CN119731194A - Pcsk9抑制剂的结晶形式、组合物及用途 - Google Patents

Pcsk9抑制剂的结晶形式、组合物及用途 Download PDF

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Publication number
CN119731194A
CN119731194A CN202380059715.1A CN202380059715A CN119731194A CN 119731194 A CN119731194 A CN 119731194A CN 202380059715 A CN202380059715 A CN 202380059715A CN 119731194 A CN119731194 A CN 119731194A
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CN
China
Prior art keywords
crystalline form
caprate
compound
formula
ray powder
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
CN202380059715.1A
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English (en)
Chinese (zh)
Inventor
J·孔
R·J·瓦尔索罗纳
R·德斯蒙德
P·E·马利格雷斯
蔡富蓉
C·A·P·西佩尔曼
A·克拉帕斯
L·罗比森
A·李
T·皮欧
L·科丹
P·拉彭特
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.)
Weltenstein Biopharmaceutical Co
Merck Sharp and Dohme BV
Original Assignee
Weltenstein Biopharmaceutical Co
Merck Sharp and Dohme BV
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 Weltenstein Biopharmaceutical Co, Merck Sharp and Dohme BV filed Critical Weltenstein Biopharmaceutical Co
Publication of CN119731194A publication Critical patent/CN119731194A/zh
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)
CN202380059715.1A 2022-08-17 2023-08-16 Pcsk9抑制剂的结晶形式、组合物及用途 Pending CN119731194A (zh)

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
CN119731194A true CN119731194A (zh) 2025-03-28

Family

ID=89942405

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202380059715.1A Pending CN119731194A (zh) 2022-08-17 2023-08-16 Pcsk9抑制剂的结晶形式、组合物及用途

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
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
KR20250048468A (ko) 2025-04-08
CO2025001998A2 (es) 2025-03-17
WO2024040125A1 (en) 2024-02-22
MX2025001887A (es) 2025-03-07

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