ECSP21003643A - Compuestos antagonistas de pcsk9 - Google Patents
Compuestos antagonistas de pcsk9Info
- Publication number
- ECSP21003643A ECSP21003643A ECSENADI20213643A ECDI202103643A ECSP21003643A EC SP21003643 A ECSP21003643 A EC SP21003643A EC SENADI20213643 A ECSENADI20213643 A EC SENADI20213643A EC DI202103643 A ECDI202103643 A EC DI202103643A EC SP21003643 A ECSP21003643 A EC SP21003643A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- antagonist compounds
- formula
- disclosed
- pcsk9
- 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)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se divulgan compuestos de Fórmula I, la que consta en el resumen, o una sal de los mismos: donde A, B, D, X, R1, R2 y R8 son como se definen en el presente documento, compuestos que tienen propiedades para antagonizar PCSK9. También se describen Formulaciones farmacéuticas que comprenden los compuestos de la Fórmula I o sus sales, y métodos para tratar enfermedades cardiovasculares y afecciones relacionadas con la actividad de PCSK9, ej., aterosclerosis, hipercolesterolemia, cardiopatía coronaria, síndrome metabólico, síndrome coronario agudo o enfermedad cardiovascular relacionada y afecciones cardiometabólicas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862687913P | 2018-06-21 | 2018-06-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP21003643A true ECSP21003643A (es) | 2021-02-26 |
Family
ID=67263083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI20213643A ECSP21003643A (es) | 2018-06-21 | 2021-01-18 | Compuestos antagonistas de pcsk9 |
Country Status (38)
| Country | Link |
|---|---|
| US (3) | US11427616B2 (es) |
| EP (2) | EP4660303A3 (es) |
| JP (3) | JP7112531B2 (es) |
| KR (2) | KR20250161677A (es) |
| CN (2) | CN121130044A (es) |
| AR (1) | AR115597A1 (es) |
| AU (2) | AU2019290163C1 (es) |
| BR (1) | BR112020025274A8 (es) |
| CA (1) | CA3102629A1 (es) |
| CL (2) | CL2020003257A1 (es) |
| CO (1) | CO2021000456A2 (es) |
| CR (1) | CR20210031A (es) |
| DK (1) | DK3810626T3 (es) |
| DO (1) | DOP2020000250A (es) |
| EA (1) | EA202190086A1 (es) |
| EC (1) | ECSP21003643A (es) |
| ES (1) | ES3047399T3 (es) |
| FI (1) | FI3810626T3 (es) |
| GE (2) | GEAP202215540A (es) |
| HR (1) | HRP20251302T1 (es) |
| HU (1) | HUE073367T2 (es) |
| IL (2) | IL279363B2 (es) |
| JO (1) | JOP20190150A1 (es) |
| LT (1) | LT3810626T (es) |
| MA (1) | MA52967B1 (es) |
| MD (1) | MD3810626T2 (es) |
| MX (1) | MX2020013726A (es) |
| NI (1) | NI202000101A (es) |
| PE (1) | PE20211584A1 (es) |
| PH (1) | PH12020552187A1 (es) |
| PL (1) | PL3810626T3 (es) |
| PT (1) | PT3810626T (es) |
| RS (1) | RS67338B1 (es) |
| SG (1) | SG11202012451WA (es) |
| SI (1) | SI3810626T1 (es) |
| TW (1) | TWI840376B (es) |
| UA (1) | UA129467C2 (es) |
| WO (1) | WO2019246349A1 (es) |
Families Citing this family (30)
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| KR100558932B1 (ko) * | 2005-04-21 | 2006-03-10 | 주식회사 엠제이스마트 테크놀러지 | 다공성 세라믹 분리막 제조방법과, 이에 의해 제조되어진 다공성 세라믹 분리막 |
| RS62633B1 (sr) | 2013-03-15 | 2021-12-31 | Protagonist Therapeutics Inc | Analozi hepcidina i njihove primene |
| SI3143037T1 (sl) | 2014-05-16 | 2021-11-30 | Protagonist Therapeutics, Inc. | Antagonisti integrin alpha4beta7 tioeterskih peptidov |
| CN107206254B (zh) | 2014-07-17 | 2021-08-24 | 领导医疗有限公司 | 白细胞介素-23受体的口服肽抑制剂以及其治疗炎症性肠病的用途 |
| EP4501952A3 (en) | 2018-02-08 | 2025-04-16 | Protagonist Therapeutics, Inc. | Conjugated hepcidin mimetics |
| EP3810178A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES TO INHIBIT PCSK9 |
| WO2019246386A1 (en) | 2018-06-21 | 2019-12-26 | Ra Pharmaceuticals Inc. | Cyclic polypeptides for pcsk9 inhibition |
| US11306125B2 (en) | 2018-06-21 | 2022-04-19 | Merck Sharp & Dohme Corp. | PCSK9 antagonists bicyclo-compounds |
