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1 PATENTNI ZAHTEVKI 1. Spojina, ki je označena s tem, da ima splošno formulo 1 ooA compound which is characterized in that it has the general formula Io*2 ali njena stereoizomema komponenta, v katere formuli je položaj 1,2 nasičen ali pa je tam dvojna vez, Ri je vodik ali razvejen ali nerazvejen ogljikovodik, ki ima verigo z 1-4 ogljikovimi atomi, R2 je razvejen ali nerazvejen ogljikovodik, ki ima verigo z 1-10 ogljikovimi atomi, R3 je acil, ki ima razvejeno ali nerazvejeno, nasičeno ali nenasičeno ogljikovodikovo verigo z 11-20 ogljikovimi atomi in sta Xi in X2 oba fluor, in pod pogojem, da kadar je na položaju 1,2 dvojna vez, Ri in R2 nista naenkrat metilni skupini.* 2 or a stereoisomeric component thereof, in the formula of which the position 1,2 is saturated or there is a double bond, R 1 is hydrogen or a branched or unbranched hydrocarbon having a chain of 1-4 carbon atoms, R 2 is a branched or unbranched hydrocarbon which has a chain of 1-10 carbon atoms, R3 is acyl having a branched or unbranched, saturated or unsaturated hydrocarbon chain of 11-20 carbon atoms and Xi and X2 are both fluorine, and provided that when in position 1.2 double bond, R 1 and R 2 are not simultaneously methyl groups.2. Spojina po prvem zahtevku, kije označena s tem, daje v splošni formuli 1 položaj 1,2 nasičen.A compound according to the first claim, characterized in that in general formula 1 the position 1,2 is saturated.3. Spojina po kateremkoli izmed zahtevkov 1-2, ki je označena s tem, daje R3 acil, ki ima 11-20 ogljikovih atomov. 2A compound according to any one of claims 1-2, wherein R 3 is acyl having 11-20 carbon atoms. 24. Spojina po tretjem zahtevku, kije označena s tem, daje položaj 1,2 nasičen, Ri je vodik, R2 je propilna skupina, Xj je fluor in X2 je fluor.A compound according to the third claim, wherein position 1,2 is saturated, R 1 is hydrogen, R 2 is a propyl group, X 1 is fluorine and X 2 is fluorine.5. Spojina po prvem zahtevku, ki je označena s tem, da je na položaju 1,2 dvojna vez, Ri je vodik, R2 je propilna skupina, R3 je palmitoilna skupina, Xi je fluor, X2 je fluor.A compound according to the first claim, characterized in that at position 1,2 there is a double bond, R 1 is hydrogen, R 2 is a propyl group, R 3 is a palmitoyl group, X 1 is fluorine, X 2 is fluorine.6. Spojina po prvem zahtevku, kije označena s tem, da ima formulo n c=oA compound according to the first claim, which has the formula n c = o7. Postopek za pripravo spojine s splošno formulo 1, kakor je definirana v prvem zahtevku, kije označen s tem, da obsega a) reakcijo spojine s formulo CHaOH c.oA process for the preparation of a compound of general formula 1 as defined in the first claim, which comprises a) reacting a compound of formula CHaOH c.o.X| kjer so Ri, R2, Xi in X2 definirani kot v prvem zahtevku, s spojino s formulo 3 RtCOOH kjer je R4 razvejena ali nerazvejena, nasičena ali nenasičena alkilna skupina, ki ima 10-19 ogljikovih atomov, ali b) reakcijo spojine s formuloX | wherein R 1, R 2, X 1 and X 2 are as defined in the first claim, with a compound of formula 3 RtCOOH wherein R 4 is a branched or unbranched, saturated or unsaturated alkyl group having 10-19 carbon atoms, or b) the reaction of a compound of formulakjer so Rj, R2, Xj in X2 definirani kot v prvem zahtevku, s spojino s formulo R4COX kjer je R4 definiran kakor zgoraj in je X halogen ali alifatski del -OOCR4, ali c) reakcijo spojine s fomulowherein R 1, R 2, X 1 and X 2 are as defined in the first claim, with a compound of formula R 4 COX wherein R 4 is as defined above and X is halogen or an aliphatic moiety of -OOCR 4, or c) reacting the compound with formula4 kjer so Rb R2 Xi in X2 definirani kot v prvem zahtevku in je Y halogen, mezilat ali p-toluensulfonat, s spojino s formulo R4COOA® kjer je Rj definiran zgoraj in A® je kation, nakar, če je tako dobljena spojina epimema zmes in želimo čisti epimer, ločimo epimemo zmes v njene stereoizomeme komponente.4 wherein R b R 2 X 1 and X 2 are as defined in the first claim and Y is halogen, mesylate or p-toluenesulfonate, with a compound of formula R 4 COOA® wherein R 1 is as defined above and A® is a cation, whereas if the compound thus obtained is an epime mixture and wanting a pure epimer, we separate the epime mixture into its stereoisomeric components.8. Postopek po sedmem zahtevku, ki je označen s tem, da pripravimo spojino, ki ustreza kateremukoli izmed zahtevkov 2-6.Process according to claim 7, characterized in that a compound according to any one of claims 2-6 is prepared.9. Farmacevtski preparat, ki je označen s tem, da kot aktivno sestavino vsebuje spojino, ki ustreza kateremukoli izmed zahtevkov 1-6.Pharmaceutical preparation, characterized in that it contains as active ingredient a compound according to any one of Claims 1 to 6.10. Farmacevtski preparat, ki ustreza zahtevku 9 in je označen s tem, da vsebuje liposome, ki vsebujejo farmakološko aktivno spojino, ki ustreza zahtevku 3.Pharmaceutical preparation according to Claim 9, characterized in that it contains liposomes containing a pharmacologically active compound according to Claim 3.11. Farmacevtski preparat po zahtevkih 9-10, kije označen s tem, daje v obliki enote za doziranje.Pharmaceutical preparation according to Claims 9 to 10, characterized in that it is in the form of a dosage unit.12. Farmacevtski preparat po zahtevkih 9-11, kije označen s tem, da vsebuje aktivno sestavino, združeno s farmacevtsko sprejemljivim nosilcem.Pharmaceutical composition according to Claims 9 to 11, characterized in that it contains the active ingredient in association with a pharmaceutically acceptable carrier.13. Spojina po kateremkoli izmed zahtevkov 1-6, kije označena s tem, daje uporabna kot terapevtsko aktivna substanca.A compound according to any one of claims 1-6, which is useful as a therapeutically active substance.14. Uporaba spojine po kateremkoli od zahtevkov 1-6 za pripravo zdravil z anti-inflamatomo in antialergijsko aktivnostjo.Use of a compound according to any one of claims 1-6 for the preparation of medicaments with anti-inflammatory and anti-allergic activity.
SI9210064A1991-02-041992-01-22Novel antiinflamatory and antialergic active compounds, glucocorticosteroids and processes for their preparation
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