AU2021401741A1 - Macrocycles and their use - Google Patents

Macrocycles and their use Download PDF

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Publication number
AU2021401741A1
AU2021401741A1 AU2021401741A AU2021401741A AU2021401741A1 AU 2021401741 A1 AU2021401741 A1 AU 2021401741A1 AU 2021401741 A AU2021401741 A AU 2021401741A AU 2021401741 A AU2021401741 A AU 2021401741A AU 2021401741 A1 AU2021401741 A1 AU 2021401741A1
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AU
Australia
Prior art keywords
alkyl
alkylene
compound
pharmaceutically acceptable
acceptable salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
AU2021401741A
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English (en)
Other versions
AU2021401741A9 (en
Inventor
Jingrong J. Cui
Evan W. ROGERS
Eugene Rui
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Blossomhill Therapeutics Inc
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Blossomhill Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Blossomhill Therapeutics Inc filed Critical Blossomhill Therapeutics Inc
Publication of AU2021401741A1 publication Critical patent/AU2021401741A1/en
Publication of AU2021401741A9 publication Critical patent/AU2021401741A9/en
Pending legal-status Critical Current

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    • 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
    • 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
    • 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

Landscapes

  • 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)
AU2021401741A 2020-12-17 2021-12-16 Macrocycles and their use Pending AU2021401741A1 (en)

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
AU2021401741A1 true AU2021401741A1 (en) 2023-06-29
AU2021401741A9 AU2021401741A9 (en) 2024-09-19

Family

ID=82058646

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021401741A Pending AU2021401741A1 (en) 2020-12-17 2021-12-16 Macrocycles and their use

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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3062B1 (ar) * 2010-10-05 2017-03-15 Lilly Co Eli R)-(e)-2-(4-(2-(5-(1-(3، 5-داي كلورو بيريدين-4-يل)إيثوكسي)-1h-إندازول-3-يل)?ينيل)-1h-بيرازول-1-يل)إيثانول بلوري
DK2822953T5 (en) * 2012-03-06 2017-09-11 Pfizer Macrocyclic derivatives for the treatment of proliferative diseases
EP3333157B1 (en) * 2015-08-07 2020-12-23 Harbin Zhenbao Pharmaceutical Co., Ltd. Vinyl compounds as fgfr and vegfr inhibitors
CN111269245B (zh) * 2018-12-04 2021-08-27 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
BR112021012057A2 (pt) * 2018-12-21 2021-10-19 Revolution Medicines, Inc. Compostos que participam de ligação cooperativa e usos dos mesmos

Also Published As

Publication number Publication date
KR20230121773A (ko) 2023-08-21
IL303419A (en) 2023-08-01
US20240182487A1 (en) 2024-06-06
WO2022133037A1 (en) 2022-06-23
EP4262796A4 (en) 2025-04-02
JP2023553835A (ja) 2023-12-26
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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