| JOP20190150A1 (ar) * | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| ES3015132T3 (en) | 2018-06-21 | 2025-04-29 | Ucb Holdings Inc | Cyclic polypeptides for pcsk9 inhibition |
| EP3810196A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES FOR PCSK9 INHIBITION |
| TW202123960A (zh) * | 2019-08-30 | 2021-07-01 | 美商默沙東藥廠 | Pcsk9拮抗劑化合物 |
| EP4076492A4 (en) * | 2019-12-20 | 2024-01-17 | Merck Sharp & Dohme LLC | PCSK9 ANTAGONIST COMPOUNDS |
| EP4090669A4 (en) | 2020-01-15 | 2024-11-20 | Janssen Biotech, Inc. | PEPTIDE INHIBITORS OF THE INTERLEUKIN-23 RECEPTOR AND THEIR USE IN TREATING INFLAMMATORY DISEASES |
| SI4090670T1 (sl) | 2020-01-15 | 2025-08-29 | Janssen Biotech, Inc. | Peptidni zaviralci receptorja interlevkina-23 in njihova uporaba za zdravljenje vnetnih bolezni |
| IL316550A (en) | 2020-11-20 | 2024-12-01 | Janssen Pharmaceutica Nv | Compositions of interleukin-23 receptor peptide inhibitors |
| US11932705B2 (en) | 2020-12-18 | 2024-03-19 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| IL310061A (en) | 2021-07-14 | 2024-03-01 | Janssen Biotech Inc | Peptide inhibitors linked to fatty residues of the interleukin-23 receptor |
| IL310851A (en) * | 2021-08-19 | 2024-04-01 | Merck Sharp & Dohme Llc | Compounds for the treatment of diseases associated with PCSK9 activity |
| US20230406885A1 (en) | 2022-06-15 | 2023-12-21 | Merck Sharp & Dohme Llc | Cyclic peptides for trapping interleukin-1 beta |
| US20260035411A1 (en) * | 2022-08-17 | 2026-02-05 | Merck Sharp & Dohme Llc | Crystalline forms of a pcsk9 inhibitor, compositions and uses |
| WO2024259310A2 (en) * | 2023-06-15 | 2024-12-19 | Merck Sharp & Dohme Llc | Passive permeable pcsk9 antagonist compounds |
| WO2025106386A1 (en) | 2023-11-14 | 2025-05-22 | Merck Sharp & Dohme Llc | A cyclic peptide for trapping interleukin-1 beta |
| TW202542176A (zh) | 2023-12-15 | 2025-11-01 | 美商默沙東有限責任公司 | 用於治療動脈粥樣硬化及發炎病症之環狀肽IL-1β捕捉劑 |
| WO2025242221A1 (zh) * | 2024-05-24 | 2025-11-27 | 上海翰森生物医药科技有限公司 | 新型修饰侧链、其制备方法和应用 |
| WO2025264781A1 (en) * | 2024-06-18 | 2025-12-26 | Kemira Oy J | Cationizing agents for saccharides and methods |
| WO2026019622A1 (en) * | 2024-07-15 | 2026-01-22 | Merck Sharp & Dohme Llc | Crystal forms of a cyclictetrapeptide and processes for preparing |
| 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 |
| WO2026034639A1 (ja) * | 2024-08-09 | 2026-02-12 | 株式会社Spin Wave | ペプチド合成用可溶性担体およびこれを用いた合成方法 |
| 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 |
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| EP3810178A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES TO INHIBIT PCSK9 |
| TW202123960A (zh) | 2019-08-30 | 2021-07-01 | 美商默沙東藥廠 | Pcsk9拮抗劑化合物 |
| EP4076492A4 (en) | 2019-12-20 | 2024-01-17 | Merck Sharp & Dohme LLC | PCSK9 ANTAGONIST COMPOUNDS |
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2018
- 2018-06-21 JO JOP/2019/0150A patent/JOP20190150A1/ar unknown
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2019
- 2019-06-20 AU AU2019290163A patent/AU2019290163C1/en active Active
- 2019-06-20 DK DK19739801.9T patent/DK3810626T3/da active
- 2019-06-20 PE PE2020002109A patent/PE20211584A1/es unknown
- 2019-06-20 CA CA3102629A patent/CA3102629A1/en active Pending
- 2019-06-20 LT LTEPPCT/US2019/038155T patent/LT3810626T/lt unknown
- 2019-06-20 US US16/446,940 patent/US11427616B2/en active Active
- 2019-06-20 HR HRP20251302TT patent/HRP20251302T1/hr unknown
- 2019-06-20 BR BR112020025274A patent/BR112020025274A8/pt unknown
- 2019-06-20 WO PCT/US2019/038155 patent/WO2019246349A1/en not_active Ceased
- 2019-06-20 MA MA52967A patent/MA52967B1/fr unknown
- 2019-06-20 HU HUE19739801A patent/HUE073367T2/hu unknown
- 2019-06-20 GE GEAP202215540A patent/GEAP202215540A/en unknown
- 2019-06-20 JP JP2020570427A patent/JP7112531B2/ja active Active
- 2019-06-20 CR CR20210031A patent/CR20210031A/es unknown
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