BR112020025274A8 - Compostos antagonistas de pcsk9 - Google Patents
Compostos antagonistas de pcsk9Info
- Publication number
- BR112020025274A8 BR112020025274A8 BR112020025274A BR112020025274A BR112020025274A8 BR 112020025274 A8 BR112020025274 A8 BR 112020025274A8 BR 112020025274 A BR112020025274 A BR 112020025274A BR 112020025274 A BR112020025274 A BR 112020025274A BR 112020025274 A8 BR112020025274 A8 BR 112020025274A8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- pcsk9
- antagonist compounds
- pcsk9 antagonist
- 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
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- 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
-
- 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)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Biophysics (AREA)
- General Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Epidemiology (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
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862687913P | 2018-06-21 | 2018-06-21 | |
US62/687,913 | 2018-06-21 | ||
PCT/US2019/038155 WO2019246349A1 (en) | 2018-06-21 | 2019-06-20 | Pcsk9 antagonist compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112020025274A2 BR112020025274A2 (pt) | 2021-03-09 |
BR112020025274A8 true BR112020025274A8 (pt) | 2023-02-14 |
Family
ID=67263083
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112020025274A BR112020025274A8 (pt) | 2018-06-21 | 2019-06-20 | Compostos antagonistas de pcsk9 |
Country Status (25)
Country | Link |
---|---|
US (2) | US11427616B2 (pt) |
EP (1) | EP3810626A1 (pt) |
JP (2) | JP7112531B2 (pt) |
KR (1) | KR20210024035A (pt) |
CN (1) | CN112313243A (pt) |
AR (1) | AR115597A1 (pt) |
AU (2) | AU2019290163C1 (pt) |
BR (1) | BR112020025274A8 (pt) |
CA (1) | CA3102629A1 (pt) |
CL (2) | CL2020003257A1 (pt) |
CO (1) | CO2021000456A2 (pt) |
CR (1) | CR20210031A (pt) |
DO (1) | DOP2020000250A (pt) |
EA (1) | EA202190086A1 (pt) |
EC (1) | ECSP21003643A (pt) |
GE (1) | GEP20237506B (pt) |
IL (1) | IL279363A (pt) |
JO (1) | JOP20190150A1 (pt) |
MA (1) | MA52967A (pt) |
MX (1) | MX2020013726A (pt) |
NI (1) | NI202000101A (pt) |
PE (1) | PE20211584A1 (pt) |
PH (1) | PH12020552187A1 (pt) |
SG (1) | SG11202012451WA (pt) |
WO (1) | WO2019246349A1 (pt) |
Families Citing this family (18)
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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 |
DK2968443T3 (da) | 2013-03-15 | 2021-12-06 | Protagonist Therapeutics Inc | Hepcidinanaloger og anvendelser deraf |
WO2015176035A1 (en) | 2014-05-16 | 2015-11-19 | Protagonist Therapeutics, Inc. | α4β7 INTEGRIN THIOETHER PEPTIDE ANTAGONISTS |
EP3169403B1 (en) | 2014-07-17 | 2024-02-14 | Protagonist Therapeutics, Inc. | Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases |
EP3749345A4 (en) | 2018-02-08 | 2022-04-06 | Protagonist Therapeutics, Inc. | CONJUGATED HEPCIDIN MIMETICS |
WO2019246352A1 (en) | 2018-06-21 | 2019-12-26 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist bicyclo-compounds |
US11814445B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
US11814444B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
WO2020009805A2 (en) | 2018-06-21 | 2020-01-09 | Merck Sharp & Dohme Corp. | Cyclic polypeptides for pcsk9 inhibition |
EP3810196A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
JOP20190150A1 (ar) | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ 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 |
WO2021146441A1 (en) | 2020-01-15 | 2021-07-22 | Janssen Biotech, Inc. | Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases |
TW202237167A (zh) | 2020-11-20 | 2022-10-01 | 比利時商健生藥品公司 | 介白素-23受體之肽抑制劑組合物 |
US11932705B2 (en) | 2020-12-18 | 2024-03-19 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
AU2022330007A1 (en) * | 2021-08-19 | 2024-02-15 | Merck Sharp & Dohme Llc | Compounds for treating conditions related to pcsk9 activity |
US20230406885A1 (en) | 2022-06-15 | 2023-12-21 | Merck Sharp & Dohme Llc | Cyclic peptides for trapping interleukin-1 beta |
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US4393046A (en) | 1981-01-30 | 1983-07-12 | Merck & Co., Inc. | Combination of thiopeptin and other related sulfur-containing cyclic polypeptide antibiotics with rumen-active diimides to improve ruminant feed efficiency |
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 |
DE69819311T2 (de) | 1997-03-07 | 2004-07-29 | Metabasis Therapeutics Inc., San Diego | Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase |
WO1998039344A1 (en) | 1997-03-07 | 1998-09-11 | Metabasis Therapeutics, Inc. | Novel 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 |
NZ510308A (en) | 1998-09-09 | 2003-06-30 | Metabasis Therapeutics Inc | Heteroaromatic alkylene substituted phosphonate derivatives useful as inhibitors of Fructose 1,6-bisphosphatase |
DE60128475T2 (de) | 2000-07-25 | 2008-02-07 | Merck & Co., Inc. | N-substituierte indole mit anwendung in der behandlung von diabetes |
WO2002060388A2 (en) | 2001-01-30 | 2002-08-08 | 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 |
