HRP20180319T1 - Predlijek adrenomedulina baziran na polietilen glikolu i njegova uporaba - Google Patents
Predlijek adrenomedulina baziran na polietilen glikolu i njegova uporaba Download PDFInfo
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- HRP20180319T1 HRP20180319T1 HRP20180319TT HRP20180319T HRP20180319T1 HR P20180319 T1 HRP20180319 T1 HR P20180319T1 HR P20180319T T HRP20180319T T HR P20180319TT HR P20180319 T HRP20180319 T HR P20180319T HR P20180319 T1 HRP20180319 T1 HR P20180319T1
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- WVLAAKXASPCBGT-UHFFFAOYSA-N reproterol Chemical compound C1=2C(=O)N(C)C(=O)N(C)C=2N=CN1CCCNCC(O)C1=CC(O)=CC(O)=C1 WVLAAKXASPCBGT-UHFFFAOYSA-N 0.000 claims 1
- 201000004193 respiratory failure Diseases 0.000 claims 1
- 229960002052 salbutamol Drugs 0.000 claims 1
- 229960004017 salmeterol Drugs 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 229960003310 sildenafil Drugs 0.000 claims 1
- 229960002909 spirapril Drugs 0.000 claims 1
- HRWCVUIFMSZDJS-SZMVWBNQSA-N spirapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2(C1)SCCS2)C(O)=O)CC1=CC=CC=C1 HRWCVUIFMSZDJS-SZMVWBNQSA-N 0.000 claims 1
- 108700035424 spirapril Proteins 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 1
- 229960005187 telmisartan Drugs 0.000 claims 1
- 229960000195 terbutaline Drugs 0.000 claims 1
- 229960005461 torasemide Drugs 0.000 claims 1
- 229960005294 triamcinolone Drugs 0.000 claims 1
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 claims 1
- 229960000859 tulobuterol Drugs 0.000 claims 1
- 229960004699 valsartan Drugs 0.000 claims 1
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims 1
- 229960002381 vardenafil Drugs 0.000 claims 1
Classifications
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- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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- 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
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Claims (10)
1. Lijek, koji sadrži spoj formule (I)
[image]
u kojoj
n predstavlja broj 0, 1, 2 ili 3,
R1 predstavlja vodik, metil, etil, n-propil ili izopropil,
R2 predstavlja ravni ili razgranatni PEG 20kDa do 80kDa zaklopljen s metoksi skupinom,
ili jedna od njegovih soli, njegovi solvati ili solvati njegovih soli, u kombinaciji s inertnim netoksičnim farmaceutski prikladnim ekscipijentom, pri čemu je lijek u farmaceutskom obliku za inhalaciju.
2. Lijek prema zahtjevu 1, naznačen time da je spoj s formulom (I) definiran kako slijedi:
n predstavlja broj 1 ili 2,
R1 predstavlja vodik ili metil,
R2 predstavlja ravni PEG 40kDa zaklopljen s metoksi skupinom.
3. Lijek prema bilo kojem od zahtjeva 1 do 2, naznačen time da je spoj s formulom (I) definiran kako slijedi:
n predstavlja broj 1 ili 2,
R1 predstavlja vodik,
R2 predstavlja ravni PEG 40kDa zaklopljen s metoksi skupinom.
4. Lijek prema bilo kojem od zahtjeva 1 do 3, naznačen time da je farmaceutski oblik za inhalaciju odabran iz skupine koja se sastoji od inhalatora praha i nebulizatora.
5. Lijek prema bilo kojem od zahtjeva 1 do 4, naznačen time da je nadalje u kombinaciji s dodatnim aktivnim sastojkom odabranim iz skupine koja se sastoji od ACE inhibitora, antagonista angiotenzinskih receptora, agonista beta-2 receptora, inhibitora fosfodiesteraze, agonista glukokortikoidnog receptora, diuretika, rekombinantnog angiotenzin pretvarajućeg enzima-2 i acetilsalicilne kiseline.
6. Lijek prema zahtjevu 5, naznačen time da je dodatni aktivni sastojak odabran iz skupine koju čine ACE inhibitor odabran iz skupine koju čine enalapril, kinapril, kaptopril, lizinopril, ramipril, delapril, fosinopril, perindopril, cilazapril, imidapril, benazepril, moeksipril, spirapril i trandopril, antagonist receptora angiotenzina, odabran iz skupine koju čine losartan, kandesartan, valsartan, telmisartan i embusartan, agonist beta-2 receptora, odabran iz skupine koju čine salbutamol, pirbuterol, salmeterol, terbutalin, fenoterol, tulobuterol, klenbuterol, reproterol i formoterol, inhibitor fosfodiesteraze (PDE) odabran iz skupine koju čine milrinon, amrinon, pimobendan, cilostazol, sildenafil, vardenafil i tadalafil, agonist glukokortikoidnog receptora odabran iz skupine koju čine kortizol, kortizon, hidrokortizon, prednizon, metil-metilprednizolon, predniliden, deflazakor, fluokortolon, triamcinolon, deksametazon i betametazon, diuretik, furosemid, torasemid i hidroklorotiazid, rekombinantni angiotenzin pretvarajući enzim-2 i acetilsalicilna kiselina.
