CN103857413A - 载体连接的曲罗尼尔前药 - Google Patents

载体连接的曲罗尼尔前药 Download PDF

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Publication number
CN103857413A
CN103857413A CN201280049725.9A CN201280049725A CN103857413A CN 103857413 A CN103857413 A CN 103857413A CN 201280049725 A CN201280049725 A CN 201280049725A CN 103857413 A CN103857413 A CN 103857413A
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carrier
alkyl
formula
linked
alkynyl
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CN201280049725.9A
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Chinese (zh)
Inventor
U·赫泽尔
H·拉乌
T·莱斯曼
N·比塞科
G·迈特罗
K·斯普罗格
T·韦格
O·凯尔
J·策特勒
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Ascendis Pharma AS
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Publication of CN103857413A publication Critical patent/CN103857413A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • 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
    • A61K47/64—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
    • A61K47/641—Branched, dendritic or hypercomb peptides
    • 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
    • A61K47/64—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
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
CN201280049725.9A 2011-08-12 2012-08-10 载体连接的曲罗尼尔前药 Pending CN103857413A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP11177409 2011-08-12
EP11177409.7 2011-08-12
EP11195615 2011-12-23
EP11195615.7 2011-12-23
EP12165508 2012-04-25
EP12165508.8 2012-04-25
PCT/EP2012/065745 WO2013024052A1 (en) 2011-08-12 2012-08-10 Carrier-linked treprostinil prodrugs

Publications (1)

Publication Number Publication Date
CN103857413A true CN103857413A (zh) 2014-06-11

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CN201280049725.9A Pending CN103857413A (zh) 2011-08-12 2012-08-10 载体连接的曲罗尼尔前药

Country Status (14)

Country Link
US (2) US9561287B2 (enExample)
EP (1) EP2741781A1 (enExample)
JP (1) JP6092867B2 (enExample)
KR (1) KR101997939B1 (enExample)
CN (1) CN103857413A (enExample)
AU (1) AU2012296954B2 (enExample)
BR (1) BR112014003225A2 (enExample)
CA (1) CA2843883C (enExample)
HK (1) HK1198359A1 (enExample)
IL (1) IL230712A (enExample)
IN (1) IN2014CN00989A (enExample)
MX (1) MX349950B (enExample)
WO (1) WO2013024052A1 (enExample)
ZA (1) ZA201400977B (enExample)

Cited By (4)

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CN108349926A (zh) * 2015-06-17 2018-07-31 康赛制药公司 曲前列环素衍生物及其组合物和用途
US11407707B2 (en) 2015-06-17 2022-08-09 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
CN116113415A (zh) * 2020-06-09 2023-05-12 联合治疗公司 曲前列尼尔的富马酰基二酮哌啶前药
WO2023131349A1 (zh) * 2022-01-07 2023-07-13 广州楷石医药有限公司 一种氧化氮供体型曲前列尼尔类衍生物及其药物组合物和用途

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HK1198359A1 (en) * 2011-08-12 2015-04-10 Ascendis Pharma A/S Carrier-linked treprostinil prodrugs
WO2013160340A1 (en) * 2012-04-25 2013-10-31 Ascendis Pharma A/S Prodrugs of hydroxyl-comprising drugs
AU2013353985B2 (en) 2012-12-07 2017-07-13 Ascendis Pharma A/S Carrier-linked prostanoid prodrugs
EP3712142B1 (en) 2013-01-11 2022-07-06 Corsair Pharma, Inc. Prodrugs of treprostinil
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
CA2908244C (en) * 2013-03-25 2021-04-20 United Therapeutics Corporation Process of making prostacyclin compounds with linker thiol and pegylated forms
CA2911172C (en) 2013-04-30 2021-10-19 United Therapeutics Corporation Controlled release pharmaceutical formulations
BR112016009207B1 (pt) 2013-10-25 2022-11-22 Insmed Incorporated Compostos de prostaciclina
JO3624B1 (ar) * 2014-05-08 2020-08-27 Lilly Co Eli تركيبات إنسولين سريعة المفعول
JP2017517550A (ja) * 2014-06-13 2017-06-29 ユナイテッド セラピューティクス コーポレイション トレプロスチニル製剤
EP3169660A1 (en) * 2014-07-16 2017-05-24 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
CA2967385C (en) 2014-11-18 2023-05-16 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
TWI540121B (zh) 2014-12-01 2016-07-01 臺灣永光化學工業股份有限公司 曲前列環素二乙醇胺之合成方法及新穎中間體
IL252577B (en) 2014-12-03 2022-07-01 Steadymed Ltd Preservative-free treprostinil formulations and methods and devices for use with same
US11389510B2 (en) 2016-01-08 2022-07-19 Ascendis Pharma Growth Disorders A/S Controlled-release CNP agonists with low initial NPR-B activity
IL297375B2 (en) 2016-01-08 2024-02-01 Ascendis Pharma Growth Disorders As Controlled-release CNP agonists with low NPR–C binding
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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108349926A (zh) * 2015-06-17 2018-07-31 康赛制药公司 曲前列环素衍生物及其组合物和用途
US11407707B2 (en) 2015-06-17 2022-08-09 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
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KR20140070545A (ko) 2014-06-10
WO2013024052A1 (en) 2013-02-21
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US20190105400A1 (en) 2019-04-11
ZA201400977B (en) 2017-11-29
BR112014003225A2 (pt) 2017-03-01
IN2014CN00989A (enExample) 2015-04-10
IL230712A0 (en) 2014-03-31
US9561287B2 (en) 2017-02-07
IL230712A (en) 2017-08-31
AU2012296954B2 (en) 2016-09-15
MX2014001497A (es) 2014-04-25
CA2843883A1 (en) 2013-02-21
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US20140296150A1 (en) 2014-10-02
US10729778B2 (en) 2020-08-04
JP6092867B2 (ja) 2017-03-08
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CA2843883C (en) 2020-04-28
KR101997939B1 (ko) 2019-07-08
JP2014527050A (ja) 2014-10-09

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