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KR20150127622A - 혈청 저밀도 지단백질 （ｌｄｌ） 수준을 조절하기 위한 전구단백질 컨버타제 서브틸리신/켁신 유형 9 （ｐｃｓｋ９） 알로스테릭 결합 리간드 - Google Patents

혈청 저밀도 지단백질 （ｌｄｌ） 수준을 조절하기 위한 전구단백질 컨버타제 서브틸리신/켁신 유형 9 （ｐｃｓｋ９） 알로스테릭 결합 리간드 Download PDF

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KR20150127622A
KR20150127622A KR1020157025152A KR20157025152A KR20150127622A KR 20150127622 A KR20150127622 A KR 20150127622A KR 1020157025152 A KR1020157025152 A KR 1020157025152A KR 20157025152 A KR20157025152 A KR 20157025152A KR 20150127622 A KR20150127622 A KR 20150127622A
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South Korea
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KR1020157025152A
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마이클 엠. 무에흘레만
토마스 이. 바르타
카일 디. 먼로
조나단 윌리엄 본
마가렛 톰슨 리스
베사 네발라이넨
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에스알엑스 카디오, 엘엘씨
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Publication of KR20150127622A publication Critical patent/KR20150127622A/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10—Peptides having 12 to 20 amino acids
    • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020157025152A 2013-02-15 2014-02-15 혈청 저밀도 지단백질 （ｌｄｌ） 수준을 조절하기 위한 전구단백질 컨버타제 서브틸리신/켁신 유형 9 （ｐｃｓｋ９） 알로스테릭 결합 리간드 KR20150127622A (ko)

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 (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
KR20150127622A true KR20150127622A (ko) 2015-11-17

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ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157025152A KR20150127622A (ko) 2013-02-15 2014-02-15 혈청 저밀도 지단백질 （ｌｄｌ） 수준을 조절하기 위한 전구단백질 컨버타제 서브틸리신/켁신 유형 9 （ｐｃｓｋ９） 알로스테릭 결합 리간드

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)

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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

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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

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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
SG11201506336XA (en) 2015-09-29
HK1219048A1 (zh) 2017-03-24
JP2016508722A (ja) 2016-03-24
WO2014127316A4 (fr) 2014-12-04
EP2956154A4 (fr) 2016-07-27

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