MA52967B1 - Composés antagonistes du pcsk9 - Google Patents
Composés antagonistes du pcsk9Info
- Publication number
- MA52967B1 MA52967B1 MA52967A MA52967A MA52967B1 MA 52967 B1 MA52967 B1 MA 52967B1 MA 52967 A MA52967 A MA 52967A MA 52967 A MA52967 A MA 52967A MA 52967 B1 MA52967 B1 MA 52967B1
- Authority
- MA
- Morocco
- Prior art keywords
- compounds
- antagonist compounds
- pcsk9 antagonist
- pcsk9
- formula
- Prior art date
Links
Classifications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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)
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
L'invention concerne des composés de formule I, ou un sel de ceux-ci, formule dans laquelle A, B, D, X, R1, R2 et R8 sont tels que définis dans la description, lesdits composés présentant des propriétés antagonistes au niveau du PCSK9. L'invention concerne également des formulations pharmaceutiques comprenant les composés de formule I ou leurs sels, et des procédés de traitement de maladies cardiovasculaires et d'états liés à l'activité du PCSK9, par exemple l'athérosclérose, l'hypercholestérolémie, la coronaropathie, le syndrome métabolique, le syndrome coronarien aigu ou les maladies cardiovasculaires et cardiométaboliques associées.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862687913P | 2018-06-21 | 2018-06-21 | |
| EP19739801.9A EP3810626B1 (fr) | 2018-06-21 | 2019-06-20 | Composés antagonistes du pcsk9 |
| PCT/US2019/038155 WO2019246349A1 (fr) | 2018-06-21 | 2019-06-20 | Composés antagonistes du pcsk9 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA52967A MA52967A (fr) | 2021-04-28 |
| MA52967B1 true MA52967B1 (fr) | 2025-09-30 |
Family
ID=67263083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA52967A MA52967B1 (fr) | 2018-06-21 | 2019-06-20 | Composés antagonistes du pcsk9 |
Country Status (38)
| Country | Link |
|---|---|
| US (3) | US11427616B2 (fr) |
| EP (2) | EP4660303A3 (fr) |
| JP (3) | JP7112531B2 (fr) |
| KR (2) | KR20250161677A (fr) |
| CN (2) | CN112313243B (fr) |
| AR (1) | AR115597A1 (fr) |
| AU (2) | AU2019290163C1 (fr) |
| BR (1) | BR112020025274A8 (fr) |
| CA (1) | CA3102629A1 (fr) |
| CL (2) | CL2020003257A1 (fr) |
| CO (1) | CO2021000456A2 (fr) |
| CR (1) | CR20210031A (fr) |
| DK (1) | DK3810626T3 (fr) |
| DO (1) | DOP2020000250A (fr) |
| EA (1) | EA202190086A1 (fr) |
| EC (1) | ECSP21003643A (fr) |
| ES (1) | ES3047399T3 (fr) |
| FI (1) | FI3810626T3 (fr) |
| GE (2) | GEP20237506B (fr) |
| HR (1) | HRP20251302T1 (fr) |
| HU (1) | HUE073367T2 (fr) |
| IL (2) | IL279363B2 (fr) |
| JO (1) | JOP20190150A1 (fr) |
| LT (1) | LT3810626T (fr) |
| MA (1) | MA52967B1 (fr) |
| MD (1) | MD3810626T2 (fr) |
| MX (1) | MX2020013726A (fr) |
| NI (1) | NI202000101A (fr) |
| PE (1) | PE20211584A1 (fr) |
| PH (1) | PH12020552187A1 (fr) |
| PL (1) | PL3810626T3 (fr) |
| PT (1) | PT3810626T (fr) |
