DOP2020000250A - Compuestos antagonistas de la pcsk9 - Google Patents
Compuestos antagonistas de la pcsk9Info
- Publication number
- DOP2020000250A DOP2020000250A DO2020000250A DO2020000250A DOP2020000250A DO P2020000250 A DOP2020000250 A DO P2020000250A DO 2020000250 A DO2020000250 A DO 2020000250A DO 2020000250 A DO2020000250 A DO 2020000250A DO P2020000250 A DOP2020000250 A DO P2020000250A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- compounds
- pcsk9
- formula
- antagonist compounds
- conditions
- 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 describen compuestos de Fórmula I, o una sal de los mismos: Formula I, donde A, B, D, X, R1, R2 y R8 son como se definen en la presente solicitud, compuestos que tienen propiedades para antagonizar PCSK9. También se describen formulaciones farmacéuticas que comprenden los compuestos de Fórmula I o sus sales, y procedimientos para la fabricación de medicamentos útiles para tratar enfermedades cardiovasculares y condiciones relacionadas con la actividad de PCSK9, por ejemplo, aterosclerosis, hipercolesterolemia, enfermedad cardíaca coronaria, síndrome metabólico, síndrome coronario agudo o enfermedad cardiovascular relacionada y condiciones cardiometabólicas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862687913P | 2018-06-21 | 2018-06-21 | |
| PCT/US2019/038155 WO2019246349A1 (en) | 2018-06-21 | 2019-06-20 | Pcsk9 antagonist compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DOP2020000250A true DOP2020000250A (es) | 2021-02-28 |
Family
ID=67263083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DO2020000250A DOP2020000250A (es) | 2018-06-21 | 2020-12-17 | Compuestos antagonistas de la pcsk9 |
Country Status (26)
| 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) |
| TW (1) | TWI840376B (es) |
| WO (1) | WO2019246349A1 (es) |
Families Citing this family (19)
| 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 |
| PT2968443T (pt) | 2013-03-15 | 2021-12-28 | Protagonist Therapeutics Inc | Análogos de hepcidina e seus usos |
| LT3143037T (lt) | 2014-05-16 | 2021-10-11 | Protagonist Therapeutics, Inc. | Alfa4beta7 integrino tioeterio peptidų antagonistaii |
| 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 |
| 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 |
| US11505575B2 (en) | 2018-06-21 | 2022-11-22 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| US11530244B2 (en) | 2018-06-21 | 2022-12-20 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| JOP20190150A1 (ar) * | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| EP3810176A4 (en) | 2018-06-21 | 2022-05-18 | RA Pharmaceuticals, Inc. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
| EP3810177A4 (en) | 2018-06-21 | 2022-05-11 | RA Pharmaceuticals, Inc. | CYCLIC PEPTIDES FOR PCSK9 INHIBITION |
| 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 |
| 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. |
| US11845808B2 (en) | 2020-01-15 | 2023-12-19 | Janssen Biotech, Inc. | Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases |
| IL302996A (en) | 2020-11-20 | 2023-07-01 | Janssen Pharmaceutica Nv | Compositions of peptide inhibitors of the interleukin-23 receptor |
| US11932705B2 (en) | 2020-12-18 | 2024-03-19 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| MX2024002146A (es) | 2021-08-19 | 2024-03-08 | Merck Sharp & Dohme Llc | Compuestos para el tratamiento de afecciones relacionadas con la actividad de pcsk9. |
| WO2023244554A1 (en) | 2022-06-15 | 2023-12-21 | Merck Sharp & Dohme Llc | Cyclic peptides for trapping interleukin-1 beta |
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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 |
| US5114937A (en) | 1989-11-28 | 1992-05-19 | Warner-Lambert Company | Renin inhibiting nonpeptides |
| US5095119A (en) | 1990-03-08 | 1992-03-10 | American Home Products Corporation | Renin inhibitors |
| ATE253073T1 (de) | 1997-03-07 | 2003-11-15 | Metabasis Therapeutics Inc | Neue benzimidazol inhibitoren der fructose-1,6- bisphosphatase |
