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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- 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
-
- 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
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)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Biophysics (AREA)
- General Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (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 (25)
| Country | Link |
|---|---|
| US (2) | US11427616B2 (es) |
| EP (1) | EP3810626A1 (es) |
| JP (2) | JP7112531B2 (es) |
| KR (1) | KR20210024035A (es) |
| CN (1) | CN112313243A (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) |
| DO (1) | DOP2020000250A (es) |
| EA (1) | EA202190086A1 (es) |
| EC (1) | ECSP21003643A (es) |
| GE (1) | GEP20237506B (es) |
| IL (1) | IL279363A (es) |
| JO (1) | JOP20190150A1 (es) |
| MA (1) | MA52967A (es) |
| MX (1) | MX2020013726A (es) |
| NI (1) | NI202000101A (es) |
| PE (1) | PE20211584A1 (es) |
| PH (1) | PH12020552187A1 (es) |
| SG (1) | SG11202012451WA (es) |
| WO (1) | WO2019246349A1 (es) |
Families Citing this family (18)
| 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 |
| SG11201507226YA (en) | 2013-03-15 | 2015-10-29 | Protagonist Therapeutics Inc | Hepcidin analogues and uses therof |
| ES2890600T3 (es) | 2014-05-16 | 2022-01-20 | Protagonist Therapeutics Inc | Péptidos de tioéter antagonistas de integrina alfa4beta7 |
| BR112017001010A2 (pt) | 2014-07-17 | 2017-11-14 | Protagonist Therapeutics Inc | inibidores peptídicos orais do receptor de interleucina-23 e seu uso para tratar doenças inflamatórias intestinais |
| EP3749345A4 (en) | 2018-02-08 | 2022-04-06 | Protagonist Therapeutics, Inc. | CONJUGATED HEPCIDIN MIMETICS |
| EP3810129B1 (en) | 2018-06-21 | 2023-08-16 | Merck Sharp & Dohme LLC | Pcsk9 antagonist bicyclo-compounds |
| EP3810176A4 (en) | 2018-06-21 | 2022-05-18 | RA Pharmaceuticals, Inc. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
| EP3810196A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
| EP3810177A4 (en) | 2018-06-21 | 2022-05-11 | RA Pharmaceuticals, Inc. | CYCLIC PEPTIDES FOR PCSK9 INHIBITION |
| JOP20190150A1 (ar) | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| EP3810178A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES TO INHIBIT PCSK9 |
| WO2021041770A1 (en) * | 2019-08-30 | 2021-03-04 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist compounds |
| WO2021127460A1 (en) * | 2019-12-20 | 2021-06-24 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist compounds |
| CN118005736A (zh) | 2020-01-15 | 2024-05-10 | 詹森生物科技公司 | 介白素-23受体的肽抑制剂及其治疗炎性疾病的用途 |
| 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 |
| IL310851A (en) | 2021-08-19 | 2024-04-01 | Merck Sharp & Dohme Llc | Compounds for the treatment of diseases associated with PCSK9 activity |
| TW202404574A (zh) | 2022-06-15 | 2024-02-01 | 美商默沙東有限責任公司 | 用於捕捉介白素-1 β之環狀肽 |
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| DE3841520A1 (de) | 1988-12-09 | 1990-06-13 | Hoechst Ag | Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung |
| US5104869A (en) | 1989-10-11 | 1992-04-14 | American Cyanamid Company | Renin inhibitors |
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| US5095119A (en) | 1990-03-08 | 1992-03-10 | American Home Products Corporation | Renin inhibitors |
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| DE69910045T2 (de) | 1998-09-09 | 2004-04-22 | Metabasis Therapeutics Inc., San Diego | Neue heteroaromatische fructose 1,6-bisphosphatase inhibitoren |
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| CA2669424A1 (en) | 2006-11-07 | 2008-05-29 | Merck & Co., Inc. | Antagonists of pcsk9 |
| WO2009001836A1 (en) | 2007-06-28 | 2008-12-31 | Semiconductor Energy Laboratory Co., Ltd. | Manufacturing method of semiconductor device |
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| EP2480576A4 (en) | 2009-09-25 | 2013-04-10 | Merck Sharp & Dohme | ANTAGONISTS OF PCSK9 |
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| SG191305A1 (en) | 2010-12-28 | 2013-07-31 | Cadila Healthcare Ltd | Heterocyclic compounds suitable for the treatment of dyslipidemia |
| BR112013032667A2 (pt) * | 2011-06-20 | 2017-12-12 | Genentech Inc | polipeptídeo de ligação a pcsk9, ácido nucleico isolado, vetor, célula hospedeira, método para produzir o polipeptídeo, composição farmacêutica, método de redução do nível de colesterol ldl em um sujeito, método de tratamento de disfunção relacionada ao colesterol em um sujeito, método de tratamento de hipercolesterolemia em um sujeito, método de inibição da ligação de pcsk9 a ldlr e método de detecção da proteína pcsk9 em uma amostra |
