JP2025508272A - Ｐｐａｒｇ逆アゴニストおよびその使用 - Google Patents

Ｐｐａｒｇ逆アゴニストおよびその使用 Download PDF

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Publication number
JP2025508272A
JP2025508272A JP2024526592A JP2024526592A JP2025508272A JP 2025508272 A JP2025508272 A JP 2025508272A JP 2024526592 A JP2024526592 A JP 2024526592A JP 2024526592 A JP2024526592 A JP 2024526592A JP 2025508272 A JP2025508272 A JP 2025508272A
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JP
Japan
Prior art keywords
compound
formula
pharma
halo
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
JP2024526592A
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English (en)
Japanese (ja)
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JP2025508272A5 (enExample
Inventor
ダイ，ダンメイ
ジェン，ボー
ワーン，フェイ
ツォン，リチン
ホワーン，ヤオフイ
リ，ルニャン
ワーン，シャオヤン
ウェード，ピーター
ウィルソン，ジョナサン・イー
オーディア，ジェームズ・イー
スタッキー，ジェイコブ・アイ
ガイアー，マイケル・ジェイ
スコット，マーク・イー
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Flare Therapeutics Inc
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Flare 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 Flare Therapeutics Inc filed Critical Flare Therapeutics Inc
Publication of JP2025508272A publication Critical patent/JP2025508272A/ja
Publication of JP2025508272A5 publication Critical patent/JP2025508272A5/ja
Pending legal-status Critical Current

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Classifications

    • 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024526592A 2021-11-02 2022-11-01 Ｐｐａｒｇ逆アゴニストおよびその使用 Pending JP2025508272A (ja)

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 (2)

Publication Number Publication Date
JP2025508272A true JP2025508272A (ja) 2025-03-24
JP2025508272A5 JP2025508272A5 (enExample) 2025-11-07

Family

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JP2024526592A Pending JP2025508272A (ja) 2021-11-02 2022-11-01 Ｐｐａｒｇ逆アゴニストおよびその使用

Country Status (25)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024508908A (ja) * 2021-03-02 2024-02-28 フレア・セラビューティクス・インコーポレーテッド Ｐｐａｒｇ逆アゴニストおよびその使用

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SMT202500447T1 (it) * 2021-11-02 2026-01-12 Flare Therapeutics Inc Agonisti inversi di pparg e loro usi
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
IL327890A (en) 2023-10-27 2026-06-01 Flare Therapeutics Inc Pparg inverse agonists and immunotherapies for treating cancer
CN122122131A (zh) * 2023-11-10 2026-05-29 北京丹擎医药科技有限公司 杂环衍生物及其组合物和应用
WO2026046259A1 (zh) * 2024-08-27 2026-03-05 杭州英创医药科技有限公司 作为pparg反向激动剂的化合物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009502970A (ja) * 2005-07-29 2009-01-29 レスバーロジックス コーポレイション 複合疾患の予防および処置のための薬学的組成物および挿入可能な医療用デバイスによるその送達
CN107522657A (zh) * 2017-09-28 2017-12-29 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
JP2024529534A (ja) * 2021-08-05 2024-08-06 フレア・セラビューティクス・インコーポレーテッド Ｐｐａｒｇ逆アゴニストおよびその使用
JP7853310B2 (ja) * 2021-03-02 2026-04-28 フレア・セラピューティクス・インコーポレーテッド Ｐｐａｒｇ逆アゴニストおよびその使用

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