CR20220139A - Inhibidor de diacilglicerol aciltransferasa 2 - Google Patents

Inhibidor de diacilglicerol aciltransferasa 2

Info

Publication number
CR20220139A
CR20220139A CR20220139A CR20220139A CR20220139A CR 20220139 A CR20220139 A CR 20220139A CR 20220139 A CR20220139 A CR 20220139A CR 20220139 A CR20220139 A CR 20220139A CR 20220139 A CR20220139 A CR 20220139A
Authority
CR
Costa Rica
Prior art keywords
sup
inhibitor
diacylglycerol acyltransferase
inhibitors
acyltransferase
Prior art date
Application number
CR20220139A
Other languages
English (en)
Inventor
David James Edmonds
Kentaro Futatsugi
Daniel Jonathan Smaltz
Jack Chang Hung Lee
Kevin James Filipski
Michelle Renee Garnsey
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 CR20220139A publication Critical patent/CR20220139A/es

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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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (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 Formula (I) <img src="data:image/png;base64,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 (***)
CR20220139A 2019-10-04 2020-09-30 Inhibidor de diacilglicerol aciltransferasa 2 CR20220139A (es)

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Application Number Priority Date Filing Date Title
US201962911094P 2019-10-04 2019-10-04
US202063074123P 2020-09-03 2020-09-03
PCT/IB2020/059145 WO2021064590A1 (en) 2019-10-04 2020-09-30 Diacylglycerol acyltransferase 2 inhibitor

Publications (1)

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CR20220139A true CR20220139A (es) 2022-05-06

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CR20220139A CR20220139A (es) 2019-10-04 2020-09-30 Inhibidor de diacilglicerol aciltransferasa 2

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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)
EC (1) ECSP22026478A (es)
ES (1) ES2966340T3 (es)
IL (1) IL291763A (es)
MX (1) MX2022004035A (es)
PE (1) PE20221444A1 (es)
TW (1) TWI771766B (es)
WO (1) WO2021064590A1 (es)

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EP4038060B1 (en) 2023-11-15
TWI771766B (zh) 2022-07-21
US11471458B2 (en) 2022-10-18
CL2022000835A1 (es) 2023-01-27
WO2021064590A1 (en) 2021-04-08
JP2022543499A (ja) 2022-10-12
EP4038060A1 (en) 2022-08-10
KR20220079906A (ko) 2022-06-14
IL291763A (en) 2022-06-01
US11065249B2 (en) 2021-07-20
CA3095028A1 (en) 2021-04-04
CO2022004286A2 (es) 2022-04-29
EP4038060C0 (en) 2023-11-15
ES2966340T3 (es) 2024-04-22
ECSP22026478A (es) 2022-05-31
PE20221444A1 (es) 2022-09-21
JP7161081B2 (ja) 2022-10-25
AU2020358955B2 (en) 2023-08-17
US20210100796A1 (en) 2021-04-08
US20210100798A1 (en) 2021-04-08
AU2020358955A1 (en) 2022-04-21
MX2022004035A (es) 2022-05-02
CN114787146A (zh) 2022-07-22
TW202126635A (zh) 2021-07-16

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