MA52967B1 - Composés antagonistes du pcsk9 - Google Patents

Composés antagonistes du pcsk9

Info

Publication number
MA52967B1
MA52967B1 MA52967A MA52967A MA52967B1 MA 52967 B1 MA52967 B1 MA 52967B1 MA 52967 A MA52967 A MA 52967A MA 52967 A MA52967 A MA 52967A MA 52967 B1 MA52967 B1 MA 52967B1
Authority
MA
Morocco
Prior art keywords
compounds
antagonist compounds
pcsk9 antagonist
pcsk9
formula
Prior art date
Application number
MA52967A
Other languages
English (en)
Other versions
MA52967A (fr
Inventor
Fa-Xiang Ding
Chengwei WU
Elisabetta Bianchi
Harold B. Wood
Hubert B. Josien
Thomas Joseph Tucker
Angela Dawn KEREKES
Ling Tong
Abbas M. Walji
Anilkumar G. NAIR
Danila Branca
Yusheng Xiong
Sookhee Nicole Ha
Jian Liu
Sobhana Babu Boga
Original Assignee
Merck Sharp & Dohme Llc
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 Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme Llc
Publication of MA52967A publication Critical patent/MA52967A/fr
Publication of MA52967B1 publication Critical patent/MA52967B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6454—Dibasic site splicing serine proteases, e.g. kexin (3.4.21.61); furin (3.4.21.75) and other proprotein convertases
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21061—Kexin (3.4.21.61), i.e. proprotein convertase subtilisin/kexin type 9
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Steroid Compounds (AREA)

Abstract

L'invention concerne des composés de formule I, ou un sel de ceux-ci, formule dans laquelle A, B, D, X, R1, R2 et R8 sont tels que définis dans la description, lesdits composés présentant des propriétés antagonistes au niveau du PCSK9. L'invention concerne également des formulations pharmaceutiques comprenant les composés de formule I ou leurs sels, et des procédés de traitement de maladies cardiovasculaires et d'états liés à l'activité du PCSK9, par exemple l'athérosclérose, l'hypercholestérolémie, la coronaropathie, le syndrome métabolique, le syndrome coronarien aigu ou les maladies cardiovasculaires et cardiométaboliques associées.
MA52967A 2018-06-21 2019-06-20 Composés antagonistes du pcsk9 MA52967B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862687913P 2018-06-21 2018-06-21
EP19739801.9A EP3810626B1 (fr) 2018-06-21 2019-06-20 Composés antagonistes du pcsk9
PCT/US2019/038155 WO2019246349A1 (fr) 2018-06-21 2019-06-20 Composés antagonistes du pcsk9

Publications (2)

Publication Number Publication Date
MA52967A MA52967A (fr) 2021-04-28
MA52967B1 true MA52967B1 (fr) 2025-09-30

Family

ID=67263083

Family Applications (1)

Application Number Title Priority Date Filing Date
MA52967A MA52967B1 (fr) 2018-06-21 2019-06-20 Composés antagonistes du pcsk9

Country Status (38)

Country Link
US (3) US11427616B2 (fr)
EP (2) EP4660303A3 (fr)
JP (2) JP7112531B2 (fr)
KR (2) KR20250161677A (fr)
CN (2) CN112313243B (fr)
AR (1) AR115597A1 (fr)
AU (2) AU2019290163C1 (fr)
BR (1) BR112020025274A8 (fr)
CA (1) CA3102629A1 (fr)
CL (2) CL2020003257A1 (fr)
CO (1) CO2021000456A2 (fr)
CR (1) CR20210031A (fr)
DK (1) DK3810626T3 (fr)
DO (1) DOP2020000250A (fr)
EA (1) EA202190086A1 (fr)
EC (1) ECSP21003643A (fr)
ES (1) ES3047399T3 (fr)
FI (1) FI3810626T3 (fr)
GE (2) GEP20237506B (fr)
HR (1) HRP20251302T1 (fr)
HU (1) HUE073367T2 (fr)
IL (2) IL279363B2 (fr)
JO (1) JOP20190150A1 (fr)
LT (1) LT3810626T (fr)
MA (1) MA52967B1 (fr)
MD (1) MD3810626T2 (fr)
MX (1) MX2020013726A (fr)
NI (1) NI202000101A (fr)
PE (1) PE20211584A1 (fr)
PH (1) PH12020552187A1 (fr)
PL (1) PL3810626T3 (fr)
PT (1) PT3810626T (fr)
RS (1) RS67338B1 (fr)
SG (1) SG11202012451WA (fr)
SI (1) SI3810626T1 (fr)
TW (1) TWI840376B (fr)
UA (1) UA129467C2 (fr)
WO (1) WO2019246349A1 (fr)