| JP6151707B2 (ja) | 2011-10-27 | 2017-06-21 | マサチューセッツ インスティテュート オブ テクノロジー | 薬物内包微小球の形成が可能なｎ−末端で官能基化されたアミノ酸誘導体 |
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| EP2968266B1 (en) * | 2013-03-15 | 2019-05-01 | Shifa Biomedical Corporation | Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds in the treatment and/or prevention of cardiovascular diseases |
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| BR112018076242A2 (pt) | 2016-06-24 | 2019-03-26 | Hoffmann La Roche | inibidores de pcsk9, pcsk9 inibido, composição farmacêutica, métodos para modular a atividade de pcsk9, para inibir a ligação de pcsk9 a ldlr, para aumentar a disponibilidade de ldlr, para reduzir um nível de ldl-c, para reduzir o nível sérico de ldl-c, para o tratamento de um distúrbio relacionado com colesterol, métodos para o tratamento de um distúrbio associado a um nível anormal de ldl-c, de uma condição associada a um nível elevado de ldl-c, de dislipidemia, de hipercolesterolemia, usos de um inibidor de pcsk9 e método para identificar um composto candidato como um inibidor de pcsk9 que liga um epítopo da seq id nº 1 |
| US10577357B2 (en) | 2016-09-19 | 2020-03-03 | The Texas A&M University System | Inhibitors of LDLR-PCSK9 protein-protein interaction and methods of their use |
| CN107158002B (zh) * | 2017-07-01 | 2020-06-16 | 维亚生物科技(上海)有限公司 | 苄撑巴比妥类化合物在作为pcsk9拮抗剂和降低低密度脂蛋白中的应用 |
| JOP20190150A1 (ar) * | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| EP3810177A4 (en) | 2018-06-21 | 2022-05-11 | RA Pharmaceuticals, Inc. | CYCLIC PEPTIDES FOR PCSK9 INHIBITION |
| EP3810176A4 (en) | 2018-06-21 | 2022-05-18 | RA Pharmaceuticals, Inc. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
| EP3810196A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
| EP3810129B1 (en) | 2018-06-21 | 2023-08-16 | Merck Sharp & Dohme LLC | Pcsk9 antagonist bicyclo-compounds |
| EP3810178A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES TO INHIBIT PCSK9 |
| WO2021041770A1 (en) | 2019-08-30 | 2021-03-04 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist compounds |
-
2018
- 2018-06-21 JO JOP/2019/0150A patent/JOP20190150A1/ar unknown
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2019
- 2019-06-20 SG SG11202012451WA patent/SG11202012451WA/en unknown
- 2019-06-20 CN CN201980041438.5A patent/CN112313243A/zh active Pending
- 2019-06-20 PE PE2020002109A patent/PE20211584A1/es unknown
- 2019-06-20 JP JP2020570427A patent/JP7112531B2/ja active Active
- 2019-06-20 EA EA202190086A patent/EA202190086A1/ru unknown
- 2019-06-20 US US16/446,940 patent/US11427616B2/en active Active
- 2019-06-20 EP EP19739801.9A patent/EP3810626A1/en active Pending
- 2019-06-20 CA CA3102629A patent/CA3102629A1/en active Pending
- 2019-06-20 BR BR112020025274A patent/BR112020025274A8/pt unknown
- 2019-06-20 MA MA052967A patent/MA52967A/fr unknown
- 2019-06-20 MX MX2020013726A patent/MX2020013726A/es unknown
- 2019-06-20 GE GEAP201915540A patent/GEP20237506B/en unknown
- 2019-06-20 CR CR20210031A patent/CR20210031A/es unknown
- 2019-06-20 WO PCT/US2019/038155 patent/WO2019246349A1/en unknown
- 2019-06-20 AU AU2019290163A patent/AU2019290163C1/en active Active
- 2019-06-20 KR KR1020217001723A patent/KR20210024035A/ko active Search and Examination
- 2019-06-21 AR ARP190101718A patent/AR115597A1/es unknown
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2020
- 2020-12-10 IL IL279363A patent/IL279363A/en unknown
- 2020-12-14 NI NI202000101A patent/NI202000101A/es unknown
- 2020-12-16 PH PH12020552187A patent/PH12020552187A1/en unknown
- 2020-12-16 CL CL2020003257A patent/CL2020003257A1/es unknown
- 2020-12-17 DO DO2020000250A patent/DOP2020000250A/es unknown
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2021
- 2021-01-18 EC ECSENADI20213643A patent/ECSP21003643A/es unknown
- 2021-01-19 CO CONC2021/0000456A patent/CO2021000456A2/es unknown
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2022
- 2022-01-05 CL CL2022000027A patent/CL2022000027A1/es unknown
- 2022-06-30 US US17/854,379 patent/US20230159592A1/en active Pending
- 2022-07-22 JP JP2022117123A patent/JP2022141879A/ja active Pending
- 2022-10-25 AU AU2022259744A patent/AU2022259744A1/en active Pending
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