CL2022001323A1 - Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x - Google Patents

Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x

Info

Publication number
CL2022001323A1
CL2022001323A1 CL2022001323A CL2022001323A CL2022001323A1 CL 2022001323 A1 CL2022001323 A1 CL 2022001323A1 CL 2022001323 A CL2022001323 A CL 2022001323A CL 2022001323 A CL2022001323 A CL 2022001323A CL 2022001323 A1 CL2022001323 A1 CL 2022001323A1
Authority
CL
Chile
Prior art keywords
hepatic
receptor agonists
oxadiazole derivatives
compound
formula
Prior art date
Application number
CL2022001323A
Other languages
English (en)
Inventor
D Boss Kelly
Fan Yi
Nathanson FLYER Alec
HARDY Declan
Huang Zhihong
Taylor LINKENS Kathryn
Christopher Loren Jon
Ma Fupeng
Molteni Valentina
Shaw Duncan
Smith Jeffrey
Fooks SOLOVAY Catherine
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of CL2022001323A1 publication Critical patent/CL2022001323A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Abstract

Se proporcionan aquí compuestos y composiciones farmacéuticas útiles para el tratamiento de la disfunción de la glándula de Meibomio (MGD), que comprende administrar a un sujeto que lo necesita una cantidad terapéuticamente eficaz de un compuesto de Fórmula (I) o un compuesto de Fórmula (I’), o una composición farmacéutica descripta en la presente memoria.
CL2022001323A 2019-11-25 2022-05-19 Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x CL2022001323A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962940061P 2019-11-25 2019-11-25
US202063106293P 2020-10-27 2020-10-27

Publications (1)

Publication Number Publication Date
CL2022001323A1 true CL2022001323A1 (es) 2023-03-24

Family

ID=73654860

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2022001323A CL2022001323A1 (es) 2019-11-25 2022-05-19 Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x

Country Status (19)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20240238305A1 (en) * 2021-05-20 2024-07-18 Novartis Ag Formulations of 3-((3-(4-(2-(isobutylsulfonyl)phenoxy)-3-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-5-yl)methyl)-5,5-dimethyl-1-(2-morpholinoethyl)imidazolidine-2,4-dione
WO2022249006A1 (en) * 2021-05-24 2022-12-01 Novartis Ag Use of 1,2,4-oxadiazole derivatives as liver x receptor agonists
KR20240059836A (ko) 2022-10-28 2024-05-08 (주)케이메디켐 신규 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 인지기능 개선용 조성물

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
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
US20200188297A1 (en) 2018-12-13 2020-06-18 eyeNOS, Inc. LXR Agonist in Topical Ophthalmic Formulation for Treatment of Dry-Eye Disorder

Also Published As

Publication number Publication date
CN114746149A (zh) 2022-07-12
BR112022009942A2 (pt) 2022-08-09
KR20220106778A (ko) 2022-07-29
MX2022006151A (es) 2022-08-02
UY38964A (es) 2021-06-30
JOP20220124A1 (ar) 2023-01-30
WO2021105857A1 (en) 2021-06-03
US20220340573A1 (en) 2022-10-27
CA3157657A1 (en) 2021-06-03
TW202132289A (zh) 2021-09-01
ECSP22040362A (es) 2022-06-30
AU2020394597A1 (en) 2022-06-02
IL291958A (en) 2022-06-01
EP4065228A1 (en) 2022-10-05
US20220064164A1 (en) 2022-03-03
CR20220227A (es) 2022-06-15
US11427586B2 (en) 2022-08-30
PE20221785A1 (es) 2022-11-22
JP2023503320A (ja) 2023-01-27
CO2022006645A2 (es) 2022-05-31
AU2020394597B2 (en) 2024-03-14

Similar Documents

Publication Publication Date Title
CL2022001323A1 (es) Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x
PE20191541A1 (es) Composiciones y metodos para inhibir la accion de la arginasa
BR112021020335A2 (pt) Agonistas glp-1r e usos dos mesmos
CO2021008089A2 (es) Agonistas de glp-1r y usos de los mismos
CL2023001738A1 (es) Inhibidores de prmt5
DOP2021000183A (es) Compuestos tricíclicos condensados útiles como agentes anticancerígenos
CL2017002636A1 (es) Composiciones que comprenden una combinación de un anticuerpo anti muerte programada 1 (pd-1) y otro anticuerpo.
ECSP21080535A (es) Compuestos y métodos para el tratamiento de covid-19
PE20191474A1 (es) Compuestos de amino-triazolopiridina y su uso en el tratamiento del cancer
CL2022001743A1 (es) Dosis de gamma-hidroxibutirato (ghb)
CL2011000504A1 (es) Compuestos derivados de piridin-4-il-tiazol-2il-amida 2-amida-pirrolidin-1,2-dicarboxilico, inhibidores de quinasa de fosfatidil-inositol-3; composicion farmaceutica que comprende a uno de los compuestos; y uso de los compuestos en la preparacion de un medicamento para el tratamiento del cancer.
AR069490A1 (es) Agonistas de los receptores de glucocorticoides
ECSP088120A (es) Derivados de piridazinona como agonistas del receptorde la hormona tiroidea
BR112016002651A2 (pt) composto, sal farmaceuticamente aceitável de um composto, composição farmacêutica, combinação, formulação farmacêutica, métodos para exterminar uma micobactéria e/ou inibir a replicação das micobactérias, e para tratar uma infecção e uma doença, e, uso de um composto
CL2021003455A1 (es) Análogos de 3-(5-meti l-1 ,3-tiazol-2-1 l)-n--{( 1 r)-1-[2-(trifluoro-metil)pirimidin-5-il]etil}benzamida
UY38228A (es) Compuestos de triazolopirimidina y su uso en el tratamiento del cáncer
MX2022000945A (es) Composicion para incrementar la expresion de pgc-1alfa.
ECSP19044591A (es) Amidas aromáticas de ácido carboxílico como antagonistas del receptor b1 de la bradiquinina
AR125457A2 (es) Compuestos inhibidores dobles de magl y faah y composición farmacéutica
CO2020013834A2 (es) Ciertos compuestos de pladienolida y métodos de uso
CL2011001860A1 (es) Compuestos derivados de indol; procedimiento de preparacion de dichos compuestos; composicion y combinacion farmaceutica; y uso en el tratamiento del cancer.
AR127470A1 (es) Inhibidores de lrrk2
AR117844A1 (es) Derivados de tiazolopiridina como antagonistas del receptor de adenosina
CL2022000893A1 (es) Derivados de 2-azaspiro[3,4]octano como agonistas de m4
AR101901A1 (es) Tratamiento de enfermedades neurodegenerativas con una combinación de laquinimod y fingolimod