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EP2956154A4 - Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to mudulate serum low density lipoprotein (ldl) levels - Google Patents

Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to mudulate serum low density lipoprotein (ldl) levels

Info

Publication number
EP2956154A4
EP2956154A4 EP14751148.9A EP14751148A EP2956154A4 EP 2956154 A4 EP2956154 A4 EP 2956154A4 EP 14751148 A EP14751148 A EP 14751148A EP 2956154 A4 EP2956154 A4 EP 2956154A4
Authority
EP
European Patent Office
Prior art keywords
mudulate
pcsk9
ldl
levels
low density
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP14751148.9A
Other languages
German (de)
French (fr)
Other versions
EP2956154A2 (en
Inventor
Michael M Muehlemann
Thomas E Barta
Kyle D Monroe
Jonathan William Bourne
Margaret Thompson Reece
Vesa Nevalainen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SRX Cardio LLC
Original Assignee
SRX Cardio LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by SRX Cardio LLC filed Critical SRX Cardio LLC
Publication of EP2956154A2 publication Critical patent/EP2956154A2/en
Publication of EP2956154A4 publication Critical patent/EP2956154A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/37—Digestive system
    • A61K35/407—Liver; Hepatocytes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C12N9/6402—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals
    • C12N9/6405—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals not being snakes
    • C12N9/6408—Serine endopeptidases (3.4.21)
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Wood Science & Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nutrition Science (AREA)
  • Developmental Biology & Embryology (AREA)
  • Physiology (AREA)
  • Cell Biology (AREA)
  • Biophysics (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • General Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Microbiology (AREA)
  • Obesity (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP14751148.9A 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to mudulate serum low density lipoprotein (ldl) levels Withdrawn EP2956154A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361765423P 2013-02-15 2013-02-15
US201361836381P 2013-06-18 2013-06-18
PCT/US2014/016640 WO2014127316A2 (en) 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to mudulate serum low density lipoprotein (ldl) levels

Publications (2)

Publication Number Publication Date
EP2956154A2 EP2956154A2 (en) 2015-12-23
EP2956154A4 true EP2956154A4 (en) 2016-07-27

Family

ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
EP14751148.9A Withdrawn EP2956154A4 (en) 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to mudulate serum low density lipoprotein (ldl) levels

Country Status (10)

Country Link
EP (1) EP2956154A4 (en)
JP (1) JP2016508722A (en)
KR (1) KR20150127622A (en)
CN (1) CN105378159A (en)
AU (1) AU2014216091A1 (en)
CA (1) CA2901436A1 (en)
HK (1) HK1219048A1 (en)
IL (1) IL240583A0 (en)
SG (1) SG11201506336XA (en)
WO (1) WO2014127316A2 (en)

