HK1198926A1 - Tyrosine based linkers for the releasable connection of peptides - Google Patents

Tyrosine based linkers for the releasable connection of peptides Download PDF

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Publication number
HK1198926A1
HK1198926A1 HK14112488.8A HK14112488A HK1198926A1 HK 1198926 A1 HK1198926 A1 HK 1198926A1 HK 14112488 A HK14112488 A HK 14112488A HK 1198926 A1 HK1198926 A1 HK 1198926A1
Authority
HK
Hong Kong
Prior art keywords
group
tert
represents hydrogen
value
compound
Prior art date
Application number
HK14112488.8A
Other languages
English (en)
Chinese (zh)
Inventor
Ingo Flamme
Johannes KÖBBERLING
Hans-Georg Lerchen
Nils Griebenow
Rudolf Schohe-Loop
Sven WITTROCK
Ursula Krenz
Original Assignee
Bayer Intellectual Property Gmbh
Bayer Pharma Aktiengesellschaft
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 Bayer Intellectual Property Gmbh, Bayer Pharma Aktiengesellschaft filed Critical Bayer Intellectual Property Gmbh
Publication of HK1198926A1 publication Critical patent/HK1198926A1/xx

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
HK14112488.8A 2011-11-03 2012-10-29 Tyrosine based linkers for the releasable connection of peptides HK1198926A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11187737.9 2011-11-03
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 (1)

Publication Number Publication Date
HK1198926A1 true HK1198926A1 (en) 2015-06-19

Family

ID=47088883

Family Applications (1)

Application Number Title Priority Date Filing Date
HK14112488.8A HK1198926A1 (en) 2011-11-03 2012-10-29 Tyrosine based linkers for the releasable connection of peptides

Country Status (16)

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

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JOP20190001B1 (ar) * 2011-11-03 2022-03-15 Bayer Pharma AG عقار أولي معتمد على جليكول عديد إثيلين من أدرينومدالين واستخدامه
CN107001440A (zh) 2014-09-26 2017-08-01 拜耳制药股份公司 稳定化的肾上腺髓质素衍生物及其用途
US11207991B2 (en) * 2016-12-15 2021-12-28 Ford Global Technologies, Llc Vehicle charging system for DC fast charging electrified vehicles
US10905770B2 (en) 2017-07-17 2021-02-02 Macregen, Inc. Topical delivery of therapeutic agents using cell-penetrating peptides for the treatment of age-related macular degeneration and other eye diseases
CA3143584A1 (en) 2019-06-18 2020-12-24 Bayer Aktiengesellschaft Adrenomedullin-analogues for long-term stabilization and their use
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
EP4126062A1 (en) * 2020-04-03 2023-02-08 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
IL310248A (en) 2021-08-20 2024-03-01 Bayer Ag Process for the preparation of pegylated adrenomedullin, its intermediates and use thereof
CN117358213B (zh) * 2023-09-27 2026-08-04 南京工业大学 金属有机骨架吸附剂及其制备方法和应用
CN119606958B (zh) * 2025-02-14 2025-05-13 江苏长泰药业股份有限公司 一种含有丙酮酸盐的组合物及其制备方法和应用

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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
US20050271615A1 (en) 2002-08-30 2005-12-08 Doron Shabat Self-immolative dendrimers releasing many active moieties upon a single activating event
WO2004043493A1 (en) 2002-11-14 2004-05-27 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
CA2786794C (en) 2004-03-23 2017-09-12 Complex Biosystems Gmbh Aromatic polymeric cascade prodrug linker reagent
AU2005231467A1 (en) * 2004-04-01 2005-10-20 Elan Pharmaceuticals, Inc. Steroid sparing agents and methods of using same
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
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WO2009092073A2 (en) * 2008-01-18 2009-07-23 Shire Llc Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects
LT2459220T (lt) * 2009-07-31 2020-12-28 Ascendis Pharma A/S Biologiškai suyrantys vandenyje netirpūs hidrogeliai polietilenglikolio pagrindu
JOP20190001B1 (ar) * 2011-11-03 2022-03-15 Bayer Pharma AG عقار أولي معتمد على جليكول عديد إثيلين من أدرينومدالين واستخدامه

Also Published As

Publication number Publication date
CN104144705A (zh) 2014-11-12
KR20150000464A (ko) 2015-01-02
IN2014DN03213A (enExample) 2015-05-22
BR112014010806A2 (pt) 2017-05-02
EP2773375A1 (en) 2014-09-10
CA2854095A1 (en) 2013-05-10
JP6051223B2 (ja) 2016-12-27
EA026184B1 (ru) 2017-03-31
IL232152A0 (en) 2014-05-28
JP2014533244A (ja) 2014-12-11
AU2012331279A1 (en) 2014-05-08
ZA201402939B (en) 2015-11-25
EA201490901A1 (ru) 2014-10-30
CN104144705B (zh) 2017-03-01
ES2624626T3 (es) 2017-07-17
WO2013064455A1 (en) 2013-05-10
CA2854095C (en) 2021-03-30
MX2014004953A (es) 2014-05-28
US20150051160A1 (en) 2015-02-19
EP2773375B1 (en) 2017-02-08
US9315543B2 (en) 2016-04-19

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