KR20220106778A - 간 x 수용체 작용제로서의 1,2,4-옥사디아졸 유도체 - Google Patents

간 x 수용체 작용제로서의 1,2,4-옥사디아졸 유도체 Download PDF

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Publication number
KR20220106778A
KR20220106778A KR1020227020461A KR20227020461A KR20220106778A KR 20220106778 A KR20220106778 A KR 20220106778A KR 1020227020461 A KR1020227020461 A KR 1020227020461A KR 20227020461 A KR20227020461 A KR 20227020461A KR 20220106778 A KR20220106778 A KR 20220106778A
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South Korea
Prior art keywords
methyl
trifluoromethyl
phenyl
compound
dione
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Ceased
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KR1020227020461A
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English (en)
Korean (ko)
Inventor
켈리 디. 보스
이 판
앨릭 나단슨 플라이어
데클랜 하디
지홍 후앙
캐서린 테일러 링켄스
존 크리스토퍼 로렌
푸펭 마
발렌티나 몰테니
던칸 쇼
제프리 스미스
캐서린 포크스 솔로베이
Original Assignee
노파르티스 아게
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Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20220106778A publication Critical patent/KR20220106778A/ko
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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 system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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 two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020227020461A 2019-11-25 2020-11-23 간 x 수용체 작용제로서의 1,2,4-옥사디아졸 유도체 Ceased KR20220106778A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962940061P 2019-11-25 2019-11-25
US62/940,061 2019-11-25
US202063106293P 2020-10-27 2020-10-27
US63/106,293 2020-10-27
PCT/IB2020/061053 WO2021105857A1 (en) 2019-11-25 2020-11-23 1,2,4-oxadiazole derivatives as liver x receptor agonists

Publications (1)

Publication Number Publication Date
KR20220106778A true KR20220106778A (ko) 2022-07-29

Family

ID=73654860

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227020461A Ceased KR20220106778A (ko) 2019-11-25 2020-11-23 간 x 수용체 작용제로서의 1,2,4-옥사디아졸 유도체

Country Status (22)

Country Link
US (2) US11427586B2 (https=)
EP (1) EP4065228A1 (https=)
JP (1) JP2023503320A (https=)
KR (1) KR20220106778A (https=)
CN (1) CN114746149A (https=)
AU (1) AU2020394597B2 (https=)
BR (1) BR112022009942A2 (https=)
CA (1) CA3157657A1 (https=)
CL (1) CL2022001323A1 (https=)
CO (1) CO2022006645A2 (https=)
CR (1) CR20220227A (https=)
DO (1) DOP2022000107A (https=)
EC (1) ECSP22040362A (https=)
IL (1) IL291958A (https=)
JO (1) JOP20220124A1 (https=)
MX (1) MX2022006151A (https=)
PE (1) PE20221785A1 (https=)
PH (1) PH12022551248A1 (https=)
PY (1) PY2077235A (https=)
TW (1) TW202132289A (https=)
UY (1) UY38964A (https=)
WO (1) WO2021105857A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20240059836A (ko) 2022-10-28 2024-05-08 (주)케이메디켐 신규 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 인지기능 개선용 조성물

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024518128A (ja) * 2021-05-20 2024-04-24 ノバルティス アーゲー ３－（（３－（４－（２－（イソブチルスルホニル）フェノキシ）－３－（トリフルオロメチル）フェニル）－１，２，４－オキサジアゾール－５－イル）メチル）－５，５－ジメチル－１－（２－モルホリノエチル）イミダゾリジン－２，４－ジオンの製剤
WO2022249006A1 (en) * 2021-05-24 2022-12-01 Novartis Ag Use of 1,2,4-oxadiazole derivatives as liver x receptor agonists

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201120016A (en) 2009-12-08 2011-06-16 Abbott Lab Novel oxadiazole compounds
US8729109B2 (en) * 2011-09-08 2014-05-20 Allergan, Inc. 3-(4-(5-phenyl-1 ,2,4-oxadiazol-3-yl)phenoxy)propan-2-ol derivatives as sphingosine-1phosphate receptors modulators
WO2013131018A1 (en) 2012-03-02 2013-09-06 Zalicus Pharmaceuticals Ltd. Biaryl inhibitors of the sodium channel
WO2015187840A2 (en) * 2014-06-03 2015-12-10 Duke University Methods and formulations for treatment of ocular disorders
JP2022514257A (ja) 2018-12-13 2022-02-10 アイノス，インコーポレイテッド ドライアイ疾患の治療のための局所点眼製剤におけるｌｘｒアゴニスト

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20240059836A (ko) 2022-10-28 2024-05-08 (주)케이메디켐 신규 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 인지기능 개선용 조성물
KR20240060524A (ko) 2022-10-28 2024-05-08 (주)케이메디켐 신규 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 인지기능 개선용 조성물

Also Published As

Publication number Publication date
MX2022006151A (es) 2022-08-02
EP4065228A1 (en) 2022-10-05
US11427586B2 (en) 2022-08-30
JOP20220124A1 (ar) 2022-05-23
AU2020394597B2 (en) 2024-03-14
TW202132289A (zh) 2021-09-01
ECSP22040362A (es) 2022-06-30
PY2077235A (es) 2022-10-31
CO2022006645A2 (es) 2022-05-31
PH12022551248A1 (en) 2023-09-11
US20220340573A1 (en) 2022-10-27
UY38964A (es) 2021-06-30
CN114746149A (zh) 2022-07-12
IL291958A (en) 2022-06-01
JP2023503320A (ja) 2023-01-27
DOP2022000107A (es) 2022-06-15
AU2020394597A1 (en) 2022-06-02
CL2022001323A1 (es) 2023-03-24
CA3157657A1 (en) 2021-06-03
PE20221785A1 (es) 2022-11-22
WO2021105857A1 (en) 2021-06-03
BR112022009942A2 (pt) 2022-08-09
CR20220227A (es) 2022-06-15
US20220064164A1 (en) 2022-03-03

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