JP7866141B2 - Ｐｃｓｋ９阻害薬の結晶形態、組成物及び使用 - Google Patents

Ｐｃｓｋ９阻害薬の結晶形態、組成物及び使用

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Publication number
JP7866141B2
JP7866141B2 JP2025508431A JP2025508431A JP7866141B2 JP 7866141 B2 JP7866141 B2 JP 7866141B2 JP 2025508431 A JP2025508431 A JP 2025508431A JP 2025508431 A JP2025508431 A JP 2025508431A JP 7866141 B2 JP7866141 B2 JP 7866141B2
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caprate
formula
crystalline form
compound represented
approximately
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English (en)
Japanese (ja)
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JP2025527471A5 (enExample
JP2025527471A (ja
Inventor
コン，ジョンロック
ヴァルソロナ，リチャード・ジェイ
デズモンド，リチャード
マリグレス，ピーター・イー
ツァイ，フー－ロン
シーパーマン，カルロス・アルベルト・ポンス
クラパルス，アーティス
ロビンソン，リー
リー，アルフレッド
ピウ，ティファニー
コダン，ロレンツォ
ラーペント，パトリック
Original Assignee
メルク・シャープ・アンド・ドーム・エルエルシー
ヴェルテンシュタイン・バイオファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
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    • 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
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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)
JP2025508431A 2022-08-17 2023-08-16 Ｐｃｓｋ９阻害薬の結晶形態、組成物及び使用 Active JP7866141B2 (ja)

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 (3)

Publication Number Publication Date
JP2025527471A JP2025527471A (ja) 2025-08-22
JP2025527471A5 JP2025527471A5 (enExample) 2025-12-23
JP7866141B2 true JP7866141B2 (ja) 2026-05-26

Family

ID=89942405

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2025508431A Active JP7866141B2 (ja) 2022-08-17 2023-08-16 Ｐｃｓｋ９阻害薬の結晶形態、組成物及び使用

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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20210069288A1 (en) 2019-08-30 2021-03-11 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds
US20210214395A1 (en) 2018-06-21 2021-07-15 Merck Sharp & Dohme Corp. Pcsk9 antagonists bicyclo-compounds
JP2021522311A (ja) 2018-06-21 2021-08-30 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｐｃｓｋ９アンタゴニスト化合物
US20210284694A1 (en) 2018-06-21 2021-09-16 Merck Sharp & Dohme Corp. Cyclic polypeptides for pcsk9 inhibition

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20210214395A1 (en) 2018-06-21 2021-07-15 Merck Sharp & Dohme Corp. Pcsk9 antagonists bicyclo-compounds
JP2021522311A (ja) 2018-06-21 2021-08-30 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｐｃｓｋ９アンタゴニスト化合物
US20210284694A1 (en) 2018-06-21 2021-09-16 Merck Sharp & Dohme Corp. Cyclic polypeptides for pcsk9 inhibition
US20210069288A1 (en) 2019-08-30 2021-03-11 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
薬剤学，2008年，Vol.68, No.5，p.344-349

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
US20260035411A1 (en) 2026-02-05
KR20250048468A (ko) 2025-04-08
IL319006A (en) 2025-04-01

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