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ECSP22026478A - Inhibidor de diacilglicerol aciltransferasa 2 - Google Patents

Inhibidor de diacilglicerol aciltransferasa 2

Info

Publication number
ECSP22026478A
ECSP22026478A ECSENADI202226478A ECDI202226478A ECSP22026478A EC SP22026478 A ECSP22026478 A EC SP22026478A EC SENADI202226478 A ECSENADI202226478 A EC SENADI202226478A EC DI202226478 A ECDI202226478 A EC DI202226478A EC SP22026478 A ECSP22026478 A EC SP22026478A
Authority
EC
Ecuador
Prior art keywords
diacylglycerol
acytransferase
inhibitor
inhibitors
dgat2
Prior art date
Application number
ECSENADI202226478A
Other languages
English (en)
Inventor
Kentaro Futatsugi
David James Edmonds
Daniel Jonathan Smaltz
Kevin James Filipski
Michelle Renee Garnsey
Jack Chang Hung Lee
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of ECSP22026478A publication Critical patent/ECSP22026478A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 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
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

En la presente se describen compuestos de la Fórmula (I) en donde R1, R2, R3, R4, R5, R6, R7, R8 y R9 se definen en la presente, su uso como inhibidores de diacilglicerol aciltransferasa 2 (DGAT2), composiciones farmacéuticas que contienen dichos inhibidores y el uso de dichos inhibidores para tratar, por ejemplo, NASH.
ECSENADI202226478A 2019-10-04 2022-04-04 Inhibidor de diacilglicerol aciltransferasa 2 ECSP22026478A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962911094P 2019-10-04 2019-10-04
US202063074123P 2020-09-03 2020-09-03

Publications (1)

Publication Number Publication Date
ECSP22026478A true ECSP22026478A (es) 2022-05-31

Family

ID=72826929

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202226478A ECSP22026478A (es) 2019-10-04 2022-04-04 Inhibidor de diacilglicerol aciltransferasa 2

Country Status (19)

Country Link
US (2) US11471458B2 (es)
EP (1) EP4038060B1 (es)
JP (1) JP7161081B2 (es)
KR (1) KR20220079906A (es)
CN (1) CN114787146A (es)
AU (1) AU2020358955B2 (es)
CA (1) CA3095028A1 (es)
CL (1) CL2022000835A1 (es)
CO (1) CO2022004286A2 (es)
CR (1) CR20220139A (es)
DO (1) DOP2022000070A (es)
EC (1) ECSP22026478A (es)
ES (1) ES2966340T3 (es)
IL (1) IL291763A (es)
MX (1) MX2022004035A (es)
PE (1) PE20221444A1 (es)
PH (1) PH12022550812A1 (es)
TW (1) TWI771766B (es)
WO (1) WO2021064590A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022058085A (ja) * 2020-02-24 2022-04-11 ファイザー・インク ジアシルグリセロールアシルトランスフェラーゼ2阻害剤とアセチル-CoAカルボキシラーゼ阻害剤との組合せ
US11976061B2 (en) 2020-10-08 2024-05-07 Merck Sharp & Dohme, LLC Preparation of benzimidazolone derivatives as novel diacylglyceride O-acyltransferase 2 inhibitors
CN115429810B (zh) * 2021-06-03 2024-03-08 苏州禾研生物技术有限公司 异黄酮类化合物在制备预防或治疗酒精性肝损伤或解酒保肝的药物中的用途
AU2023400409A1 (en) 2022-12-02 2025-06-26 Merck Sharp & Dohme Llc Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors

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US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
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Also Published As

Publication number Publication date
PH12022550812A1 (en) 2023-07-17
TWI771766B (zh) 2022-07-21
TW202126635A (zh) 2021-07-16
MX2022004035A (es) 2022-05-02
JP7161081B2 (ja) 2022-10-25
US11065249B2 (en) 2021-07-20
JP2022543499A (ja) 2022-10-12
US11471458B2 (en) 2022-10-18
KR20220079906A (ko) 2022-06-14
CA3095028A1 (en) 2021-04-04
IL291763A (en) 2022-06-01
CN114787146A (zh) 2022-07-22
ES2966340T3 (es) 2024-04-22
PE20221444A1 (es) 2022-09-21
US20210100798A1 (en) 2021-04-08
WO2021064590A1 (en) 2021-04-08
DOP2022000070A (es) 2022-05-15
AU2020358955B2 (en) 2023-08-17
AU2020358955A1 (en) 2022-04-21
CO2022004286A2 (es) 2022-04-29
EP4038060B1 (en) 2023-11-15
EP4038060A1 (en) 2022-08-10
US20210100796A1 (en) 2021-04-08
CR20220139A (es) 2022-05-06
CL2022000835A1 (es) 2023-01-27
EP4038060C0 (en) 2023-11-15

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