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SG11201506336XA - Proprotein convertase subtilisin/kexin type 9 allosteric binding ligands to modulate serum low density lipoprotein - Google Patents

Proprotein convertase subtilisin/kexin type 9 allosteric binding ligands to modulate serum low density lipoprotein

Info

Publication number
SG11201506336XA
SG11201506336XA SG11201506336XA SG11201506336XA SG11201506336XA SG 11201506336X A SG11201506336X A SG 11201506336XA SG 11201506336X A SG11201506336X A SG 11201506336XA SG 11201506336X A SG11201506336X A SG 11201506336XA SG 11201506336X A SG11201506336X A SG 11201506336XA
Authority
SG
Singapore
Prior art keywords
low density
density lipoprotein
binding ligands
proprotein convertase
convertase subtilisin
Prior art date
Application number
SG11201506336XA
Other languages
English (en)
Inventor
Michael M Muehlemann
Thomas E Barta
Kyle D Monroe
Jonathan William Bourne
Margaret Thompson Reece
Vesa Nevalainen
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 SG11201506336XA publication Critical patent/SG11201506336XA/en

Links

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/37Digestive system
    • A61K35/407Liver; Hepatocytes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6402Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals
    • C12N9/6405Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals not being snakes
    • C12N9/6408Serine endopeptidases (3.4.21)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
SG11201506336XA 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 allosteric binding ligands to modulate serum low density lipoprotein SG11201506336XA (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 (fr) 2013-02-15 2014-02-15 Ligands de liaison allostériques de la proprotéine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux sériques de lipoprotéines de basse densité (ldl)

Publications (1)

Publication Number Publication Date
SG11201506336XA true SG11201506336XA (en) 2015-09-29

Family

ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201506336XA SG11201506336XA (en) 2013-02-15 2014-02-15 Proprotein convertase subtilisin/kexin type 9 allosteric binding ligands to modulate serum low density lipoprotein

Country Status (10)

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

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
EP4091624A1 (fr) 2013-03-15 2022-11-23 Protagonist Therapeutics, Inc. Analogues d'hepcidine et leurs utilisations
DK3143037T3 (da) 2014-05-16 2021-09-20 Protagonist Therapeutics Inc Alpha4beta7-integrin-thioether-peptidantagonister
EP3169403B9 (fr) 2014-07-17 2024-07-03 Protagonist Therapeutics, Inc. Peptides inhibiteurs par voie orale du récepteur de l'interleukine-23 et leur utilisation dans le traitement des maladies inflammatoires de l'intestin
JP2017528448A (ja) * 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 プロタンパク質コンバターゼであるスブチリシン/ケキシンタイプ9(pcsk9)のタンパク質活性のモジュレーションのための、結合リガンドとしての小分子の組成物およびその使用方法
AU2015328002A1 (en) 2014-10-01 2017-04-27 Protagonist Therapeutics, Inc. Novel alpha4beta7 peptide monomer and dimer antagonists
EP3201217A4 (fr) 2014-10-01 2018-07-18 Protagonist Therapeutics Inc. Nouveaux peptides monomères et dimères cycliques possédant une activité antagoniste de l'intégrine
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 (fr) 2015-08-21 2019-03-27 Portola Pharmaceuticals, Inc. Modulateurs phénylpipérazine proprotéine convertase subtilisine/kexine de type 9 (pcsk9) et leur utilisation
WO2017034990A1 (fr) 2015-08-21 2017-03-02 Portola Pharmaceuticals, Inc. Composition et procédés d'utilisation de petites molécules de type tétrahydroisoquinoline pour se lier à pcsk9 et moduler l'activité protéique de pcsk9
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 (fr) * 2015-09-28 2017-04-06 Agency For Science, Technology And Research Revêtement pour nanoparticules métalliques
WO2017117411A1 (fr) 2015-12-30 2017-07-06 Protagonist Therapeutics, Inc. Analogues de mimétiques d'hepcidine à demi-vie in vivo améliorée
WO2017147328A1 (fr) 2016-02-23 2017-08-31 Portola Pharmaceuticals, Inc. Composés se liant à la proprotéine convertase subtilisine/kexine de type 9 (pcsk9)
EP3432906A4 (fr) 2016-03-23 2020-04-01 Protagonist Therapeutics, Inc. Procédés de synthèse d'antagonistes de peptide alpha4beta7
KR102449308B1 (ko) 2016-06-24 2022-10-04 에프. 호프만-라 로슈 아게 심혈관 질환의 치료를 위한 조성물 및 방법
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 (fr) 2017-09-11 2022-11-23 Protagonist Therapeutics, Inc. Peptides d'agoniste opioïde et leurs utilisations
US11753443B2 (en) 2018-02-08 2023-09-12 Protagonist Therapeutics, Inc. Conjugated hepcidin mimetics
CA3125765A1 (fr) 2019-01-18 2020-07-23 Astrazeneca Ab Inhibiteurs de pcsk9 et leurs procedes d'utilisation
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.
CR20220332A (es) 2020-01-15 2022-11-28 Janssen Biotech Inc Inhibidores de péptidos del receptor de interleucina-23 y su uso para tratar enfermedades inflamatorias
CA3168135A1 (fr) 2020-01-15 2021-07-22 Janssen Biotech, Inc. Inhibiteurs peptidiques du recepteur de l'interleukine-23 et leur utilisation pour traiter des maladies inflammatoires
PE20240631A1 (es) 2020-11-20 2024-03-26 Janssen Pharmaceutica Nv Composiciones de inhibidores peptidicos del receptor de interleucina-23
US12115154B2 (en) 2020-12-16 2024-10-15 Srx Cardio, Llc Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)
CA3213636A1 (fr) 2021-03-18 2022-09-22 Seagen Inc. Liberation selective de medicament a partir de conjugues internalises de composes biologiquement actifs

Family Cites Families (3)

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Publication number Priority date Publication date Assignee Title
US7928189B2 (en) * 2008-05-05 2011-04-19 Ottawa Health Research Institute PCSK9 polypeptide fragment
PL2483266T3 (pl) * 2009-10-01 2015-08-31 Cadila Healthcare Ltd Związki do leczenia dyslipidemii i chorób pokrewnych
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
EP2956154A2 (fr) 2015-12-23
CA2901436A1 (fr) 2014-08-21
WO2014127316A3 (fr) 2014-10-09
WO2014127316A2 (fr) 2014-08-21
CN105378159A (zh) 2016-03-02
IL240583A0 (en) 2015-09-24
AU2014216091A1 (en) 2015-09-03
KR20150127622A (ko) 2015-11-17
HK1219048A1 (zh) 2017-03-24
JP2016508722A (ja) 2016-03-24
WO2014127316A4 (fr) 2014-12-04
EP2956154A4 (fr) 2016-07-27

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