CN114746149A - 作为肝脏x受体激动剂的1,2,4-噁二唑衍生物 - Google Patents

作为肝脏x受体激动剂的1,2,4-噁二唑衍生物 Download PDF

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Publication number
CN114746149A
CN114746149A CN202080081467.7A CN202080081467A CN114746149A CN 114746149 A CN114746149 A CN 114746149A CN 202080081467 A CN202080081467 A CN 202080081467A CN 114746149 A CN114746149 A CN 114746149A
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CN
China
Prior art keywords
methyl
trifluoromethyl
compound
phenyl
oxadiazol
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
CN202080081467.7A
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English (en)
Chinese (zh)
Inventor
K·D·博斯
范艺
A·N·弗莱尔
D·哈代
黄志红
K·T·林肯斯
J·C·洛伦
马缚鹏
V·莫尔泰尼
D·肖
J·史密斯
C·F·索洛维
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Novartis AG
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Novartis AG
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Filing date
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Publication of CN114746149A publication Critical patent/CN114746149A/zh
Pending 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)
CN202080081467.7A 2019-11-25 2020-11-23 作为肝脏x受体激动剂的1,2,4-噁二唑衍生物 Pending CN114746149A (zh)

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
CN114746149A true CN114746149A (zh) 2022-07-12

Family

ID=73654860

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080081467.7A Pending CN114746149A (zh) 2019-11-25 2020-11-23 作为肝脏x受体激动剂的1,2,4-噁二唑衍生物

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=)

Families Citing this family (3)

* 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
KR102882404B1 (ko) 2022-10-28 2025-11-06 (주)케이메디켐 신규 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 인지기능 개선용 조성물

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015187840A2 (en) * 2014-06-03 2015-12-10 Duke University Methods and formulations for treatment of ocular disorders

Family Cites Families (4)

* 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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015187840A2 (en) * 2014-06-03 2015-12-10 Duke University Methods and formulations for treatment of ocular disorders

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JOSHUA R. SCHULTZ，等: "Role of LXRs in control of lipogenesis", 《GENES & DEVELOPMENT 》, vol. 14, 31 December 2000 (2000-12-31), pages 2831 *
YA ¸SAR DÜRÜST，等: "Synthesis and crystal structure of new heterocycles containing 1, 2, 4-oxadiazole, 1, 2, 4-oxadiazolone (thione), hydantoin, and mercaptobenzimidazole units", 《MOL DIVERS 》, vol. 18, 4 May 2014 (2014-05-04), pages 545 *

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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
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
KR20220106778A (ko) 2022-07-29
CR20220227A (es) 2022-06-15
US20220064164A1 (en) 2022-03-03

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