Abstract:
Die vorliegende Erfindung betrifft lipidanaloge Phosphorsäureverbindungen und insbesondere Phosphorsäuretriester, Phosphorsäurediesteramide sowie Phosphorsäurediester. Bevorzugt handelt es sich um kationische Phospholipide, welche vorzugsweise wenigstens eine freie Hydroxylgruppe aufweisen.
Abstract:
Die Erfindung betrifft neue Strukturanaloga zu Phosphatidyloligoglycerinen. Diese Verbindungen können insbesondere zur Herstellung von Liposomen mit langer Zirkulationszeit mit oder ohne Thermolabilität eingesetzt werden. Die Erfindung betrifft weiterhin solche Verbindungen enthaltende Liposome sowie Arzneimittelzusammensetzungen.
Abstract:
The invention concerns a pharmaceutical preparation which improves penetration of active substances through the tissue membrane or barrier of the target organ.
Abstract:
Ein thermolabiles Liposom mit geregelter Freigabetemperatur für den Liposominhalt ist im Wesentlichen aus mindestens einem Phosphatidylcholin mit einer Hauptumwandlungstemperatur, die im Bereich von 0 bis 80 °C liegt und 2 bis 15 Gew.-% Phosphatidyloligoglycerin gebildet.
Abstract:
The invention concerns compounds of the general formula (I), in which R is a C10-C22 alkyl group, R is an O-CO-R , NH-CO-R , -OH, -OCH3, -OC2H5, -OC3H7, -NH2, -NHCH3, -N(CH3)2 or -N (CH3)3Cl group, R is a C1-C20 alkyl group and R is one of the following groups: -C2H4-N (CH3)3, -C2H4-N H(CH3)2, -C2H4-N H2CH3, -C2H4-N H3, pentahydroxycyclohexanyl derivatives, in particular myo-inositol derivatives, 1,2- or 2,3-(R or S)-dihydroxypropanyl, seryl (D or L), N-methylseryl (D or L), N,N-dimethylseryl, (D or L), N,N,N-trimethylseryl (D or L), H, methyl, ethyl, hydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, R and (II) being interchangeable with each other, plus enantiomers thereof.
Abstract:
Die vorliegende Erfindung betrifft neue Arzneimittelformulierungen, die als Wirkstoffe Alkylphosphocholine und Analoga, Alkyl-alkandiol-phoshocholine und Analoga sowie (Ether)- Lysolecithine und Analoga in verschiedenen Ausführungsformen enthalten. Die Wirkstoffe sind dabei integrale Bestandteile von Liposomen, die außerdem Cholesterin und Analoga sowie einen negativen Ladungsträger enthalten. Die Arzneimittelformulierungen sind besonders geeignet zur Behandlung oder / und Prophylaxe von Krebs, von Protozoenerkrankungen wie Leishmaniosen und Amöbenerkrankungen, von Acariasis und von Erkrankungen, die durch Arthropoden verursacht werden sowie von bakteriellen Erkrankungen, wie z. B. Ehrlichiose, geeignet. Auch Augenerkrankungen, die mit unkontrollierten zellulären Prozessen einhergehen, können günstig beeinflusst werden.
Abstract:
The mannite derivatives have the formula (I) wherein R and R , identical or different, represent when they are identical a straight or branched alkyl, alkenyl or alkynyl group containing from 6 to 24 atoms of carbon which may be substituted by a cycloalkyl rest having from 3 to 6 atoms of carbon, an aryl, benzyloxy, allyloxy, mesyloxy rest and/or halogen atoms and when R and R are different, they represent a straight or branched alkyl group with 1 to 24 atoms of carbon, which may be substituted by a cycloalkyl rest having from 3 to 6 atoms of carbon, an aryl, benzyloxy, allyloxy, mesyloxy rest and/or halogen atoms, with the possibility for R of being also a trityl group. From said mannite derivatives, it is possible to obtain in a simple way and with good yields the phospholipids in the form of their optical stereo isomers.
Abstract:
PCT No. PCT/EP93/00605 Sec. 371 Date Feb. 15, 1995 Sec. 102(e) Date Feb. 15, 1995 PCT Filed Mar. 16, 1993 PCT Pub. No. WO93/18749 PCT Pub. Date Sep. 30, 1993The present invention concerns liposomes with a negative excess charge and pharmaceutical compositions produced therefrom. The liposomes contain 30 to 50 mol % cholesterol, 49 to 56 mol % phospholipids and 1 to 14 mol % of one or several compounds of the general formula I (I) or salts thereof in relation to the total lipid components of the liposomes, in which R1 and R2 are the same or different and represent hydrogen, C1-C4 alkyl groups or saturated or unsaturated C8-C24 acyl groups which are unbranched or branched or/and unsubstituted or substituted, provided that at least one of the residues R1 and R2 is an acyl group as defined above. A process for the production of the liposomes in accordance with the invention is also provided.
Abstract:
A b s t r a c t New liposome structures are described which are characterized in that they contain at least 1 mol-% of a compound having the general formula (I) with an excess positive charge (I) in which R1 denotes alkoyl or alkyl each with 14 to 18 C atoms, oleoyl or oleyl, R2 denotes the group PNN R3 = -O-R1, -O-PNN, -O-Gly, NH3+, NH2CH3+, NH(CH3)2 or N(CH3)3+, R has one of the meanings stated for R1, R2 or R3 and n denotes a whole number from 0 to 3, and preferably denotes 0, provided that the molecule contains one of the said groups with a positive charge. Due to their organ-specific characteristics the liposomes according to the present invention are especially suitable as pharmaceutical carriers in a pharmaceutical preparation for the treatment of diseases in the liver organ which contains one or several active substances which are active in the liver enclosed in the liposomes according to the present invention.