EA201490901A1 - Линкеры на основе тирозина для свободного соединения пептидов - Google Patents

Линкеры на основе тирозина для свободного соединения пептидов

Info

Publication number
EA201490901A1
EA201490901A1 EA201490901A EA201490901A EA201490901A1 EA 201490901 A1 EA201490901 A1 EA 201490901A1 EA 201490901 A EA201490901 A EA 201490901A EA 201490901 A EA201490901 A EA 201490901A EA 201490901 A1 EA201490901 A1 EA 201490901A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tyrosine
peptide
free connection
linkers based
preparation
Prior art date
Application number
EA201490901A
Other languages
English (en)
Other versions
EA026184B1 (ru
Inventor
Инго Фламмэ
Ёханнес Кёбберлинг
Ханс-Георг Лерхен
Нильс Грибенов
Рудольф Шоэ-Лооп
Свен Виттрок
Урзула Кренц
Original Assignee
Байер Интеллектуэль Проперти Гмбх
Байер Фарма Акциенгезельшафт
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 Байер Интеллектуэль Проперти Гмбх, Байер Фарма Акциенгезельшафт filed Critical Байер Интеллектуэль Проперти Гмбх
Publication of EA201490901A1 publication Critical patent/EA201490901A1/ru
Publication of EA026184B1 publication Critical patent/EA026184B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/44—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/04—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C233/05—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C5/00—Preparation of hydrocarbons from hydrocarbons containing the same number of carbon atoms
    • C07C5/02—Preparation of hydrocarbons from hydrocarbons containing the same number of carbon atoms by hydrogenation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0215—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing natural amino acids, forming a peptide bond via their side chain functional group, e.g. epsilon-Lys, gamma-Glu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Изобретение относится к новым линкерам на основе тирозина, способствующим разъёмному соединению пептидов или белков с другими молекулярными соединениями, например полиэтиленгликолем, способам их получения и их применению для приготовления лекарственных средств для лечения и/или профилактики заболеваний.
EA201490901A 2011-11-03 2012-10-29 Линкеры на основе тирозина для свободного соединения пептидов EA026184B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11187737 2011-11-03
PCT/EP2012/071373 WO2013064455A1 (en) 2011-11-03 2012-10-29 Tyrosine based linkers for the releasable connection of peptides

Publications (2)

Publication Number Publication Date
EA201490901A1 true EA201490901A1 (ru) 2014-10-30
EA026184B1 EA026184B1 (ru) 2017-03-31

Family

ID=47088883

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490901A EA026184B1 (ru) 2011-11-03 2012-10-29 Линкеры на основе тирозина для свободного соединения пептидов

Country Status (16)

Country Link
US (1) US9315543B2 (ru)
EP (1) EP2773375B1 (ru)
JP (1) JP6051223B2 (ru)
KR (1) KR20150000464A (ru)
CN (1) CN104144705B (ru)
AU (1) AU2012331279A1 (ru)
BR (1) BR112014010806A2 (ru)
CA (1) CA2854095C (ru)
EA (1) EA026184B1 (ru)
ES (1) ES2624626T3 (ru)
HK (1) HK1198926A1 (ru)
IL (1) IL232152A0 (ru)
IN (1) IN2014DN03213A (ru)
MX (1) MX2014004953A (ru)
WO (1) WO2013064455A1 (ru)
ZA (1) ZA201402939B (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20190001B1 (ar) * 2011-11-03 2022-03-14 Bayer Pharma AG عقار أولي معتمد على جليكول عديد إثيلين من أدرينومدالين واستخدامه
AU2015323769A1 (en) 2014-09-26 2017-04-13 Bayer Pharma Aktiengesellschaft Stabilized adrenomedullin derivatives and use thereof
US11207991B2 (en) * 2016-12-15 2021-12-28 Ford Global Technologies, Llc Vehicle charging system for DC fast charging electrified vehicles
AU2018302022A1 (en) 2017-07-17 2020-02-27 Macregen, Inc. Topical delivery of therapeutic agents comprising cell-penetrating peptides for use for the treatment of age-related macular degeneration and other eye diseases
CN114174326A (zh) 2019-06-18 2022-03-11 拜耳公司 长期稳定的肾上腺髓质素类似物及其用途
CN110591077B (zh) * 2019-10-17 2022-01-07 江南大学 一种酶催化制备酪氨酸寡肽和接枝单甲氧基聚乙二醇的方法
AU2021249447A1 (en) * 2020-04-03 2022-11-03 Bayer Aktiengesellschaft Liquid pharmaceutical formulations polyethylene glycol-based prodrugs of adrenomedullin and use
CN112457218B (zh) * 2020-11-05 2022-08-09 宁夏医科大学 2,4-二氨基丁酸衍生物的合成方法
AU2022330343A1 (en) 2021-08-20 2024-02-08 Bayer Aktiengesellschaft Process for the preparation of pegylated adrenomedullin, its intermediates and use thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4812590A (en) 1987-06-25 1989-03-14 Merck & Co., Inc. Carbamates of 4-hydroxyanisole as prodrugs for chemotherapy of melanoma
US6624142B2 (en) 1997-12-30 2003-09-23 Enzon, Inc. Trimethyl lock based tetrapartate prodrugs
EP1243276A1 (en) 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
US8877901B2 (en) * 2002-12-13 2014-11-04 Immunomedics, Inc. Camptothecin-binding moiety conjugates
WO2004019993A1 (en) 2002-08-30 2004-03-11 Ramot At Tel Aviv University Ltd. Self-immolative dendrimers releasing many active moieties upon a single activating event
US7705045B2 (en) 2002-11-14 2010-04-27 Syntarga, B.V. Prodrugs built as multiple self-elimination-release spacers
AU2005232371B2 (en) 2004-03-23 2010-10-14 Complex Biosystems Gmbh Polymeric prodrug with a self-immolative linker
WO2005097162A2 (en) * 2004-04-01 2005-10-20 Elan Pharmaceuticals, Inc. Steroid sparing agents and their use
GB2427360A (en) 2005-06-22 2006-12-27 Complex Biosystems Gmbh Aliphatic prodrug linker
US8273325B2 (en) * 2006-12-20 2012-09-25 Ge Healthcare As Contrast agents
CN101641119A (zh) * 2006-12-20 2010-02-03 通用电气医疗集团股份有限公司 造影剂
WO2009092071A2 (en) * 2008-01-18 2009-07-23 Shire Llc Amino acid and peptide pro-drugs of phenolic analgesics and uses thereof
LT2459220T (lt) * 2009-07-31 2020-12-28 Ascendis Pharma A/S Biologiškai suyrantys vandenyje netirpūs hidrogeliai polietilenglikolio pagrindu
JOP20190001B1 (ar) * 2011-11-03 2022-03-14 Bayer Pharma AG عقار أولي معتمد على جليكول عديد إثيلين من أدرينومدالين واستخدامه

