CA2901436A1 - Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to modulate serum low density lipoprotein (ldl) levels - Google Patents

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

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Publication number
CA2901436A1
CA2901436A1 CA2901436A CA2901436A CA2901436A1 CA 2901436 A1 CA2901436 A1 CA 2901436A1 CA 2901436 A CA2901436 A CA 2901436A CA 2901436 A CA2901436 A CA 2901436A CA 2901436 A1 CA2901436 A1 CA 2901436A1
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Canada
Prior art keywords
ser
thr
trp
compound
leu
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Abandoned
Application number
CA2901436A
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English (en)
French (fr)
Inventor
Michael M. Muehlemann
Thomas E. Barta
Kyle D. MONROE
Jonathan William BOURNE
Margaret Thompson REECE
Vesa Nevalainen
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SRX Cardio LLC
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SRX Cardio LLC
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Publication of CA2901436A1 publication Critical patent/CA2901436A1/en
Abandoned legal-status Critical Current

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    • 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)
  • 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)
  • Enzymes And Modification Thereof (AREA)
CA2901436A 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to modulate serum low density lipoprotein (ldl) levels Abandoned CA2901436A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361765423P 2013-02-15 2013-02-15
US61/765,423 2013-02-15
US201361836381P 2013-06-18 2013-06-18
US61/836,381 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 (1)

Publication Number Publication Date
CA2901436A1 true CA2901436A1 (en) 2014-08-21

Family

ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2901436A Abandoned CA2901436A1 (en) 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 (pcsk9) allosteric binding ligands to modulate serum low density lipoprotein (ldl) levels

Country Status (10)

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

Families Citing this family (24)

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Publication number Priority date Publication date Assignee Title
US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
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
US10034892B2 (en) 2014-08-21 2018-07-31 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
SG11201702553RA (en) 2014-10-01 2017-04-27 Protagonist Therapeutics Inc NOVEL α4β7 PEPTIDE MONOMER AND DIMER ANTAGONISTS
WO2016054445A1 (en) 2014-10-01 2016-04-07 Protagonist Therapeutics, Inc. Novel cyclic monomer and dimer peptides having integrin antagonist activity
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
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
WO2017034997A1 (en) * 2015-08-21 2017-03-02 Portola Pharmaceuticals, Inc. Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (pcsk9) modulators and their use
US10865185B2 (en) 2015-08-21 2020-12-15 Srx Cardio, Llc Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity
US20180289843A1 (en) * 2015-09-28 2018-10-11 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
US20190119236A1 (en) 2016-02-23 2019-04-25 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
WO2017165676A1 (en) 2016-03-23 2017-09-28 Protagonist Therapeutics, Inc. METHODS FOR SYNTHESIZING α4β7 PEPTIDE ANTAGONISTS
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
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
EP4092038A1 (en) 2017-09-11 2022-11-23 Protagonist Therapeutics, Inc. Opioid agonist peptides and uses thereof
EP3749345A4 (en) 2018-02-08 2022-04-06 Protagonist Therapeutics, Inc. CONJUGATED HEPCIDIN MIMETICS
WO2020150473A2 (en) 2019-01-18 2020-07-23 Dogma Therapeutics, Inc. Pcsk9 inhibitors and methods of use thereof
MX2022000397A (es) 2019-07-10 2022-04-25 Protagonist Therapeutics Inc Inhibidores peptídicos del receptor de interleucina-23 y su uso para tratar enfermedades inflamatorias.
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

Family Cites Families (3)

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US7928189B2 (en) * 2008-05-05 2011-04-19 Ottawa Health Research Institute PCSK9 polypeptide fragment
BR112012007241A2 (pt) * 2009-10-01 2019-09-24 Cadila Healthcare Ltd Soc Indiana compostos , composição farmacêutica, método para tratar desordens, uso dos compostos, medicamento, método para selecionar inibidores com pequenas moléculas de pcsk9 e pequenas moléculas
CN102206249B (zh) * 2011-04-26 2013-07-03 中国农业科学院哈尔滨兽医研究所 乙型脑炎病毒ns1蛋白特异性b细胞抗原表位多肽及其应用

Also Published As

Publication number Publication date
HK1219048A1 (zh) 2017-03-24
EP2956154A4 (en) 2016-07-27
WO2014127316A2 (en) 2014-08-21
CN105378159A (zh) 2016-03-02
JP2016508722A (ja) 2016-03-24
WO2014127316A4 (en) 2014-12-04
EP2956154A2 (en) 2015-12-23
AU2014216091A1 (en) 2015-09-03
KR20150127622A (ko) 2015-11-17
WO2014127316A3 (en) 2014-10-09
IL240583A0 (en) 2015-09-24
SG11201506336XA (en) 2015-09-29

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Effective date: 20200217