CA2901436A1 - Ligands de liaison allosteriques de la proproteine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux seriques de lipoproteines de basse densite (ldl) - Google Patents

Ligands de liaison allosteriques de la proproteine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux seriques de lipoproteines de basse densite (ldl) Download PDF

Info

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
Authority
CA
Canada
Prior art keywords
ser
thr
trp
compound
leu
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.)
Abandoned
Application number
CA2901436A
Other languages
English (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 CA2901436A1 publication Critical patent/CA2901436A1/fr
Abandoned 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
CA2901436A 2013-02-15 2014-02-15 Ligands de liaison allosteriques de la proproteine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux seriques de lipoproteines de basse densite (ldl) Abandoned CA2901436A1 (fr)

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
CA2901436A1 true CA2901436A1 (fr) 2014-08-21

Family

ID=51354696

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2901436A Abandoned CA2901436A1 (fr) 2013-02-15 2014-02-15 Ligands de liaison allosteriques de la proproteine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux seriques de lipoproteines de basse densite (ldl)

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 (24)

* 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
EP2968443B1 (fr) 2013-03-15 2021-09-29 Protagonist Therapeutics, Inc. Analogues d'hepcidine et leurs utilisations
NZ726337A (en) 2014-05-16 2023-10-27 Protagonist Therapeutics Inc Α4β7 integrin thioether peptide antagonists
CA2955460A1 (fr) 2014-07-17 2016-01-21 Protagonist Therapeutics, Inc. Peptides inhibiteurs par voie orale du recepteur de l'interleukine-23 et leur utilisation dans le traitement des maladies inflammatoires de l'intestin
EP3182971A4 (fr) 2014-08-21 2018-04-25 SRX Cardio, LLC Composition et procédés d'utilisation de petites molécules en tant que ligands de liaison pour la modulation de l'activité proprotéine convertase subtilisine/protéine kexine de type 9 (pcsk9)
EP3201217A4 (fr) 2014-10-01 2018-07-18 Protagonist Therapeutics Inc. Nouveaux peptides monomères et dimères cycliques possédant une activité antagoniste de l'intégrine
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
EP3337497B1 (fr) 2015-08-21 2023-07-12 SRX Cardio, LLC Composition et procédés d'utilisation de nouveaux petits composés organiques de phénylalanine pour moduler directement l'activité de la protéine pcsk9
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
WO2017034997A1 (fr) * 2015-08-21 2017-03-02 Portola Pharmaceuticals, Inc. Modulateurs phénylpipérazine proprotéine convertase subtilisine/kexine de type 9 (pcsk9) et leur utilisation
US20180289843A1 (en) * 2015-09-28 2018-10-11 Agency For Science, Technology And Research Coating for metal nanoparticles
US20190002503A1 (en) 2015-12-30 2019-01-03 Protagonist Therapeutics, Inc. Analogues of hepcidin mimetics with improved in vivo half lives
WO2017147328A1 (fr) 2016-02-23 2017-08-31 Portola Pharmaceuticals, Inc. Composés se liant à la proprotéine convertase subtilisine/kexine de type 9 (pcsk9)
CA3017926C (fr) 2016-03-23 2023-10-10 Protagonist Therapeutics, Inc. Procedes de synthese d'antagonistes de peptide .alpha.4.beta.7
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
TW201920234A (zh) 2017-09-11 2019-06-01 美商領導醫療有限公司 類鴉片促效劑肽及其用途
CA3089868A1 (fr) 2018-02-08 2019-08-15 Protagonist Therapeutics, Inc. Mimetiques d'hepcidine conjugues
MX2021008533A (es) 2019-01-18 2021-08-19 Astrazeneca Ab Inhibidores de la pcsk9 y metodos de uso de los mismos.
EP3997105A4 (fr) 2019-07-10 2023-09-13 Protagonist Therapeutics, Inc. Inhibiteurs peptidiques du récepteur de l'interleukine-23 et leur utilisation pour traiter des maladies inflammatoires
CA3167751A1 (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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP2956154A4 (fr) 2016-07-27
SG11201506336XA (en) 2015-09-29
IL240583A0 (en) 2015-09-24
WO2014127316A2 (fr) 2014-08-21
EP2956154A2 (fr) 2015-12-23
JP2016508722A (ja) 2016-03-24
WO2014127316A4 (fr) 2014-12-04
KR20150127622A (ko) 2015-11-17
WO2014127316A3 (fr) 2014-10-09
CN105378159A (zh) 2016-03-02
AU2014216091A1 (en) 2015-09-03
HK1219048A1 (zh) 2017-03-24

Similar Documents

Publication Publication Date Title
CA2901436A1 (fr) Ligands de liaison allosteriques de la proproteine convertase subtilisine/kexine de type 9 (pcsk9) utilisables en vue de la modulation des niveaux seriques de lipoproteines de basse densite (ldl)
US11771710B2 (en) Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands
US10287317B2 (en) Proprotein convertase subtilisin kexin type 9 (PCSK9) allosteric binding ligands to modulate serum low density lipoprotein (LDL) levels
JP2019108389A (ja) アテローム性硬化症の処置方法
US11944619B2 (en) Phenylalanine small organic compounds to directly modulate PCSK9 protein activity
US10980801B2 (en) Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use
JP6641356B2 (ja) 疾患の予防及び治療のための方法及び組成物
US20210309613A1 (en) Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate pcsk9 protein activity
JP2019104744A (ja) コレステロール誘発性ミトコンドリア機能不全を治療するための芳香族カチオン性ペプチドの使用

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20200217