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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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.
AR118119A1 (es) * 2019-02-18 2021-09-22 Genentech Inc Compuestos de pirido-pirimidinilo y métodos de uso
US20220194945A1 (en) * 2019-02-27 2022-06-23 Optikira, LLC Imidazolopyridine Compounds For IRE1 Inhibition
BR112021016974A2 (pt) * 2019-02-27 2021-11-30 Optikira Llc Compostos de pirazolopiridina para inibição de ire1
WO2020232403A1 (en) * 2019-05-15 2020-11-19 Cornell University Treatment of fibrosis with ire1 small molecule inhibitors
WO2020232401A1 (en) * 2019-05-15 2020-11-19 Cornell University Combination therapies with ire1 small molecule inhibitors
EP3983400B1 (en) * 2019-06-11 2025-05-28 Genentech, Inc. Quinazolinyl compounds and methods of use
CA3159578A1 (en) * 2019-11-01 2021-05-06 Janssen Biotech, Inc. Fluorinated quinoline and quinoxaline derivatives as dihydroorotate dehydrogenase (dhodh) inhibitors for the treatment of cancer, autoimmune and inflammatory diseases
US20240262830A1 (en) * 2020-02-03 2024-08-08 Nimbus Iaso, Inc. Ire1a 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
WO2022032078A1 (en) * 2020-08-07 2022-02-10 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
PE20250609A1 (es) 2021-12-03 2025-02-26 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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1254169B1 (en) 1999-12-30 2007-05-09 President And Fellows of Harvard College Methods relating to modulation of th2 cell subset activity by modulation of xbp-1 activity
US7906522B2 (en) 2005-04-28 2011-03-15 Kyowa Hakko Kirin Co., Ltd 2-aminoquinazoline derivatives
CA2638734A1 (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
US8940479B2 (en) 2008-01-14 2015-01-27 Cornell University 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
CN103079558B (zh) * 2010-04-05 2025-09-12 上海复星医药产业发展有限公司 IRE-1α抑制剂
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
JP2015532287A (ja) 2012-09-26 2015-11-09 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｉｒｅ１の調節
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
US9957506B2 (en) 2013-09-25 2018-05-01 Cornell University Compounds for inducing anti-tumor immunity and methods thereof
WO2017152126A1 (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
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
WO2019094641A1 (en) * 2017-11-10 2019-05-16 Quentis Therapeutics, Inc. Ire1 small molecule inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
WANG, L. et al.，Nature Chemical Biology，2012年，Vol. 8，pp. 982-989
YANG, W. et al.，Journal of Molecular Structure，2013年，Vol. 1054-1055，pp. 107-116

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

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