JP2025527471A - 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

Info

Publication number
JP2025527471A
JP2025527471A JP2025508431A JP2025508431A JP2025527471A JP 2025527471 A JP2025527471 A JP 2025527471A JP 2025508431 A JP2025508431 A JP 2025508431A JP 2025508431 A JP2025508431 A JP 2025508431A JP 2025527471 A JP2025527471 A JP 2025527471A
Authority
JP
Japan
Prior art keywords
caprate
crystalline form
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
JP2025508431A
Other languages
English (en)
Japanese (ja)
Other versions
JP2025527471A5 (https=
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
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 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 filed Critical メルク・シャープ・アンド・ドーム・エルエルシー
Publication of JP2025527471A publication Critical patent/JP2025527471A/ja
Publication of JP2025527471A5 publication Critical patent/JP2025527471A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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

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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2025508431A 2022-08-17 2023-08-16 Ｐｃｓｋ９阻害薬の結晶形態、組成物及び使用 Pending JP2025527471A (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 (2)

Publication Number Publication Date
JP2025527471A true JP2025527471A (ja) 2025-08-22
JP2025527471A5 JP2025527471A5 (https=) 2025-12-23

Family

ID=89942405

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2025508431A Pending JP2025527471A (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 (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

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, vol. 68, no. 5, JPN6022055481, 2008, pages 344 - 349, ISSN: 0005823333 *

Also Published As

Publication number Publication date
CN119731194A (zh) 2025-03-28
IL319006A (en) 2025-04-01
EP4573104A1 (en) 2025-06-25
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

Similar Documents

Publication Publication Date Title
AU2023200978B2 (en) Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
EP3222277B1 (en) A biphenylsulfonamide endothelin and angiotensin ii receptor antagonist to treat glomerulosclerosis and iga-induced nephropathy
US10898471B2 (en) Methods of inhibiting leukotriene A4 hydrolase
CA2716914A1 (en) Novel crystalline forms of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide sodium salt
TWI458481B (zh) ３－戊基苯乙酸的鹽及其藥學用途
WO2015108038A1 (ja) エチレングリコール化合物
US20260035411A1 (en) Crystalline forms of a pcsk9 inhibitor, compositions and uses
TW202515556A (zh) Ｓｌｃ６ａ１９功能之含萘基哌啶抑制劑
US20240238367A1 (en) Compounds for treating conditions related to pcsk9 activity
US20240207264A1 (en) Pharmaceutical compositions comprising inhibitors of the androgen receptor and uses thereof
KR20230027388A (ko) 지방간염, 지방증 또는 섬유증의 예방 또는 치료용 복합 제제
EP2590973B1 (en) Solifenacin salts
EA045975B1 (ru) Кристаллическая l-аргининовая соль (r)-2-(7-(4-циклопентил-3-(трифторметил)бензилокси)-1,2,3,4-тетрагидроциклопента[b]индол-3-ил)уксусной кислоты (соединения 1) для применения при расстройствах, связанных с s1p1-рецептором
HK1198010A (en) A biphenylsulfonamide endothelin and angiotensin ii receptor antagonist to treat glomerulosclerosis
HK1198010B (en) A biphenylsulfonamide endothelin and angiotensin ii receptor antagonist to treat glomerulosclerosis
HK1244687B (en) A biphenylsulfonamide endothelin and angiotensin ii receptor antagonist to treat glomerulosclerosis and iga-induced nephropathy
EP3184095A1 (en) Administration units comprising polymorph 1 of 2-(2-methylamino-pyrimidin-4-yl]-1h-indole-5-carboxylic acid [(s)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20251215

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20251215

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20251215

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20260113

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260313

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20260324

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260415

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20260421