Also Published As

Publication number Publication date
KR20150000464A (ko) 2015-01-02
ZA201402939B (en) 2015-11-25
CA2854095A1 (en) 2013-05-10
EP2773375A1 (en) 2014-09-10
IN2014DN03213A (ru) 2015-05-22
EP2773375B1 (en) 2017-02-08
JP2014533244A (ja) 2014-12-11
US20150051160A1 (en) 2015-02-19
JP6051223B2 (ja) 2016-12-27
AU2012331279A1 (en) 2014-05-08
BR112014010806A2 (pt) 2017-05-02
CN104144705A (zh) 2014-11-12
US9315543B2 (en) 2016-04-19
WO2013064455A1 (en) 2013-05-10
ES2624626T3 (es) 2017-07-17
HK1198926A1 (en) 2015-06-19
CN104144705B (zh) 2017-03-01
MX2014004953A (es) 2014-05-28
EA026184B1 (ru) 2017-03-31
CA2854095C (en) 2021-03-30
IL232152A0 (en) 2014-05-28

Similar Documents

Publication Publication Date Title
EA201490901A1 (ru) Линкеры на основе тирозина для свободного соединения пептидов
EA201270722A1 (ru) Формы рифаксимина и их применение
MX2018013981A (es) Productos farmaceuticos peptidicos mejorados para la resistencia a la insulina.
MX2019003716A (es) Formulaciones farmaceuticas de anticuerpos tnf-alfa.
TW201613958A (en) MIC-1 fusion proteins and uses thereof
EA201171494A1 (ru) Миметики белка smac
MX2023010178A (es) Conjugados de anticuerpo farmaco anti-cd70.
EA201390821A1 (ru) Антагонисты рецепторов лизофосфатидной кислоты и их применение
MX344219B (es) Productos farmaceuticos peptidicos mejorados para resistencia a insulina.
EA201391719A1 (ru) Хиназолиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201291336A1 (ru) Замещенные 5-фтор-1н-пиразолопиридины и их применение
EA201591166A1 (ru) Ингибиторы аутотаксина
CA2796215C (en) Compositions and methods for brain delivery of analgesic peptides
UA118167C2 (uk) Пептид та його застосування
EA201390803A1 (ru) Ингибиторы бромодомена и их применение
EA201491423A1 (ru) Соединения имидазопирролидинонов
EA201370178A1 (ru) Стабильные составы для парентеральной инъекции пептидных лекарственных средств
EA201391175A1 (ru) Гетеродимерные иммуноглобулины
WO2012040459A3 (en) Beta-catenin targeting peptides and uses thereof
EA201170441A1 (ru) Терапевтические противовирусные пептиды
EP4286400A3 (en) Improved peptide pharmaceuticals
EA201200515A1 (ru) Полипептиды и их применение
EA201390669A1 (ru) Способы и композиции для иммунотерапии заболеваний нервной системы
UA111098C2 (uk) Проліки адреномедуліну на основі поліетиленгліколю і їх застосування
EA201301107A1 (ru) Моноклональные антитела против ингибитора пути тканевого фактора (tfpi)

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU