CO2025001998A2 - Formas cristalinas de un inhibidor de la pcsk9, composiciones y usos - Google Patents

Formas cristalinas de un inhibidor de la pcsk9, composiciones y usos

Info

Publication number
CO2025001998A2
CO2025001998A2 CONC2025/0001998A CO2025001998A CO2025001998A2 CO 2025001998 A2 CO2025001998 A2 CO 2025001998A2 CO 2025001998 A CO2025001998 A CO 2025001998A CO 2025001998 A2 CO2025001998 A2 CO 2025001998A2
Authority
CO
Colombia
Prior art keywords
disease
compositions
crystal forms
methods
pcsk9 inhibitor
Prior art date
Application number
CONC2025/0001998A
Other languages
English (en)
Spanish (es)
Inventor
Jongrock Kong
Richard J Varsolona
Richard Desmond
Peter E Maligres
Fuh-Rong Tsay
Carlos Alberto Pons Siepermann
Artis Klapars
Lee Robison
Alfred Lee
Tiffany Piou
Lorenzo Codan
Patrick Larpent
Original Assignee
Merck Sharp & Dohme Llc
Werthenstein Biopharma Gmbh
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, Werthenstein Biopharma Gmbh filed Critical Merck Sharp & Dohme Llc
Publication of CO2025001998A2 publication Critical patent/CO2025001998A2/es

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
    • 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)
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CONC2025/0001998A 2022-08-17 2025-02-25 Formas cristalinas de un inhibidor de la pcsk9, composiciones y usos CO2025001998A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202263371690P 2022-08-17 2022-08-17
US202263384298P 2022-11-18 2022-11-18
PCT/US2023/072326 WO2024040125A1 (en) 2022-08-17 2023-08-16 Crystalline forms of a pcsk9 inhibitor, compositions and uses

Publications (1)

Publication Number Publication Date
CO2025001998A2 true CO2025001998A2 (es) 2025-03-17

Family

ID=89942405

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2025/0001998A CO2025001998A2 (es) 2022-08-17 2025-02-25 Formas cristalinas de un inhibidor de la pcsk9, composiciones y usos

Country Status (10)

Country Link
US (1) US20260035411A1 (enExample)
EP (1) EP4573104A4 (enExample)
JP (1) JP7866141B2 (enExample)
KR (1) KR20250048468A (enExample)
CN (1) CN119731194A (enExample)
AU (1) AU2023325144A1 (enExample)
CO (1) CO2025001998A2 (enExample)
IL (1) IL319006A (enExample)
MX (1) MX2025001887A (enExample)
WO (1) WO2024040125A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026032253A1 (zh) * 2024-08-06 2026-02-12 石药集团中奇制药技术（石家庄）有限公司 环肽类似物及其制备方法和用途
WO2026101894A1 (en) * 2024-11-07 2026-05-15 Merck Sharp & Dohme Llc Process for preparing a peptide

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20250161677A (ko) 2018-06-21 2025-11-17 머크 샤프 앤드 돔 엘엘씨 Pcsk9 길항제 화합물
EP3810129B1 (en) 2018-06-21 2023-08-16 Merck Sharp & Dohme LLC Pcsk9 antagonist bicyclo-compounds
WO2019246405A1 (en) 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Cyclic polypeptides for pcsk9 inhibition
EP4021919A1 (en) * 2019-08-30 2022-07-06 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

Also Published As

Publication number Publication date
EP4573104A4 (en) 2026-08-05
WO2024040125A1 (en) 2024-02-22
AU2023325144A1 (en) 2025-01-30
MX2025001887A (es) 2025-03-07
JP2025527471A (ja) 2025-08-22
EP4573104A1 (en) 2025-06-25
CN119731194A (zh) 2025-03-28
JP7866141B2 (ja) 2026-05-26
US20260035411A1 (en) 2026-02-05
KR20250048468A (ko) 2025-04-08
IL319006A (en) 2025-04-01

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