CA3237199A1 - Pparg inverse agonists and uses thereof - Google Patents

Pparg inverse agonists and uses thereof Download PDF

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Publication number
CA3237199A1
CA3237199A1 CA3237199A CA3237199A CA3237199A1 CA 3237199 A1 CA3237199 A1 CA 3237199A1 CA 3237199 A CA3237199 A CA 3237199A CA 3237199 A CA3237199 A CA 3237199A CA 3237199 A1 CA3237199 A1 CA 3237199A1
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CA
Canada
Prior art keywords
compound
formula
pharmaceutically acceptable
acceptable salt
halo
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
CA3237199A
Other languages
English (en)
French (fr)
Inventor
Danmei Dai
Bo Zheng
Fei Wang
Liqing CONG
Yaohui Huang
Runyan LI
Xiaoyang Wang
Peter Wade
Jonathan E. Wilson
James E. Audia
Jacob I. Stuckey
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
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Flare Therapeutics Inc
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Filing date
Publication date
Application filed by Flare Therapeutics Inc filed Critical Flare Therapeutics Inc
Publication of CA3237199A1 publication Critical patent/CA3237199A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/56—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and doubly-bound oxygen atoms bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3237199A 2021-11-02 2022-11-01 Pparg inverse agonists and uses thereof Pending CA3237199A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163274596P 2021-11-02 2021-11-02
US63/274,596 2021-11-02
US202263347671P 2022-06-01 2022-06-01
US63/347,671 2022-06-01
PCT/CN2022/129034 WO2023078252A1 (en) 2021-11-02 2022-11-01 Pparg inverse agonists and uses thereof

Publications (1)

Publication Number Publication Date
CA3237199A1 true CA3237199A1 (en) 2023-05-11

Family

ID=84283142

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3237199A Pending CA3237199A1 (en) 2021-11-02 2022-11-01 Pparg inverse agonists and uses thereof

Country Status (25)

Country Link
US (2) US11820747B2 (https=)
EP (2) EP4426434B1 (https=)
JP (1) JP2025508272A (https=)
KR (1) KR20240144096A (https=)
CN (1) CN119677720A (https=)
AU (1) AU2022380979A1 (https=)
CA (1) CA3237199A1 (https=)
CL (1) CL2024001346A1 (https=)
DK (1) DK4426434T3 (https=)
ES (1) ES3053082T3 (https=)
FI (1) FI4426434T3 (https=)
HR (1) HRP20251438T1 (https=)
IL (1) IL312547A (https=)
LT (1) LT4426434T (https=)
MA (1) MA67105B1 (https=)
MD (1) MD4426434T2 (https=)
MX (1) MX2024005405A (https=)
PE (1) PE20250739A1 (https=)
PL (1) PL4426434T3 (https=)
PT (1) PT4426434T (https=)
RS (1) RS67425B1 (https=)
SI (1) SI4426434T1 (https=)
SM (1) SMT202500447T1 (https=)
TW (1) TW202334089A (https=)
WO (1) WO2023078252A1 (https=)

Families Citing this family (5)

* 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
CA3254026A1 (en) * 2022-03-08 2023-09-14 Flare Therapeutics Inc. Inverse PPARG agonists and their uses
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
AU2024367019A1 (en) 2023-10-27 2026-04-23 Flare Therapeutics Inc. Pparg inverse agonists and immunotherapies for treating cancer
WO2025098515A1 (en) * 2023-11-10 2025-05-15 Danatlas Pharmaceuticals Co., Ltd. Heterocyclic derivatives, compositions and uses thereof

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