CA3227603A1 - Pparg inverse agonists and uses thereof - Google Patents

Pparg inverse agonists and uses thereof Download PDF

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Publication number
CA3227603A1
CA3227603A1 CA3227603A CA3227603A CA3227603A1 CA 3227603 A1 CA3227603 A1 CA 3227603A1 CA 3227603 A CA3227603 A CA 3227603A CA 3227603 A CA3227603 A CA 3227603A CA 3227603 A1 CA3227603 A1 CA 3227603A1
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CA
Canada
Prior art keywords
halo
compound
pharmaceutically acceptable
alkyl
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
CA3227603A
Other languages
English (en)
French (fr)
Inventor
Jonathan E. Wilson
James E. Audia
Jacob I. Stuckey
Mark Scott
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.)
Flare Therapeutics Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA3227603A1 publication Critical patent/CA3227603A1/en
Pending legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
CA3227603A 2021-08-05 2022-08-04 Pparg inverse agonists and uses thereof Pending CA3227603A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163229861P 2021-08-05 2021-08-05
US63/229,861 2021-08-05
PCT/US2022/039385 WO2023014861A1 (en) 2021-08-05 2022-08-04 Pparg inverse agonists and uses thereof

Publications (1)

Publication Number Publication Date
CA3227603A1 true CA3227603A1 (en) 2023-02-09

Family

ID=83149096

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3227603A Pending CA3227603A1 (en) 2021-08-05 2022-08-04 Pparg inverse agonists and uses thereof

Country Status (6)

Country Link
US (1) US20250122169A1 (https=)
EP (1) EP4380928B1 (https=)
JP (1) JP2024529534A (https=)
AU (1) AU2022323260A1 (https=)
CA (1) CA3227603A1 (https=)
WO (1) WO2023014861A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117616012A (zh) * 2021-03-02 2024-02-27 弗拉雷治疗公司 Pparg反向激动剂及其用途
EP4490147A1 (en) * 2022-03-08 2025-01-15 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
CA3254026A1 (en) * 2022-03-08 2023-09-14 Flare Therapeutics Inc. Inverse PPARG agonists and their uses
US20230382910A1 (en) * 2022-04-22 2023-11-30 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2024211969A1 (en) * 2023-04-12 2024-10-17 Setonix Pharmaceuticals Pty Ltd Pparg modulators
WO2024221455A1 (en) * 2023-04-28 2024-10-31 Flare Therapeutics, Inc. Crystalline forms of 3- (5, 7-difluoro-4-oxo-1, 4-dihydroquinolin-2-yl) -4- (methylsulfonyl) benzonitrile

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2496234A1 (en) * 2009-11-07 2012-09-12 Merck Patent GmbH Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors
WO2017061957A1 (en) * 2015-10-09 2017-04-13 Agency For Science, Technology And Research Compounds for treatment of cancer and epigenetics
CN107522657B (zh) * 2017-09-28 2020-06-26 上海中医药大学 一种具有ppar多重激动活性的化合物及其制备方法和应用
CN117616012A (zh) * 2021-03-02 2024-02-27 弗拉雷治疗公司 Pparg反向激动剂及其用途

Also Published As

Publication number Publication date
EP4380928A1 (en) 2024-06-12
US20250122169A1 (en) 2025-04-17
WO2023014861A1 (en) 2023-02-09
EP4380928B1 (en) 2025-10-01
AU2022323260A1 (en) 2024-02-15
JP2024529534A (ja) 2024-08-06

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