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CN101636179B (zh) | 2006-11-07 | 2012-10-10 | 默沙东公司 | Pcsk9拮抗剂 |
KR101404781B1 (ko) | 2007-06-28 | 2014-06-12 | 가부시키가이샤 한도오따이 에네루기 켄큐쇼 | 반도체 장치의 제조 방법 |
JP2010531307A (ja) | 2007-06-28 | 2010-09-24 | メルク フロスト カナダ リミテツド | Gpr105活性のアンタゴニストとしての置換縮合ピリミジン |
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CA2813049A1 (en) | 2010-09-23 | 2012-03-29 | The Trustees Of The University Of Pennsylvania | Modified compstatin with improved stability and binding properties |
MY169485A (en) | 2010-12-28 | 2019-04-15 | Cadila Healthcare Ltd | Heterocyclic compounds suitable for the treatment of dyslipidemia |
EP2721063A4 (en) | 2011-06-20 | 2015-01-14 | Hoffmann La Roche | PCSK9 BINDING POLYPEPTIDES AND METHOD OF USE THEREOF |
PE20150041A1 (es) | 2011-10-27 | 2015-01-28 | Massachusetts Inst Technology | Derivados de aminoacidos funcionalizados en la terminal n capaces de formar microesferas encapsuladoras de farmaco |
WO2013138340A1 (en) | 2012-03-13 | 2013-09-19 | Tensive Controls Inc. | Melanocortin analogs having enhanced activity and transport |
ES2755104T3 (es) | 2012-05-17 | 2020-04-21 | Ra Pharmaceuticals Inc | Inhibidores peptídicos y peptidomiméticos |
BR112015021681A2 (pt) | 2013-03-14 | 2017-11-14 | Daiichi Sankyo Co Ltd | proteínas de ligação para pcsk9 |
AU2014237312B2 (en) * | 2013-03-15 | 2019-03-28 | Shifa Biomedical Corporation | Anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases |
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 |
AU2017281332A1 (en) | 2016-06-24 | 2018-12-20 | F. Hoffmann-La Roche Ag | Compositions and methods for treating cardiovascular disease |
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 |
WO2019246352A1 (en) | 2018-06-21 | 2019-12-26 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist bicyclo-compounds |
JOP20190150A1 (ar) | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
US11814445B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
US11814444B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
EP3810196A4 (en) | 2018-06-21 | 2022-05-04 | Merck Sharp & Dohme Corp. | CYCLIC POLYPEPTIDES FOR INHIBITION OF PCSK9 |
WO2020009805A2 (en) | 2018-06-21 | 2020-01-09 | 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 |
-
2018
- 2018-06-21 JO JOP/2019/0150A patent/JOP20190150A1/ar unknown
-
2019
- 2019-06-20 WO PCT/US2019/038155 patent/WO2019246349A1/en unknown
- 2019-06-20 BR BR112020025274A patent/BR112020025274A8/pt unknown
- 2019-06-20 EP EP19739801.9A patent/EP3810626A1/en active Pending
- 2019-06-20 CA CA3102629A patent/CA3102629A1/en active Pending
- 2019-06-20 AU AU2019290163A patent/AU2019290163C1/en active Active
- 2019-06-20 US US16/446,940 patent/US11427616B2/en active Active
- 2019-06-20 CN CN201980041438.5A patent/CN112313243A/zh active Pending
- 2019-06-20 EA EA202190086A patent/EA202190086A1/ru unknown
- 2019-06-20 KR KR1020217001723A patent/KR20210024035A/ko active Search and Examination
- 2019-06-20 PE PE2020002109A patent/PE20211584A1/es unknown
- 2019-06-20 GE GEAP201915540A patent/GEP20237506B/en unknown
- 2019-06-20 CR CR20210031A patent/CR20210031A/es unknown
- 2019-06-20 MX MX2020013726A patent/MX2020013726A/es unknown
- 2019-06-20 JP JP2020570427A patent/JP7112531B2/ja active Active
- 2019-06-20 SG SG11202012451WA patent/SG11202012451WA/en unknown
- 2019-06-20 MA MA052967A patent/MA52967A/fr unknown
- 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 CL CL2020003257A patent/CL2020003257A1/es unknown
- 2020-12-16 PH PH12020552187A patent/PH12020552187A1/en unknown
- 2020-12-17 DO DO2020000250A patent/DOP2020000250A/es unknown
-
2021
- 2021-01-18 EC ECSENADI20213643A patent/ECSP21003643A/es unknown
- 2021-01-19 CO CONC2021/0000456A patent/CO2021000456A2/es unknown
-
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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Legal Events
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B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
B25F | Entry of change of name and/or headquarter and transfer of application, patent and certif. of addition of invention: change of name on requirement |
Owner name: MERCK SHARP AND DOHME CORP. (US) Free format text: A FIM DE ATENDER A ALTERACAO DE NOME REQUERIDA ATRAVES DA PETICAO NO 870220065319, DE 25/07/2022, E NECESSARIO COMPLEMENTAR O VALOR DA GUIA DE RECOLHIMENTO, VISTO QUE TRATA-SE DE UMA TRANSFERENCIA POR INCORPORACAO E NAO DE UMA ALTERACAO DE NOME. ALEM DISSO, E PRECISO APRESENTAR A GUIA DE CUMPRIMENTO DE EXIGENCIA. |
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B25A | Requested transfer of rights approved |
Owner name: MERCK SHARP AND DOHME LLC (US) |
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B25E | Requested change of name of applicant rejected |
Owner name: MERCK SHARP AND DOHME LLC (US) Free format text: INDEFERIDO O PEDIDO DE ALTERACAO DE NOME CONTIDO NA PETICAO 870220065319 DE 25/07/2022, EM VIRTUDE DE NAO SE TRATAR DE UMA ALTERACAO DE NOME E SIM DE UMA TRANSFERENCIA DE TITULAR QUE JA FOI PUBLICADA. |