TW202334089A - Ｐｐａｒｇ反向激動劑及其用途 - Google Patents

Ｐｐａｒｇ反向激動劑及其用途 Download PDF

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Publication number
TW202334089A
TW202334089A TW111141614A TW111141614A TW202334089A TW 202334089 A TW202334089 A TW 202334089A TW 111141614 A TW111141614 A TW 111141614A TW 111141614 A TW111141614 A TW 111141614A TW 202334089 A TW202334089 A TW 202334089A
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compound
formula
pharmaceutically acceptable
alkyl
acceptable salt
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TW111141614A
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Chinese (zh)
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喬納森 Ｅ 威爾遜
詹姆斯 Ｅ 奧迪亞
雅各布 Ｉ 斯塔基
戴丹梅
鄭博
王飛
孔麗琴
黃耀輝
李潤言
王曉陽
彼得 韋德
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美商夫雷爾醫療公司
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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)
TW111141614A 2021-11-02 2022-11-01 Ｐｐａｒｇ反向激動劑及其用途 TW202334089A (zh)

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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

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TW202334089A true TW202334089A (zh) 2023-09-01

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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=)

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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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