| US6284748B1 (en) | 1997-03-07 | 2001-09-04 | Metabasis Therapeutics, Inc. | Purine inhibitors of fructose 1,6-bisphosphatase |
| AU6691798A (en) | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| SK286080B6 (sk) | 1998-09-09 | 2008-03-05 | Metabasis Therapeutics, Inc. | Heterocyklické aromatické zlúčeniny obsahujúce fosfonátovú skupinu, ich použitie a farmaceutická kompozícia obsahujúca uvedené zlúčeniny |
| DE60128475T2 (de) | 2000-07-25 | 2008-02-07 | Merck & Co., Inc. | N-substituierte indole mit anwendung in der behandlung von diabetes |
| AU2002240235B2 (en) | 2001-01-30 | 2006-07-06 | Merck & Co., Inc. | Acyl sulfamides for treatment of obesity, diabetes and lipid disorders |
| AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
| PT1537078E (pt) | 2002-08-29 | 2010-06-18 | Merck Sharp & Dohme | Indoles que possuem actividade antidiabética |
| EP1546142A4 (en) | 2002-08-29 | 2007-10-17 | Merck & Co Inc | INDOLES HAVING ANTIDIABETIC EFFECT |
| CA2512879A1 (en) | 2003-01-17 | 2004-08-12 | Soumya P. Sahoo | N-cyclohexylaminocarbonyl benzenesulfonamide derivatives |
| JP5588175B2 (ja) | 2006-11-07 | 2014-09-10 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｐｃｓｋ９のアンタゴニスト |
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| RU2014101501A (ru) | 2011-06-20 | 2015-07-27 | Дженентек, Инк. | Связывающие pcsk9 полипептиды и способы применения |
| PE20181541A1 (es) | 2011-10-27 | 2018-09-26 | Massachusetts Inst Technology | Derivados de aminoacidos funcionalizados en la terminal n capaces de formar microesferas encapsuladoras de farmaco |
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| CN105228616B (zh) * | 2013-03-15 | 2019-05-03 | 实发生物医学公司 | 抗前蛋白转化酶枯草杆菌蛋白酶Kexin 9型（抗PCSK9）化合物及其用于治疗和/或预防心血管疾病的方法 |
| WO2016119067A1 (en) | 2015-01-30 | 2016-08-04 | Pronasci Inc. | Peptides derived from human pcsk9 catalytic domain and uses there of for promoting ldl-r activity |
| WO2017181061A1 (en) | 2016-04-15 | 2017-10-19 | Ra Pharmaceuticals, Inc. | Ras binding peptides and methods of use |
| CN109475593A (zh) | 2016-06-24 | 2019-03-15 | 豪夫迈·罗氏有限公司 | 用于治疗心血管疾病的组合物和方法 |
| WO2018053517A1 (en) | 2016-09-19 | 2018-03-22 | 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 |
| EP3810176A4 (en) | 2018-06-21 | 2022-05-18 | RA Pharmaceuticals, Inc. | 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 |
| US11530244B2 (en) | 2018-06-21 | 2022-12-20 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| US11505575B2 (en) | 2018-06-21 | 2022-11-22 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
| EP3810129B1 (en) | 2018-06-21 | 2023-08-16 | Merck Sharp & Dohme LLC | Pcsk9 antagonist bicyclo-compounds |
| 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
-
2019
- 2019-06-20 MX MX2020013726A patent/MX2020013726A/es unknown
- 2019-06-20 BR BR112020025274A patent/BR112020025274A8/pt unknown
- 2019-06-20 CA CA3102629A patent/CA3102629A1/en active Pending
- 2019-06-20 EA EA202190086A patent/EA202190086A1/ru unknown
- 2019-06-20 CN CN201980041438.5A patent/CN112313243A/zh active Pending
- 2019-06-20 KR KR1020217001723A patent/KR20210024035A/ko active Search and Examination
- 2019-06-20 MA MA052967A patent/MA52967A/fr unknown
- 2019-06-20 GE GEAP201915540A patent/GEP20237506B/en unknown
- 2019-06-20 SG SG11202012451WA patent/SG11202012451WA/en unknown
- 2019-06-20 CR CR20210031A patent/CR20210031A/es unknown
- 2019-06-20 PE PE2020002109A patent/PE20211584A1/es 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 TW TW108121413A patent/TWI840376B/zh active
- 2019-06-20 WO PCT/US2019/038155 patent/WO2019246349A1/en active Application Filing
- 2019-06-20 JP JP2020570427A patent/JP7112531B2/ja active Active
- 2019-06-20 AU AU2019290163A patent/AU2019290163C1/en active Active
- 2019-06-21 AR ARP190101718A patent/AR115597A1/es unknown
-
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/AU2022259744B2/en active Active
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| AR088845A1 (es) | Composiciones farmaceuticas que contienen 7-(1h-imidazol-4-ilmetil)-5,6,7,8-tetrahidro-quinolina para el tratamiento de las enfermedades y las afecciones de la piel |