KR20250048468A - Pcsk9 억제제의 결정질 형태, 조성물 및 용도 - Google Patents

Pcsk9 억제제의 결정질 형태, 조성물 및 용도 Download PDF

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Publication number
KR20250048468A
KR20250048468A KR1020257008518A KR20257008518A KR20250048468A KR 20250048468 A KR20250048468 A KR 20250048468A KR 1020257008518 A KR1020257008518 A KR 1020257008518A KR 20257008518 A KR20257008518 A KR 20257008518A KR 20250048468 A KR20250048468 A KR 20250048468A
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KR
South Korea
Prior art keywords
caprate
crystalline form
compound
formula
ray powder
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Pending
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KR1020257008518A
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English (en)
Korean (ko)
Inventor
종락 공
리차드 제이. 바르솔로나
리차드 데스몬드
피터 이. 말리그레스
푸롱 차이
카를로스 알베르토 폰스 시퍼만
아르티스 크라파르스
리 로비슨
알프레드 리
티파니 피우
로렌조 코단
패트릭 라르펜트
Original Assignee
머크 샤프 앤드 돔 엘엘씨
베르텐스타인 바이오파마 게엠베하
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Application filed by 머크 샤프 앤드 돔 엘엘씨, 베르텐스타인 바이오파마 게엠베하 filed Critical 머크 샤프 앤드 돔 엘엘씨
Publication of KR20250048468A publication Critical patent/KR20250048468A/ko
Pending legal-status Critical Current

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    • 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

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  • 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)
KR1020257008518A 2022-08-17 2023-08-16 Pcsk9 억제제의 결정질 형태, 조성물 및 용도 Pending KR20250048468A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202263371690P 2022-08-17 2022-08-17
US63/371,690 2022-08-17
US202263384298P 2022-11-18 2022-11-18
US63/384,298 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
KR20250048468A true KR20250048468A (ko) 2025-04-08

Family

ID=89942405

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020257008518A Pending KR20250048468A (ko) 2022-08-17 2023-08-16 Pcsk9 억제제의 결정질 형태, 조성물 및 용도

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
CO2025001998A2 (es) 2025-03-17
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
IL319006A (en) 2025-04-01

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P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000