DK3075395T3 - Polyethylenglycolbaseret prodrug af adrenomedullin og anvendelse deraf - Google Patents
Polyethylenglycolbaseret prodrug af adrenomedullin og anvendelse deraf Download PDFInfo
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- DK3075395T3 DK3075395T3 DK15192265.5T DK15192265T DK3075395T3 DK 3075395 T3 DK3075395 T3 DK 3075395T3 DK 15192265 T DK15192265 T DK 15192265T DK 3075395 T3 DK3075395 T3 DK 3075395T3
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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- A61K38/22—Hormones
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- 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
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- 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
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
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- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- C07K14/575—Hormones
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- 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
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- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- Proteomics, Peptides & Aminoacids (AREA)
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Claims (10)
1. Medikament, der omfatter en forbindelse med formel (I)
hvor n er tallet 0, 1, 2 eller 3, R1 er hydrogen, methyl, ethyl, n-propyl eller isopropyl, R2 er lineær eller forgrenet 20 kDa til 80 kDa PEG, der er endecappet med en methoxygruppe, eller et af saltene deraf, solvater deraf eller solvaterne af salte deraf i kombination med et inert ikke-toksisk farmaceutisk egnet excipiens, hvor medikamentet er i en farmaceutisk form til inhalation.
2. Medikament ifølge krav 1, der er kendetegnet ved, at forbindelsen med formel (I) defineres som følger: n er tallet 1 eller 2, R1 er hydrogen eller methyl, R2 er lineær 4 0 kDa PEG, der er endecappet med en methoxygruppe.
3. Medikament ifølge et hvilket som helst af kravene 1 til 2, der er kendetegnet ved, at forbindelsen med formel (I) defineres som følger: n er tallet 1 eller 2, R1 er hydrogen, R2 er lineær 40kDa PEG, der er endecappet med en methoxygruppe.
4. Medikament ifølge et hvilket som helst af kravene 1 til 3, hvor den farmaceutiske form til inhalation er valgt fra gruppen, der består af en pulverinhalator og en nebulisator.
5. Medikament ifølge et hvilket som helst af kravene 1 til 4 1 kombination med en yderligere aktiv bestanddel valgt fra gruppen, der består af ACE-inhibitorer, angiotensinreceptorantagonister, beta-2-receptoragonister, phosphodiesterase-inhibitorer, glukokortikoidreceptoragonister, diuretika, rekombinant angiotensinkonverterende enzym-2 og acetylsalicylsyre.
6. Medikament ifølge krav 5, hvor den yderligere aktive bestanddel er valgt fra gruppen, der består af en ACE-inhibitor valgt fra gruppen, der består af enalapril, quinapril, captopril, lisinopril, ramipril, delapril, fosinopril, perindopril, cilazapril, imidapril, benazepril, moexipril, spirapril og trandopril, en angiotensinreceptorantagonist valgt fra gruppen, der består af losartan, candesartan, valsartan, telmisartan og embusartan, en beta-2-receptoragonist valgt fra gruppen, der består af salbutamol, pirbuterol, salmeterol, terbutalin, fenoterol, tulobuterol, clenbuterol, reproterol og formoterol, en phosphodiesterase (PDE)-inhibitor valgt fra gruppen, der består af milrinon, amrinon, pimobendan, cilostazol, sildenafil, vardenafil og tadalafil, en glukokortikoidreceptoragonist valgt fra gruppen, der består af cortiosol, cortison, hydrocortison, prednison, methylprednisolon, prednyliden, deflazacort, fluocortolon, triamcinolon, dexamethason og betamethason, et diuretikum valgt fra gruppen, der består af furosemid, torasemid og hydrochlorthiazid, rekombinant angiotensinkonverterende enzym- 2 og acetylsalicylsyre.
7. Medikament ifølge et hvilket som helst af kravene 1 til 6 til anvendelse til behandling og/eller forebyggelse af en kardiovaskulær, ødematøs og/eller inflammatorisk forstyrrelse valgt fra gruppen, der består af hjertesvigt, koronar hjertesygdom, iskæmisk og/eller hæmoragisk apopleksi, hypertension, pulmonal hypertension, perifer arteriel okklusiv sygdom, præeklampsi, kronisk obstruktiv lungesygdom, astma, akut og/eller kronisk lungeødem, allergisk alveolitis og/eller pneumonitis som følge af inhaleret organisk støv og partikler af fungal, aktinomycetisk eller anden oprindelse, og/eller akut kemisk bronkitis, akut og/eller kronisk kemisk lungeødem, neurogent lungeødem, akutte og/eller kroniske lungemanifestationer som følge af stråling, akutte og/eller kroniske interstitielle lungeforstyrrelser, akut lungeskade/akut respiratorisk distresssyndrom (ALI/ARDS) hos voksen eller barn, herunder nyfødt, ALI/ARDS, der er sekundær i forhold til pneumonia og sepsis, aspirationspneumonia og ALI/ARDS, der er sekundær i forhold til aspiration, ALI/ARDS, der er sekundær i forhold til røggasinhalation, transfusionsrelateret akut lungeskade (TRALI), ALI/ARDS og/eller akut lungeinsufficiens efter operation, traume og/eller forbrændinger og/eller respiratorinduceret lungeskade (VILI), lungeskade efter mekoniumaspiration, lungefibrose, bjergsyge, glomerulonefritis, akut nyreskade, kardiorenalt syndrom, lymfødem, inflammatorisk tarmsygdom, sepsis, septisk shock, systemisk inflammatorisk responssyndrom (SIRS) af ikke-infektiøs oprindelse, inflammatorisk tarmsygdom og urticaria, som omfatter administrering til et menneske eller et dyr af en aktiv mængde af et medikament ifølge et hvilket som helst af kravene 1 til 6.
