EP2956154A4 - Allosterische proprotein-konvertase-subtilisin/-kexin typ 9 (pcsk9)-bindungsliganden zur modulation des ldl-serumspiegels - Google Patents

Allosterische proprotein-konvertase-subtilisin/-kexin typ 9 (pcsk9)-bindungsliganden zur modulation des ldl-serumspiegels

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Withdrawn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
English (en)
French (fr)
Other versions
EP2956154A2 (de
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/de
Publication of EP2956154A4 publication Critical patent/EP2956154A4/de
Withdrawn legal-status Critical Current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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Developmental Biology & Embryology (AREA)
  • Cell Biology (AREA)
  • Nutrition Science (AREA)
  • Virology (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • General Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Enzymes And Modification Thereof (AREA)
EP14751148.9A 2013-02-15 2014-02-15 Allosterische proprotein-konvertase-subtilisin/-kexin typ 9 (pcsk9)-bindungsliganden zur modulation des ldl-serumspiegels Withdrawn EP2956154A4 (de)

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 (de) 2015-12-23
EP2956154A4 true EP2956154A4 (de) 2016-07-27

Family

ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
EP14751148.9A Withdrawn EP2956154A4 (de) 2013-02-15 2014-02-15 Allosterische proprotein-konvertase-subtilisin/-kexin typ 9 (pcsk9)-bindungsliganden zur modulation des ldl-serumspiegels

Country Status (10)

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

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US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
EP4091624A1 (de) 2013-03-15 2022-11-23 Protagonist Therapeutics, Inc. Hepcidin-analoga und verwendungen davon
CA2949215C (en) 2014-05-16 2023-03-14 Protagonist Therapeutics, Inc. .alpha.4.beta.7 integrin thioether peptide antagonists
SG10201810154WA (en) 2014-07-17 2018-12-28 Protagonist Therapeutics Inc Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases
WO2016029037A1 (en) 2014-08-21 2016-02-25 Srx Cardio, Llc Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(pcsk9) protein activity
WO2016054445A1 (en) 2014-10-01 2016-04-07 Protagonist Therapeutics, Inc. Novel cyclic monomer and dimer peptides having integrin antagonist activity
JP2017535527A (ja) 2014-10-01 2017-11-30 プロタゴニスト セラピューティクス， インコーポレイテッド 新規のα４β７ペプチド単量体及び二量体拮抗薬
MA41022A (fr) * 2014-11-24 2017-10-03 Shire Human Genetic Therapies Ciblage lysosomial et utilisations correspondantes
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 (de) 2015-08-21 2019-03-27 Portola Pharmaceuticals, Inc. Phenylpiperazin-proprotein-konvertase-subtilisin/-kexin typ 9 p(csk9)-modulatoren und deren verwendung
HK1260897A1 (zh) 2015-08-21 2019-12-27 Portola Pharmaceuticals, Inc. 使用四氢异喹啉小分子来结合并调节pcsk9的蛋白活性的组合物和方法
WO2017034994A1 (en) 2015-08-21 2017-03-02 Portola Pharmaceuticals, Inc. 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
CA3009834A1 (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)
CA3017926C (en) 2016-03-23 2023-10-10 Protagonist Therapeutics, Inc. Methods for synthesizing .alpha.4.beta.7 peptide antagonists
AU2017281332A1 (en) 2016-06-24 2018-12-20 F. Hoffmann-La Roche Ag Compositions and methods for treating cardiovascular disease
WO2018022937A1 (en) 2016-07-27 2018-02-01 Protagonist Therapeutics, Inc. Peptide inhibitors of interleukin-23 and their use to treat inflammatory diseases
TW201823222A (zh) * 2016-12-23 2018-07-01 財團法人生物技術開發中心 化合物、醫藥組成物及其用途
EP3681900A4 (de) 2017-09-11 2021-09-08 Protagonist Therapeutics, Inc. Opioidagonistpeptide und verwendungen davon
WO2019157268A1 (en) 2018-02-08 2019-08-15 Protagonist Therapeutics, Inc. Conjugated hepcidin mimetics
CA3104418A1 (en) 2018-07-12 2020-01-16 Protagonist Therapeutics, Inc. Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases
WO2020150473A2 (en) 2019-01-18 2020-07-23 Dogma Therapeutics, Inc. Pcsk9 inhibitors and methods of use thereof
AU2020311395A1 (en) 2019-07-10 2022-02-03 Protagonist Therapeutics, Inc. Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases
SMT202500254T1 (it) 2020-01-15 2025-09-12 Janssen Biotech Inc Inibitori peptidici del recettore dell'interleuchina-23 e loro uso per trattare malattie infiammatorie
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.
AU2021383828A1 (en) 2020-11-20 2023-07-06 Janssen Pharmaceutica Nv Compositions of peptide inhibitors of 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)
JP2024510435A (ja) 2021-03-18 2024-03-07 シージェン インコーポレイテッド 生体活性化合物の内部移行複合体からの選択的薬物放出
KR20240034224A (ko) 2021-07-14 2024-03-13 얀센 바이오테크 인코포레이티드 인터류킨-23 수용체의 지질화된 펩티드 억제제

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

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