HRP20210351T1 - Spojevi prostaciklina - Google Patents
Spojevi prostaciklina Download PDFInfo
- Publication number
- HRP20210351T1 HRP20210351T1 HRP20210351TT HRP20210351T HRP20210351T1 HR P20210351 T1 HRP20210351 T1 HR P20210351T1 HR P20210351T T HRP20210351T T HR P20210351TT HR P20210351 T HRP20210351 T HR P20210351T HR P20210351 T1 HRP20210351 T1 HR P20210351T1
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- 150000003815 prostacyclins Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 7
- 208000002815 pulmonary hypertension Diseases 0.000 claims 7
- 150000002632 lipids Chemical class 0.000 claims 6
- 230000002209 hydrophobic effect Effects 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- LVNGJLRDBYCPGB-UHFFFAOYSA-N 1,2-distearoylphosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)OCC[NH3+])OC(=O)CCCCCCCCCCCCCCCCC LVNGJLRDBYCPGB-UHFFFAOYSA-N 0.000 claims 2
- HKJAWHYHRVVDHK-UHFFFAOYSA-N 15,16,17-trihydroxyhentriacontane-14,18-dione Chemical compound CCCCCCCCCCCCCC(=O)C(O)C(O)C(O)C(=O)CCCCCCCCCCCCC HKJAWHYHRVVDHK-UHFFFAOYSA-N 0.000 claims 2
- NEZDNQCXEZDCBI-UHFFFAOYSA-N 2-azaniumylethyl 2,3-di(tetradecanoyloxy)propyl phosphate Chemical compound CCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCCN)OC(=O)CCCCCCCCCCCCC NEZDNQCXEZDCBI-UHFFFAOYSA-N 0.000 claims 2
- RWYUSQRZIOPEQX-UHFFFAOYSA-N [2-aminoethoxy(hexadecanoyloxy)phosphoryl] hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OP(=O)(OCCN)OC(=O)CCCCCCCCCCCCCCC RWYUSQRZIOPEQX-UHFFFAOYSA-N 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- 230000000996 additive effect Effects 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims 2
- FRKBLBQTSTUKOV-UHFFFAOYSA-N diphosphatidyl glycerol Natural products OP(O)(=O)OCC(OP(O)(O)=O)COP(O)(O)=O FRKBLBQTSTUKOV-UHFFFAOYSA-N 0.000 claims 2
- 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 229920002523 polyethylene Glycol 1000 Polymers 0.000 claims 2
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 1
- -1 PEG500 Chemical compound 0.000 claims 1
- 229920002560 Polyethylene Glycol 3000 Polymers 0.000 claims 1
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 1
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 125000002960 margaryl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000008520 organization Effects 0.000 claims 1
- 125000002958 pentadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 150000003505 terpenes Chemical class 0.000 claims 1
- 235000007586 terpenes Nutrition 0.000 claims 1
Classifications
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- C07C235/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
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Claims (10)
1. Spoj formule (II):
[image]
naznačen time što R1 je O;
R2 je tetradecil, pentadecil, heksadecil, heptadecil ili oktadecil; i
n je 1.
2. Spoj prema patentnom zahtjevu 1, naznačen time što R2 je heksadecil.
3. Farmaceutski pripravak naznačen time što sadrži spoj prema zahtjevu 1 ili 2 i PEGilirani lipid.
4. Farmaceutski pripravak prema patentnom zahtjevu 3, naznačen time što PEGilirani lipid sadrži PEG400, PEG500, PEG1000, PEG2000, PEG3000, PEG4000 ili PEG5000.
5. Farmaceutski pripravak prema patentnom zahtjevu 3 ili 4, naznačen time što je lipidni dio PEGiliranog lipida kolesterol, dimiristoil fosfatidiletanolamin (DMPE), dipalmitoil fosfoetanolamin (DPPE), distearoilfosfatidiletanolamin (DSPE), dimiristoilglicerol (DMG), difosfatidilglicerol (DPG) ili disteraroilglicerol (DSG).
6. Pripravak prema patentnom zahtjevu 3, naznačen time što je PEGilirani lipid kolesterol-PEG2000, DSPE-PEG1000 ili DSG-PEG2000.
7. Pripravak prema bilo kojem od patentnih zahtjeva 3-6, naznačen time što nadalje sadrži hidrofobni aditiv, pri čemu je hidrofobni aditiv ugljikovodik, terpen ili hidrofobni lipid.
8. Spoj prema patentnom zahtjevu 1 ili 2, ili pripravak prema bilo kojem od zahtjeva 3-7, naznačen time što se koristi u postupku liječenja plućne hipertenzije (PH) kod pacijenta kojem je to potrebno.
9. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 8, naznačen time što pacijent je pacijent iz PH skupine I Svjetske zdravstvene organizacije (WHO), pacijent iz PH skupine II WHO, pacijent iz PH skupine III WHO, pacijent iz PH skupine IV WHO ili pacijent iz PH skupine V WHO.
10. Spoj ili pripravak za uporabu prema patentnom zahtjevu 8, naznačen time što se spoj ili njegova farmaceutski prihvatljiva sol ili pripravak daje pacijentu oralnim, nazalnim, potkožnim, plućnim ili intravenskim putem primjene.
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EP14855785.3A EP3060041B1 (en) | 2013-10-25 | 2014-10-24 | Prostacyclin compounds |
PCT/US2014/062232 WO2015061720A2 (en) | 2013-10-25 | 2014-10-24 | Prostacyclin compounds, compositions and methods of use thereof |
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