| RS (1) | RS67338B1 (fr) |
| SG (1) | SG11202012451WA (fr) |
| SI (1) | SI3810626T1 (fr) |
| TW (1) | TWI840376B (fr) |
| UA (1) | UA129467C2 (fr) |
| WO (1) | WO2019246349A1 (fr) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100558932B1 (ko) * | 2005-04-21 | 2006-03-10 | 주식회사 엠제이스마트 테크놀러지 | 다공성 세라믹 분리막 제조방법과, 이에 의해 제조되어진 다공성 세라믹 분리막 |
| EP4091624A1 (fr) | 2013-03-15 | 2022-11-23 | Protagonist Therapeutics, Inc. | Analogues d'hepcidine et leurs utilisations |
| CA2949215C (fr) | 2014-05-16 | 2023-03-14 | Protagonist Therapeutics, Inc. | Antagonistes du peptide thioether .alpha.4.beta.7 integrine |
| SG10201810154WA (en) | 2014-07-17 | 2018-12-28 | Protagonist Therapeutics Inc | Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases |
| WO2018022937A1 (fr) | 2016-07-27 | 2018-02-01 | Protagonist Therapeutics, Inc. | Inhibiteurs peptidiques de l'interleukine-23 et leur utilisation dans le traitement des maladies inflammatoires |
| WO2019157268A1 (fr) | 2018-02-08 | 2019-08-15 | Protagonist Therapeutics, Inc. | Mimétiques d'hepcidine conjugués |
| US11814444B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
| KR20250161677A (ko) | 2018-06-21 | 2025-11-17 | 머크 샤프 앤드 돔 엘엘씨 | Pcsk9 길항제 화합물 |
| EP3810129B1 (fr) | 2018-06-21 | 2023-08-16 | Merck Sharp & Dohme LLC | Composés bicycliques antagonistes de pcsk9 |
| EP3810178A4 (fr) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | Polypeptides cycliques pour l'inhibition de la pcsk9 |
| WO2019246405A1 (fr) | 2018-06-21 | 2019-12-26 | Merck Sharp & Dohme Corp. | Polypeptides cycliques pour l'inhibition de la pcsk9 |
| ES3015132T3 (en) | 2018-06-21 | 2025-04-29 | Ucb Holdings Inc | Cyclic polypeptides for pcsk9 inhibition |
| EP4021919A1 (fr) | 2019-08-30 | 2022-07-06 | Merck Sharp & Dohme Corp. | Composés antagonistes du pcsk9 |
| US12577259B2 (en) | 2019-12-20 | 2026-03-17 | Merck Sharp & Dohme Llc | PCSK9 antagonist compounds |
| SMT202500254T1 (it) | 2020-01-15 | 2025-09-12 | Janssen Biotech Inc | Inibitori peptidici del recettore dell'interleuchina-23 e loro uso per trattare malattie infiammatorie |
| MX2022008740A (es) | 2020-01-15 | 2022-09-23 | Janssen Biotech Inc | Peptidos inhibidores del receptor de interleucina-23 y su uso para tratar enfermedades inflamatorias. |
| AU2021383828A1 (en) | 2020-11-20 | 2023-07-06 | Janssen Pharmaceutica Nv | Compositions of peptide inhibitors of interleukin-23 receptor |
| US11932705B2 (en) | 2020-12-18 | 2024-03-19 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| KR20240034224A (ko) | 2021-07-14 | 2024-03-13 | 얀센 바이오테크 인코포레이티드 | 인터류킨-23 수용체의 지질화된 펩티드 억제제 |
| MX2024002146A (es) * | 2021-08-19 | 2024-03-08 | Merck Sharp & Dohme Llc | Compuestos para el tratamiento de afecciones relacionadas con la actividad de pcsk9. |
| SI4540267T1 (sl) | 2022-06-15 | 2026-07-31 | Merck Sharp & Dohme Llc | Ciklični peptidi za ujetje interlevkina-1 beta |