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US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
EP4091624A1 (en) 2013-03-15 2022-11-23 Protagonist Therapeutics, Inc. Hepcidin analogues and uses thereof
DK3143037T3 (en) 2014-05-16 2021-09-20 Protagonist Therapeutics Inc ALPHA4BETA7-INTEGRIN-THIOETHER-PEPTIDE ANTAGONISTS
EP3169403B9 (en) 2014-07-17 2024-07-03 Protagonist Therapeutics, Inc. Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases
JP2017528448A (en) * 2014-08-21 2017-09-28 エスアールエックス カーディオ，エル エル シー Compositions of small molecules as binding ligands and methods of use thereof for the modulation of the protein activity of the proprotein convertase subtilisin / kexin type 9 (PCSK9)
AU2015328002A1 (en) 2014-10-01 2017-04-27 Protagonist Therapeutics, Inc. Novel alpha4beta7 peptide monomer and dimer antagonists
EP3201217A4 (en) 2014-10-01 2018-07-18 Protagonist Therapeutics Inc. Novel cyclic monomer and dimer peptides having integrin antagonist activity
MA41022A (en) * 2014-11-24 2017-10-03 Shire Human Genetic Therapies LYSOSOMIAL TARGETING AND CORRESPONDING USES
US10787490B2 (en) 2015-07-15 2020-09-29 Protaganist Therapeutics, Inc. Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases
EP3337788A4 (en) 2015-08-21 2019-03-27 Portola Pharmaceuticals, Inc. Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (pcsk9) modulators and their use
WO2017034990A1 (en) 2015-08-21 2017-03-02 Portola Pharmaceuticals, Inc. Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate pcsk9 protein activity
US10821106B2 (en) 2015-08-21 2020-11-03 Srx Cardio, Llc Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity
WO2017058113A1 (en) * 2015-09-28 2017-04-06 Agency For Science, Technology And Research Coating for metal nanoparticles
WO2017117411A1 (en) 2015-12-30 2017-07-06 Protagonist Therapeutics, Inc. Analogues of hepcidin mimetics with improved in vivo half lives
WO2017147328A1 (en) 2016-02-23 2017-08-31 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
EP3432906A4 (en) 2016-03-23 2020-04-01 Protagonist Therapeutics, Inc. Methods for synthesizing alpha4beta7 peptide antagonists
KR102449308B1 (en) 2016-06-24 2022-10-04 에프. 호프만-라 로슈 아게 Compositions and methods for the treatment of cardiovascular disease
TW201823222A (en) * 2016-12-23 2018-07-01 財團法人生物技術開發中心 Compound, pharmaceutical composition and use thereof
EP4092038A1 (en) 2017-09-11 2022-11-23 Protagonist Therapeutics, Inc. Opioid agonist peptides and uses thereof
US11753443B2 (en) 2018-02-08 2023-09-12 Protagonist Therapeutics, Inc. Conjugated hepcidin mimetics
CA3125765A1 (en) 2019-01-18 2020-07-23 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
MX2022000397A (en) 2019-07-10 2022-04-25 Protagonist Therapeutics Inc Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases.
CR20220332A (en) 2020-01-15 2022-11-28 Janssen Biotech Inc Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases
CA3168135A1 (en) 2020-01-15 2021-07-22 Janssen Biotech, Inc. Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases
PE20240631A1 (en) 2020-11-20 2024-03-26 Janssen Pharmaceutica Nv COMPOSITIONS OF PEPTIDE INHIBITORS OF THE INTERLEUKIN-23 RECEPTOR
US12115154B2 (en) 2020-12-16 2024-10-15 Srx Cardio, Llc Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)
CA3213636A1 (en) 2021-03-18 2022-09-22 Seagen Inc. Selective drug release from internalized conjugates of biologically active compounds

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US7928189B2 (en) * 2008-05-05 2011-04-19 Ottawa Health Research Institute PCSK9 polypeptide fragment
PL2483266T3 (en) * 2009-10-01 2015-08-31 Cadila Healthcare Ltd Compounds for the treatment of dyslipidemia and related diseases
CN102206249B (en) * 2011-04-26 2013-07-03 中国农业科学院哈尔滨兽医研究所 Specific B cell epitope polypeptide of NS1 protein of encephalitis B virus and use thereof

Non-Patent Citations (2)

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NICOLA FERRI: "Proprotein Convertase Subtilisin/Kexin Type 9: From the Discovery to the Development of New Therapies for Cardiovascular Diseases", SCIENTIFICA, vol. 166, no. 7, 1 January 2012 (2012-01-01), pages 4334 - 21, XP055270158, DOI: 10.1016/S0140-6736(10)60284-X *
TIBOLLA G ET AL: "Proprotein convertase subtilisin/kexin type 9 (PCSK9): From structurefunction relation to therapeutic inhibition", NMCD. NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES, MILAN, IT, vol. 21, no. 11, 23 June 2011 (2011-06-23), pages 835 - 843, XP028314065, ISSN: 0939-4753, [retrieved on 20110720], DOI: 10.1016/J.NUMECD.2011.06.002 *

Also Published As

Publication number Publication date
EP2956154A2 (en) 2015-12-23
CA2901436A1 (en) 2014-08-21
WO2014127316A3 (en) 2014-10-09
WO2014127316A2 (en) 2014-08-21
CN105378159A (en) 2016-03-02
IL240583A0 (en) 2015-09-24
AU2014216091A1 (en) 2015-09-03
KR20150127622A (en) 2015-11-17
SG11201506336XA (en) 2015-09-29
HK1219048A1 (en) 2017-03-24
JP2016508722A (en) 2016-03-24
WO2014127316A4 (en) 2014-12-04

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