8. Medikament ifølge krav 7, hvor den kardiovaskulære, ødematøse og/eller inflammatoriske forstyrrelse er valgt fra gruppen, der består af pulmonal hypertension, kronisk obstruktiv lungesygdom, astma, akut og/eller kronisk lungeødem, allergisk alveolitis og/eller pneumonitis som følge af inhaleret organisk støv og partikler af fungal, aktinomycetisk eller anden oprindelse og/eller akut kemisk bronkitis, akut og/eller kronisk kemisk lungeødem, neurogent lungeødem, akutte og/eller kroniske lungemanifestationer som følge af stråling, akutte og/eller kroniske interstitielle lungeforstyrrelser, akut lungeskade/akut respiratorisk distresssyndrom (ALI/ARDS) hos voksen eller barn, herunder nyfødt, ALI/ARDS, der er sekundær i forhold til pneumonia og sepsis, aspirationspneumonia og ALI/ARDS, der er sekundær i forhold til aspiration, ALI/ARDS, der er sekundær i forhold til røggasinhalation, transfusionsrelateret akut lungeskade (TRALI), ALI/ARDS og/eller akut lungeinsufficiens efter operation, traume og/eller forbrændinger og/eller respiratorinduceret lungeskade (VILI), lungeskade efter mekoniumaspiration, lungefibrose, bjergsyge, som omfatter administrering til et menneske eller et dyr af en aktiv mængde af et medikament ifølge et hvilket som helst af kravene 1 til 6.
9. Forbindelse med formel (la)
eller et af saltene deraf, solvater deraf eller solvaterne af salte deraf.
10. Forbindelse med formel (II)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11187735 | 2011-11-03 | ||
| EP12783566.8A EP2773376B1 (en) | 2011-11-03 | 2012-10-30 | Polyethylene glycol based prodrug of adrenomedullin and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3075395T3 true DK3075395T3 (da) | 2018-02-19 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK15192265.5T DK3075395T3 (da) | 2011-11-03 | 2012-10-30 | Polyethylenglycolbaseret prodrug af adrenomedullin og anvendelse deraf |
| DK12783566.8T DK2773376T3 (da) | 2011-11-03 | 2012-10-30 | Polyethylenglycolbaseret prodrug af adrenomedullin og anvendelse deraf |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12783566.8T DK2773376T3 (da) | 2011-11-03 | 2012-10-30 | Polyethylenglycolbaseret prodrug af adrenomedullin og anvendelse deraf |
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Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20150000464A (ko) * | 2011-11-03 | 2015-01-02 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 펩티드의 방출가능한 연결을 위한 티로신 기재의 링커 |
| EP2896400A1 (en) * | 2014-01-17 | 2015-07-22 | Université Catholique De Louvain | Method for increasing the bioavailability of inhaled compounds |
| US11414474B2 (en) | 2014-03-20 | 2022-08-16 | University Of Miyazaki | Long-acting adrenomedullin derivatives |
| CU20170038A7 (es) * | 2014-09-26 | 2017-10-05 | Bayer Pharma AG | Derivados de adrenomedulina estabililzados especialmente útiles en el tratamiento y/o prevención de trastornos cardiovasculares, edematosos y/o inflamatorios |
| KR102152437B1 (ko) * | 2015-09-18 | 2020-09-07 | 고쿠리츠 다이가쿠 호징 미야자키 다이가쿠 | 장시간 작용형 아드레노메둘린 유도체 |
| JP7001285B2 (ja) | 2017-03-29 | 2022-01-19 | 国立大学法人 宮崎大学 | 長時間作用型アドレノメデュリン誘導体 |
| GB201707938D0 (en) | 2017-05-17 | 2017-06-28 | Univ Sheffield | Compounds |
| WO2020254197A1 (en) | 2019-06-18 | 2020-12-24 | Bayer Aktiengesellschaft | Adrenomedullin-analogues for long-term stabilization and their use |
| JP7498882B2 (ja) * | 2019-12-05 | 2024-06-13 | 国立大学法人 宮崎大学 | 異常タンパク質蓄積性神経変性疾患の治療剤 |
| MX2022012332A (es) | 2020-04-03 | 2022-10-27 | Bayer Ag | Formulaciones farmaceuticas liquidas de profarmacos a base de polietilenglicol de adrenomedulina y su uso. |
| US20230364245A1 (en) | 2020-04-03 | 2023-11-16 | Bayer Aktiengesellschaft | Pharmaceutical formulations polyethylene glycol-based prodrugs of adrenomedullin and use |
| AU2021341508A1 (en) | 2020-09-10 | 2023-05-25 | Precirix N.V. | Antibody fragment against fap |
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