JP2023553835A - 大環状化合物およびそれらの使用 - Google Patents

大環状化合物およびそれらの使用 Download PDF

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Publication number
JP2023553835A
JP2023553835A JP2023532465A JP2023532465A JP2023553835A JP 2023553835 A JP2023553835 A JP 2023553835A JP 2023532465 A JP2023532465 A JP 2023532465A JP 2023532465 A JP2023532465 A JP 2023532465A JP 2023553835 A JP2023553835 A JP 2023553835A
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alkyl
alkylene
pharmaceutically acceptable
acceptable salt
membered
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Japanese (ja)
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JP2023553835A5 (https=
Inventor
ジェイ ツイ,ジンロン
ルイ,ユージーン
ダブリュー ロジャーズ,エバン
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Blossomhill Therapeutics Inc
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Blossomhill Therapeutics Inc
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Publication of JP2023553835A publication Critical patent/JP2023553835A/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/529Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
    • 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2023532465A 2020-12-17 2021-12-16 大環状化合物およびそれらの使用 Pending JP2023553835A (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US202063126722P 2020-12-17 2020-12-17
US63/126,722 2020-12-17
US202163279850P 2021-11-16 2021-11-16
US63/279,850 2021-11-16
US202163284789P 2021-12-01 2021-12-01
US63/284,789 2021-12-01
US202163289014P 2021-12-13 2021-12-13
US63/289,014 2021-12-13
PCT/US2021/063721 WO2022133037A1 (en) 2020-12-17 2021-12-16 Macrocycles and their use

Publications (2)

Publication Number Publication Date
JP2023553835A true JP2023553835A (ja) 2023-12-26
JP2023553835A5 JP2023553835A5 (https=) 2024-12-24

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JP2023532465A Pending JP2023553835A (ja) 2020-12-17 2021-12-16 大環状化合物およびそれらの使用

Country Status (11)

Country Link
US (1) US20240182487A1 (https=)
EP (1) EP4262796A4 (https=)
JP (1) JP2023553835A (https=)
KR (1) KR20230121773A (https=)
AU (1) AU2021401741A1 (https=)
CA (1) CA3202770A1 (https=)
IL (1) IL303419A (https=)
MX (1) MX2023007162A (https=)
PY (1) PY21110949A (https=)
UY (1) UY39574A (https=)
WO (1) WO2022133037A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2023283476A1 (en) * 2022-06-08 2024-11-14 Blossomhill Therapeutics, Inc. Indazole macrocycles and their use
CA3258157A1 (en) * 2022-06-08 2023-12-14 Blossomhill Therapeutics, Inc. Indazole-Containing Macrocycles and Their Use
JP2025524038A (ja) * 2022-07-27 2025-07-25 上海和誉生物医薬科技有限公司 大環状egfr阻害剤、その製造方法及び薬学における応用
EP4655304A1 (en) * 2023-02-22 2025-12-03 Yuhan Corporation Macrocyclic aminopyridine compounds as egfr inhibitors
JP2026507654A (ja) * 2023-02-22 2026-03-04 ユーハン・コーポレイション Egfr阻害剤としての大環状アミノピリジン化合物
KR20250142978A (ko) * 2023-02-22 2025-09-30 주식회사유한양행 Egfr 억제제로서의 마크로시클릭 아미노피리딘 화합물
EP4688750A1 (en) 2023-04-06 2026-02-11 Pfizer Inc. Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators
AU2024266587A1 (en) * 2023-05-02 2025-09-11 Blossomhill Therapeutics, Inc. Egfr inhibitors for treating disease
EP4731213A2 (en) * 2023-06-23 2026-04-29 Blossomhill Therapeutics, Inc. Combination therapy involving macrocyclic indazole compounds
WO2025122911A1 (en) * 2023-12-07 2025-06-12 Blossomhill Therapeutics, Inc. Indazole macrocycle polymorphs
WO2025122859A1 (en) * 2023-12-08 2025-06-12 Blossomhill Therapeutics, Inc. Indazole-based macrocyclic compounds
WO2025199438A1 (en) * 2024-03-22 2025-09-25 Blossomhill Therapeutics, Inc. 7-azaindazole macrocycles and their use
WO2025245175A1 (en) * 2024-05-22 2025-11-27 Ajax Therapeutics, Inc. Macrocyclic heteroaromatic inhibitors of jak2

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013538875A (ja) * 2010-10-05 2013-10-17 イーライ リリー アンド カンパニー 結晶((r)−(e)−2−(4−(2−(5−(1−(3,5−ジクロロピリジン−4−イル)エトキシ)−1h−インダゾール−3−イル)ビニル)−1h−ピラゾール−1−イル)エタノールおよびfgfr阻害剤としての使用
JP2018531218A (ja) * 2015-08-07 2018-10-25 ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド Fgfr及びvegfr阻害剤であるビニル化合物
CN111269245A (zh) * 2018-12-04 2020-06-12 杭州百新生物医药科技有限公司 一种环状氨基嘧啶衍生物及其抑制激酶的活性和用途
US20200197391A1 (en) * 2018-12-21 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2822953T5 (en) * 2012-03-06 2017-09-11 Pfizer Macrocyclic derivatives for the treatment of proliferative diseases

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013538875A (ja) * 2010-10-05 2013-10-17 イーライ リリー アンド カンパニー 結晶((r)−(e)−2−(4−(2−(5−(1−(3,5−ジクロロピリジン−4−イル)エトキシ)−1h−インダゾール−3−イル)ビニル)−1h−ピラゾール−1−イル)エタノールおよびfgfr阻害剤としての使用
JP2018531218A (ja) * 2015-08-07 2018-10-25 ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド Fgfr及びvegfr阻害剤であるビニル化合物
CN111269245A (zh) * 2018-12-04 2020-06-12 杭州百新生物医药科技有限公司 一种环状氨基嘧啶衍生物及其抑制激酶的活性和用途
US20200197391A1 (en) * 2018-12-21 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof

Also Published As

Publication number Publication date
KR20230121773A (ko) 2023-08-21
IL303419A (en) 2023-08-01
AU2021401741A1 (en) 2023-06-29
US20240182487A1 (en) 2024-06-06
WO2022133037A1 (en) 2022-06-23
EP4262796A4 (en) 2025-04-02
EP4262796A1 (en) 2023-10-25
MX2023007162A (es) 2023-06-29
PY21110949A (es) 2023-08-07
TW202241911A (zh) 2022-11-01
AU2021401741A9 (en) 2024-09-19
CA3202770A1 (en) 2022-06-23
UY39574A (es) 2022-07-29

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