EA201690282A1 - Биоконъюгаты синтетических апелиновых полипептидов - Google Patents

Биоконъюгаты синтетических апелиновых полипептидов

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Publication number
EA201690282A1
EA201690282A1 EA201690282A EA201690282A EA201690282A1 EA 201690282 A1 EA201690282 A1 EA 201690282A1 EA 201690282 A EA201690282 A EA 201690282A EA 201690282 A EA201690282 A EA 201690282A EA 201690282 A1 EA201690282 A1 EA 201690282A1
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EA
Eurasian Patent Office
Prior art keywords
bioconjugates
relates
present
polypeptides
heart failure
Prior art date
Application number
EA201690282A
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English (en)
Inventor
Шари Л. Каплан
Андрей Голосов
Филипп Гроше
Карла Гимарэс
Аарон Кантер
Чанган Лоу
Дэвид Томас Паркер
Эрик К. Петерс
Эйми Ричардсон Юзера
Кайо Ясосима
Цзюнь Юань
Фредерик Зекри
Хунцзюань Чжао
Original Assignee
Новартис Аг
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Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201690282A1 publication Critical patent/EA201690282A1/ru

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    • 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
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/76—Albumins
    • C07K14/765—Serum albumin, e.g. HSA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/31—Fusion polypeptide fusions, other than Fc, for prolonged plasma life, e.g. albumin

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  • Molecular Biology (AREA)
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  • Heart & Thoracic Surgery (AREA)
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Abstract

Изобретение относится к биоконъюгатам, включающим синтетический полипептид формулы I'или его амид, сложный эфир или соль, в котором X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 и X13 определены в настоящем документе, и часть, продлевающую полупериод жизни, в которых пептид и часть, продлевающая полупериод жизни, ковалентно связаны или слиты, необязательно, через линкер. Полипептиды являются агонистами рецептора APJ. Изобретение относится также к способу изготовления биоконъюгатов по настоящему изобретению и их терапевтическому применению, такому как лечение или профилактика острой декомпенсированной сердечной недостаточности (ОДСН), хронической сердечной недостаточности, легочной гипертензии, фибрилляции предсердий, синдрома Бругада, желудочковой тахикардии, атеросклероза, гипертензии, рестеноза, ишемических сердечно-сосудистых заболеваний, кардиомиопатии, сердечного фиброза, аритмии, задержки жидкости, диабета (включая диабет беременных), ожирения, болезни периферических артерий, инсультов, преходящих ишемических атак, травматических повреждений головного мозга, амиотрофического бокового склероза, ожоговых повреждений (включая солнечный ожог) и преэклампсии. Настоящее изобретение относится также к комбинации фармакологически активных агентов и к фармацевтической композиции.
EA201690282A 2013-07-25 2014-07-21 Биоконъюгаты синтетических апелиновых полипептидов EA201690282A1 (ru)

Applications Claiming Priority (3)

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US201361858303P 2013-07-25 2013-07-25
US201462015848P 2014-06-23 2014-06-23
PCT/US2014/047378 WO2015013169A2 (en) 2013-07-25 2014-07-21 Bioconjugates of synthetic apelin polypeptides

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EA201690282A1 true EA201690282A1 (ru) 2016-09-30

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US (2) US9340582B2 (ru)
EP (1) EP3024492A2 (ru)
JP (1) JP2016527249A (ru)
KR (1) KR20160031552A (ru)
CN (1) CN105705167A (ru)
AP (1) AP2016009019A0 (ru)
AU (1) AU2014293387B2 (ru)
BR (1) BR112016001376A2 (ru)
CA (1) CA2918077A1 (ru)
CL (1) CL2016000157A1 (ru)
CR (1) CR20160049A (ru)
CU (1) CU20160012A7 (ru)
EA (1) EA201690282A1 (ru)
HK (1) HK1218252A1 (ru)
IL (1) IL243691A0 (ru)
MX (1) MX2016001021A (ru)
PE (1) PE20160991A1 (ru)
PH (1) PH12016500103A1 (ru)
SG (1) SG11201600208RA (ru)
TW (1) TW201518323A (ru)
UY (1) UY35671A (ru)
WO (1) WO2015013169A2 (ru)

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KR102509217B1 (ko) * 2020-08-28 2023-03-14 기초과학연구원 시스테인 선택적 결합 퀴놀리논 유도체 화합물, 이의 펩티드 결합체 및 이를 포함하는 항체-약물 접합체
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