| JP7866141B2 (ja) * | 2022-08-17 | 2026-05-26 | メルク・シャープ・アンド・ドーム・エルエルシー | Pcsk9阻害薬の結晶形態、組成物及び使用 |
| WO2024259310A2 (fr) * | 2023-06-15 | 2024-12-19 | Merck Sharp & Dohme Llc | Composés antagonistes de pcsk9 perméables passifs |
| IL328311A (en) | 2023-11-14 | 2026-07-01 | Merck Sharp & Dohme Llc | Cyclic peptide for capturing Interleukin-1 Beta |
| AU2024401721A1 (en) | 2023-12-15 | 2026-07-16 | Merck Sharp & Dohme Llc | A cyclic peptide il-1beta trap for the treatment of atherosclerosis and inflammatory disorders |
| WO2025242221A1 (fr) * | 2024-05-24 | 2025-11-27 | 上海翰森生物医药科技有限公司 | Nouvelle chaîne latérale modifiée, son procédé de préparation et son utilisation |
| WO2025264781A1 (fr) * | 2024-06-18 | 2025-12-26 | Kemira Oy J | Agents de cationisation pour saccharides et procédés |
| WO2026019622A1 (fr) * | 2024-07-15 | 2026-01-22 | Merck Sharp & Dohme Llc | Formes cristallines d'un cyclictétrapeptide et procédés de préparation |
| WO2026019624A1 (fr) * | 2024-07-15 | 2026-01-22 | Merck Sharp & Dohme Llc | Synthèse d'oligopeptides cycliques |
| WO2026032253A1 (fr) * | 2024-08-06 | 2026-02-12 | 石药集团中奇制药技术(石家庄)有限公司 | Analogue de peptide cyclique, son procédé de préparation et son utilisation |
| WO2026034639A1 (fr) * | 2024-08-09 | 2026-02-12 | 株式会社Spin Wave | Excipient soluble pour la synthèse de peptides et procédé de synthèse l'utilisant |
| CN119930471A (zh) * | 2024-12-31 | 2025-05-06 | 苏州默迪夫生物科技有限公司 | Mk-a的制备方法、所用的中间体及其合成方法 |
| CN122464947A (zh) * | 2025-01-25 | 2026-07-28 | 深圳市祥根生物有限公司 | 一种环肽类pcsk9抑制剂和用途 |
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| WO2019246405A1 (fr) | 2018-06-21 | 2019-12-26 | Merck Sharp & Dohme Corp. | Polypeptides cycliques pour l'inhibition de la pcsk9 |
| ES3015132T3 (en) | 2018-06-21 | 2025-04-29 | Ucb Holdings Inc | Cyclic polypeptides for pcsk9 inhibition |
| KR20250161677A (ko) | 2018-06-21 | 2025-11-17 | 머크 샤프 앤드 돔 엘엘씨 | Pcsk9 길항제 화합물 |
| US11814444B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
| EP3810178A4 (fr) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | Polypeptides cycliques pour l'inhibition de la pcsk9 |
| EP3810129B1 (fr) | 2018-06-21 | 2023-08-16 | Merck Sharp & Dohme LLC | Composés bicycliques antagonistes de pcsk9 |
| EP4021919A1 (fr) | 2019-08-30 | 2022-07-06 | Merck Sharp & Dohme Corp. | Composés antagonistes du pcsk9 |
| US12577259B2 (en) | 2019-12-20 | 2026-03-17 | Merck Sharp & Dohme Llc | PCSK9 antagonist compounds |
-
2019
- 2019-06-20 KR KR1020257037305A patent/KR20250161677A/ko active Pending
- 2019-06-20 IL IL279363A patent/IL279363B2/en unknown
- 2019-06-20 MD MDE20210407T patent/MD3810626T2/ro unknown
- 2019-06-20 SG SG11202012451WA patent/SG11202012451WA/en unknown
- 2019-06-20 GE GEAP201915540A patent/GEP20237506B/en unknown
- 2019-06-20 RS RS20251040A patent/RS67338B1/sr unknown
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