064837A1 (en) 2018-12-06

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