7. Lijek prema bilo kojem od zahtjeva 1 do 6 naznačen time da je za uporabu za liječenje i/ili sprječavanje kardiovaskularnog, edematoznog i/ili upalnog poremećaja odabranog iz skupine koju čine zatajenje srca, koronarna bolest srca, ishemijski i/ili hemoragijski moždani udar, hipertenzija, plućna hipertenzija, periferna arterijska okluzivna bolest, preeklampsija, kronična opstruktivna plućna bolest, astma, akutni i/ili kronični plućni edem, alergijski alveolitis i/ili pneumonitis zbog udisanja organske prašine i čestica gljivičnog, aktinomicetičkog ili drugog podrijetla, i/ili akutni kemijski bronhitis, akutni i/ili kronični kemijski plućni edem, neurogeni plućni edem, akutne i/ili kronične plućne manifestacije zbog zračenja, akutni i/ili kronični intersticijski plućni poremećaji, akutna plućna ozljeda/sindrom akutnog respiracijskog distresa (ALI/ARDS) u odrasloj dobi ili kod djeteta uključujući novorođenče, ALI/ARDS sekundarna uz upalu pluća i sepsu, aspiracijska upala pluća i ALI/ARDS sekundarna uz aspiraciju, ALI/ARDS sekundarna uz udisanje dimnih plinova, akutna ozljeda pluća izazvana transfuzijom (TRALI), ALI/ARDS i/ili akutna plućna insuficijencija nakon operacije, traume i/ili opeklina, i/ili oštećenje pluća izazvano mehaničkom ventilacijom (VILI), ozljeda pluća nakon aspiracije mekonija, plućna fibroza, planinska bolest, glomerulonefritis, akutna ozljeda bubrega, kardiorenalni sindrom, limfedem, upalna bolest crijeva, sepsa, septički šok, sindrom sustavnog upalnog odgovora (SIRS) neinfektivnog podrijetla, upalna bolest crijeva i urtikarija, koji sadrži davanje čovjeku ili životinji aktivne količine lijeka prema bilo kojem od zahtjeva 1 do 6.
8. Lijek prema zahtjevu 7, naznačen time da je kardiovaskularni, edematozni i/ili upalni poremećaj odabran iz skupine koju čine plućna hipertenzija, kronična opstruktivna plućna bolest, astma, akutni i/ili kronični plućni edem, alergijski alveolitis i/ili pneumonitis zbog udisanja organske prašine i čestica gljivičnog, aktinomicetičkog ili drugog podrijetla, i/ili akutni kemijski bronhitis, akutni i/ili kronični kemijski plućni edem, neurogeni plućni edem, akutne i/ili kronične plućne manifestacije zbog zračenja, akutni i/ili kronični intersticijski plućni poremećaji, akutna plućna ozljeda/sindrom akutnog respiracijskog distresa (ALI/ARDS) u odrasloj dobi ili kod djeteta uključujući novorođenče, ALI/ARDS sekundarna uz upalu pluća i sepsu, aspiracijska upala pluća i ALI/ARDS sekundarna uz aspiraciju, ALI/ARDS ALI/ARDS sekundarna uz udisanje dimnih plinova, akutna ozljeda pluća izazvana transfuzijom (TRALI), ALI/ARDS i/ili akutna plućna insuficijencija nakon operacije, traume i/ili opeklina, i/ili oštećenje pluća izazvano mehaničkom ventilacijom (VILI), ozljeda pluća nakon aspiracije mekonija, plućna fibroza, planinska bolest, koji sadrži davanje čovjeku ili životinji aktivne količine lijeka prema bilo kojem od zahtjeva 1 do 6.
9. Spoj s formulom (Ia)
[image]
ili jedna od njegovih soli, njegovi solvati ili solvati njegovih soli.
10. Spoj s formulom (II)
[image]
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EP11187735 | 2011-11-03 | ||
EP15192265.5A EP3075395B1 (en) | 2011-11-03 | 2012-10-30 | Polyethylene glycol based prodrug of adrenomedullin and use thereof |
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HRP20180319TT HRP20180319T1 (hr) | 2011-11-03 | 2018-02-21 | Predlijek adrenomedulina baziran na polietilen glikolu i njegova uporaba |
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IN2014DN03213A (hr) * | 2011-11-03 | 2015-05-22 | Bayer Ip Gmbh | |
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 |
AU2015323769A1 (en) | 2014-09-26 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Stabilized adrenomedullin derivatives and use thereof |
SG10202008963QA (en) | 2015-09-18 | 2020-10-29 | Univ Miyazaki | Long-acting adrenomedullin derivative |
CN110678550B (zh) | 2017-03-29 | 2023-11-14 | 国立大学法人宫崎大学 | 长效肾上腺髓质素衍生物 |
GB201707938D0 (en) | 2017-05-17 | 2017-06-28 | Univ Sheffield | Compounds |
CA3143584A1 (en) | 2019-06-18 | 2020-12-24 | Bayer Aktiengesellschaft | Adrenomedullin-analogues for long-term stabilization and their use |
JPWO2021112220A1 (hr) * | 2019-12-05 | 2021-06-10 | ||
US20230364245A1 (en) | 2020-04-03 | 2023-11-16 | Bayer Aktiengesellschaft | Pharmaceutical formulations polyethylene glycol-based prodrugs of adrenomedullin and use |
MX2022012332A (es) * | 2020-04-03 | 2022-10-27 | Bayer Ag | Formulaciones farmaceuticas liquidas de profarmacos a base de polietilenglicol de adrenomedulina y su uso. |
CN116438200A (zh) | 2020-09-10 | 2023-07-14 | 普雷西里克斯公司 | 针对fap的抗体片段 |
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 | A process for the preparation of polyethylene glycol-modified adrenomedullin, its intermediates and their use |
WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | Precirix N.V. | Pre-targeting |
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IN2014DN03213A (hr) * | 2011-11-03 | 2015-05-22 | Bayer Ip Gmbh |
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