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EP3810177B1 (fr) 2018-06-21 2024-12-04 Ra Pharmaceuticals, Inc. Peptides cycliques pour l'inhibition de la pcsk9
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US20260116923A1 (en) 2023-12-15 2026-04-30 Merck Sharp & Dohme Llc Cyclic peptide il-1beta trap for the treatment of atherosclerosis and inflammatory disorders
WO2025242221A1 (fr) * 2024-05-24 2025-11-27 上海翰森生物医药科技有限公司 Nouvelle chaîne latérale modifiée, son procédé de préparation et son utilisation
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WO2020009805A2 (fr) 2018-06-21 2020-01-09 Merck Sharp & Dohme Corp. Polypeptides cycliques pour l'inhibition de la pcsk9
EP4021919A1 (fr) 2019-08-30 2022-07-06 Merck Sharp & Dohme Corp. Composés antagonistes du pcsk9
EP4076492A4 (fr) 2019-12-20 2024-01-17 Merck Sharp & Dohme LLC Composés antagonistes du pcsk

Also Published As

Publication number Publication date
KR20250161677A (ko) 2025-11-17
US12209145B2 (en) 2025-01-28
TW202019950A (zh) 2020-06-01
SI3810626T1 (sl) 2025-12-31
IL279363B1 (en) 2025-08-01
PL3810626T3 (pl) 2025-12-22
US20230159592A1 (en) 2023-05-25
IL321719A (en) 2025-08-01
MA52967A (fr) 2021-04-28
CN112313243B (zh) 2025-09-02
WO2019246349A8 (fr) 2021-02-04
AU2022259744A1 (en) 2022-12-01
HUE073367T2 (hu) 2026-01-28
EP3810626A1 (fr) 2021-04-28
JP7607615B2 (ja) 2024-12-27
WO2019246349A1 (fr) 2019-12-26
JP2022141879A (ja) 2022-09-29
MD3810626T2 (ro) 2025-12-31
PT3810626T (pt) 2025-10-15
AU2019290163B2 (en) 2022-08-04
EP4660303A2 (fr) 2025-12-10
AU2022259744B2 (en) 2024-07-11
CL2022000027A1 (es) 2022-08-19
LT3810626T (lt) 2025-11-10
DOP2020000250A (es) 2021-02-28
NI202000101A (es) 2021-05-28
KR102884527B1 (ko) 2025-11-13
IL279363A (en) 2021-01-31
GEP20237506B (en) 2023-05-25
JP2025041712A (ja) 2025-03-26
CA3102629A1 (fr) 2019-12-26
CL2020003257A1 (es) 2021-07-23
RS67338B1 (sr) 2025-11-28
UA129467C2 (uk) 2025-05-07
CO2021000456A2 (es) 2021-01-29
BR112020025274A8 (pt) 2023-02-14
JP7112531B2 (ja) 2022-08-03
CN121130044A (zh) 2025-12-16
MX2020013726A (es) 2021-03-02
FI3810626T3 (fi) 2025-10-21
US20250206781A1 (en) 2025-06-26
AR115597A1 (es) 2021-02-03
BR112020025274A2 (pt) 2021-03-09
EA202190086A1 (ru) 2021-05-18
HRP20251302T1 (hr) 2025-12-19
JP2021522311A (ja) 2021-08-30
AU2019290163A1 (en) 2021-01-07
JOP20190150A1 (ar) 2019-12-21
TWI840376B (zh) 2024-05-01
IL279363B2 (en) 2025-12-01
GEAP202215540A (en) 2022-12-12
CN112313243A (zh) 2021-02-02
US11427616B2 (en) 2022-08-30
SG11202012451WA (en) 2021-01-28
DK3810626T3 (da) 2025-08-18
EP4660303A3 (fr) 2026-02-25
CR20210031A (es) 2021-02-11
PE20211584A1 (es) 2021-08-18
EP3810626B1 (fr) 2025-07-23
ECSP21003643A (es) 2021-02-26
KR20210024035A (ko) 2021-03-04
AU2019290163C1 (en) 2022-11-03
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US20190389909A1 (en) 2019-12-26
PH12020552187A1 (en) 2021-07-26

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