EP4727552A2 - Composés antagonistes de pcsk9 perméables passifs - Google Patents

Composés antagonistes de pcsk9 perméables passifs

Info

Publication number
EP4727552A2
EP4727552A2 EP24824271.1A EP24824271A EP4727552A2 EP 4727552 A2 EP4727552 A2 EP 4727552A2 EP 24824271 A EP24824271 A EP 24824271A EP 4727552 A2 EP4727552 A2 EP 4727552A2
Authority
EP
European Patent Office
Prior art keywords
mmol
added
int
synthesis
afford
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
EP24824271.1A
Other languages
German (de)
English (en)
Inventor
Abbas M. Walji
Harold B. Wood
Yuhua Huang
Thomas Joseph Tucker
Yi-Heng Chen
Mark W. Embrey
Fa-Xiang Ding
Jennifer HANISAK
Charles Lee Jayne
Chengwei WU
Jennifer Marie JOHNSTON
Shawn P. Walsh
Zhongxiang Sun
Danila Branca
Stefania Colarusso
Anilkumar G. Nair
Michael Man-Chu Lo
Peter Orth
Sookhee Nicole Ha
Liangqin Guo
Ling Tong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and 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 and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of EP4727552A2 publication Critical patent/EP4727552A2/fr
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Landscapes

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

Abstract

Des composés de formule (I), ou un sel pharmaceutiquement acceptable de ceux-ci (I), où A, B, R1, R2, R3, R4 et<sp />R5 sont tels que définis dans la description. Ces composés sont des antagonistes de PCSK9 et ont une perméabilité passive (ou intrinsèque) élevée de telle sorte qu'ils peuvent être utilisés sans agent d'amélioration de la perméabilité. L'invention concerne également des compositions pharmaceutiques comprenant les composés de formule I ou leurs sels, et des méthodes 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.
EP24824271.1A 2023-06-15 2024-06-14 Composés antagonistes de pcsk9 perméables passifs Pending EP4727552A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202363508454P 2023-06-15 2023-06-15
US202363517742P 2023-08-04 2023-08-04
PCT/US2024/034113 WO2024259310A2 (fr) 2023-06-15 2024-06-14 Composés antagonistes de pcsk9 perméables passifs

Publications (1)

Publication Number Publication Date
EP4727552A2 true EP4727552A2 (fr) 2026-04-22

Family

ID=93852845

Family Applications (1)

Application Number Title Priority Date Filing Date
EP24824271.1A Pending EP4727552A2 (fr) 2023-06-15 2024-06-14 Composés antagonistes de pcsk9 perméables passifs

Country Status (2)

Country Link
EP (1) EP4727552A2 (fr)
WO (1) WO2024259310A2 (fr)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3810177B1 (fr) * 2018-06-21 2024-12-04 Ra Pharmaceuticals, Inc. Peptides cycliques pour l'inhibition de la pcsk9
US11306125B2 (en) * 2018-06-21 2022-04-19 Merck Sharp & Dohme Corp. PCSK9 antagonists bicyclo-compounds
IL279363B2 (en) * 2018-06-21 2025-12-01 Merck Sharp & Dohme Pcsk9 antagonist compounds

Also Published As

Publication number Publication date
WO2024259310A3 (fr) 2025-01-16
WO2024259310A2 (fr) 2024-12-19

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