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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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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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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (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 (https=)
EP (1) EP4573104A1 (https=)
JP (1) JP2025527471A (https=)
KR (1) KR20250048468A (https=)
CN (1) CN119731194A (https=)
AU (1) AU2023325144A1 (https=)
CO (1) CO2025001998A2 (https=)
IL (1) IL319006A (https=)
MX (1) MX2025001887A (https=)
WO (1) WO2024040125A1 (https=)

Families Citing this family (1)

* 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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019246405A1 (en) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Cyclic polypeptides for pcsk9 inhibition
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
EP4021919A1 (en) * 2019-08-30 2022-07-06 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

Also Published As

Publication number Publication date
CN119731194A (zh) 2025-03-28
IL319006A (en) 2025-04-01
EP4573104A1 (en) 2025-06-25
JP2025527471A (ja) 2025-08-22
US20260035411A1 (en) 2026-02-05
AU2023325144A1 (en) 2025-01-30
CO2025001998A2 (es) 2025-03-17
WO2024040125A1 (en) 2024-02-22
MX2025001887A (es) 2025-03-07

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PA0105 International application

Patent event date: 20250314

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application