KR102748047B1 - Egfr 이량체 붕괴제 및 이의 용도 - Google Patents

Egfr 이량체 붕괴제 및 이의 용도 Download PDF

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KR102748047B1
KR102748047B1 KR1020207027147A KR20207027147A KR102748047B1 KR 102748047 B1 KR102748047 B1 KR 102748047B1 KR 1020207027147 A KR1020207027147 A KR 1020207027147A KR 20207027147 A KR20207027147 A KR 20207027147A KR 102748047 B1 KR102748047 B1 KR 102748047B1
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compound
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reaction mixture
egfr
triazaspiro
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KR20200124709A (ko
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무케시 케이. 냐티
티오도르 에스. 로렌스
크리스토퍼 와이트헤드
제이슨 크리스토퍼 레시
브레넌 테일러 워치
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더 리젠츠 오브 더 유니버시티 오브 미시간
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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D233/70One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D233/84Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems

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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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020207027147A 2018-02-23 2019-02-25 Egfr 이량체 붕괴제 및 이의 용도 Active KR102748047B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862634452P 2018-02-23 2018-02-23
US62/634,452 2018-02-23
PCT/US2019/019391 WO2019165358A1 (en) 2018-02-23 2019-02-25 Egfr dimer disruptors and use of the same

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KR20200124709A KR20200124709A (ko) 2020-11-03
KR102748047B1 true KR102748047B1 (ko) 2024-12-27

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KR1020207027147A Active KR102748047B1 (ko) 2018-02-23 2019-02-25 Egfr 이량체 붕괴제 및 이의 용도

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US (2) US11358965B2 (https=)
EP (1) EP3755323A4 (https=)
JP (2) JP7497046B2 (https=)
KR (1) KR102748047B1 (https=)
CN (1) CN111886009A (https=)
AU (1) AU2019223168B2 (https=)
BR (1) BR112020017184A2 (https=)
CA (1) CA3091834A1 (https=)
EA (1) EA202092000A1 (https=)
MX (1) MX2020008767A (https=)
WO (1) WO2019165358A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
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CA3091834A1 (en) * 2018-02-23 2019-08-29 The Regents Of The University Of Michigan Egfr dimer disruptors and use of the same
CN114286676A (zh) * 2019-08-22 2022-04-05 密歇根大学董事会 治疗kras相关癌症的方法
CA3172812A1 (en) * 2020-03-05 2021-09-10 The Regents Of The University Of Michigan Inhibitors of egfr, kras, braf, and other targets and use of the same
MX2022010977A (es) * 2020-03-05 2022-12-02 Univ Michigan Regents Inhibidores de egfr, kras, braf y otros objetivos y uso de los mismos.
IL301532A (en) 2020-09-23 2023-05-01 Scorpion Therapeutics Inc History Pyrrolo[2,3-C]pyridin-4-one is useful in cancer treatment
WO2022072632A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
BR112023006531A2 (pt) 2020-10-09 2023-10-03 Scorpion Therapeutics Inc Inibidores heterocílicos de egfr e/ou her2, para uso no tratamento de câncer
EP4225304B1 (en) * 2020-10-12 2025-12-17 The Regents of The University of Michigan Synthesis of egfr modulators
WO2022077154A1 (en) * 2020-10-12 2022-04-21 The Regents Of The University Of Michigan Synthesis of egfr modulators
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
CN121909190A (zh) 2023-06-08 2026-04-21 安塔列斯疗法股份有限公司 1,5-二氢-4H-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗
CN121712773A (zh) 2023-06-08 2026-03-20 安塔列斯疗法股份有限公司 1,5-二氢-4h-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗

Citations (1)

* Cited by examiner, † Cited by third party
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WO2014176475A2 (en) * 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof

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US3547977A (en) 1967-10-27 1970-12-15 Velsicol Chemical Corp Novel carbanilates
US5466468A (en) 1990-04-03 1995-11-14 Ciba-Geigy Corporation Parenterally administrable liposome formulation comprising synthetic lipids
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2012087943A2 (en) 2010-12-20 2012-06-28 The Regents Of The University Of Michigan Inhibitors of the epidermal growth factor receptor-heat shock protein 90 binding interaction
US9499551B2 (en) * 2014-01-24 2016-11-22 Confluence Life Sciences, Inc. Substituted pyrrolo[2,3-b]pyridines for treating cancer or inflammatory diseases
CN113563332B (zh) * 2014-12-23 2024-12-17 达纳-法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
CA3091834A1 (en) 2018-02-23 2019-08-29 The Regents Of The University Of Michigan Egfr dimer disruptors and use of the same

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014176475A2 (en) * 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof

Also Published As

Publication number Publication date
KR20200124709A (ko) 2020-11-03
BR112020017184A2 (pt) 2020-12-22
EA202092000A1 (ru) 2020-12-09
US20200377503A1 (en) 2020-12-03
WO2019165358A1 (en) 2019-08-29
AU2019223168A1 (en) 2020-09-10
CN111886009A (zh) 2020-11-03
US20220340572A1 (en) 2022-10-27
EP3755323A1 (en) 2020-12-30
AU2019223168B2 (en) 2024-09-12
JP7497046B2 (ja) 2024-06-10
EP3755323A4 (en) 2021-11-24
JP2024056735A (ja) 2024-04-23
US11999731B2 (en) 2024-06-04
CA3091834A1 (en) 2019-08-29
MX2020008767A (es) 2021-01-08
US11358965B2 (en) 2022-06-14
JP2021514001A (ja) 2021-06-03

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