Max-planck-gesellschaft Zur F&#xf6;rderung Der Wissenschaften E. V.

Ciba-geigy Corporation

Asta Pharma Aktiengesellschaft

Thermosome Gmbh

Hansjorg Eibl

Alfar Nicksch

Clemens Unger

Jurgen Engel

Walter Diembeck

Lajos Tarcsay

Peter Fankhauser

Anita Peil

Petra Kaufmann-Kolle

Stephan Kovatchev

Lars H Lindner

Stephen Kovatchev

Anneliese Kranich

The invention relates to a thermolabile liposome with a controlled release temperature for the liposome content, in particular a liposome which is stable at 37&#xb0; C. in serum and with a controlled release temperature of between 40 and 80&#xb0; C.

Thermolabile liposome with a controlled release temperature

The invention concerns a new pharmaceutical agent for oral or topical administration in the treatment of protozoal diseases, in particular of leishmaniasis, which contains as the active substance one or several compounds having the general formula I ##STR1## in which R.sup.1 is a saturated or monounsaturated or polyunsaturated hydrocarbon residue with 12 to 20 C atoms and R.sup.2, R.sup.3 and R.sup.4 denote independently of one another hydrogen, a C.sub.1 -C.sub.5 alkys group, a C.sub.3 -C.sub.6 cycloalkyl group or a C.sub.1 -C.sub.5 hydroxyalkyl group whereby two of the residues R.sup.2, R.sup.3 and R.sup.4 can together form a C.sub.2 -C.sub.5 alkylene group which, if desired, can be substituted with an --O--, --S-- or NR.sup.5 group, in which R.sup.5 is hydrogen, a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group or a C.sub.1 -C.sub.5 hydroxyalkyl group as well as, if desired the usual pharmaceutical auxiliary, diluting, carrier or/and filling substances.

Process for the production of a pharmaceutical agent for oral or topical

Cytotoxic therapeutic compositions contain as active ingredients compounds of the formula

Compositions containing a mixture of phosphorus compounds and

Liposomes with a negative excess charge

The present invention provides compounds of the formula: ##STR1## wherein R is a erucyl, brassidyl or nervonyl radical, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification, A is a valency bond or a radical as defined in the specification, and X is an oxygen atom when A is a valency bond or is an oxygen or sulphur atom when A is another radical. The present invention also provides a process for the preparation of the compounds of general formula (I) and pharmaceutical compositions containing them which can be used for the treatment of protozoal and fungal diseases, auto-immune diseases and bone marrow damage.

Eurcyl, brassidyl and nervonyl derivatives

The use of alkylphosphoric acid compounds of Formula I

Use of hexadecylphosphocholine for the treatment of psoriasis

Medicament with improved penetration of the tissue membrane

The invention relates to compositions containing hexadecylphosphocholine the use of these in treating various cancers.

Compositions containing hexadecylphosphocholine and use thereof

The invention relates to pharmaceutical compositions containing synthetic, substantially pure phosphatidyl serine and phosphatidyl choline and a substance or a mixture of substances having biological activity. The invention also relates to mixtures comprising synthetic, substantially pure phosphatidyl serine and phosphatidyl choline, and also to processes for the manufacture of the pharmaecutical compositions, and the use thereof.

Liposomes of synthetic lipids

Compositions containing hexadecylophosphocholine and alkylglycerols and

Compounds related to phospholipids and a method for their preparation are sclosed.

Phospholipid-like compounds

The invention concerns D-mannitol derivatives of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, and when R.sup.1 R.sup.2 are the same, signify a straight-chained or branched alkyl, alkenyl or alkynyl group with 6 to 24 carbon atoms, which can contain cycloalkyl radicals with 3 to 6 carbon atoms, aryl radicals, benzyloxy, allyloxy, mesyloxy and/or halogen substituents and, when R.sup.1 and R.sup.2 are different, signify a straight-chained or branched alkyl group with 1 to 24 carbon atoms, which can contain cycloalkyl radicals with 3 to 6 carbon atoms, aryl radicals, benzyloxy, allyloxy, mesyloxy and/or halogen substituents, or a straight-chained or branched alkenyl or alkynyl group with 3 to 24 carbon atoms, which can contain cycloalkyl radicals with 3 to 6 carbon atoms, aryl radicals, benzyloxy, allyloxy, mesyloxy and/or halogen substituents, and R.sup.1 can also be trityl. Starting from these D-mannitol derivatives, there can be obtained, in simple manner and with good yields, phospholipids in the form of their optically pure stereoisomers.

D-mannite derivatives as starting products for the synthesis of

Compounds related to phospholipids and a method for their preparations.

The invention concerns derivatives of N,N-bis(2-chloroethyl)-phosphoric acid amide of general formula I ##STR1## wherein X and Y are the same or different and signify oxygen or NR.sup.3, R.sup.1 and R.sup.2 are the same or different and R.sup.1 signifies the radical CH.sub.2 (OR.sup.4)--CH.sub.2 --CH.sub.2 --, CH.sub.2 (OR.sup.4)--CH(CH.sub.3)--CH.sub.2 -- or CH.sub.2 (OR.sup.4)--CH(OR.sup.5)--CH.sub.2 -- and, when X is an NR.sup.3 group, can also be hydrogen, R.sup.2 possesses one of the meanings of R.sup.1 or is ethyl, propyl, allyl, propenyl, chloroethyl, methyl or benzyl, R.sup.3 is hydrogen, methyl, ethyl, propyl or allyl and wherein the radicals R.sup.4 and R.sup.5 are the same or different and represent an alkyl radical R or an acyl radical --COR, whereby R signifies a straight-chained or branched, saturated or unsaturated alkyl group with 1 to 25 carbon atoms, or an aralkyl radical with 1 to 25 carbon atoms in the alkyl chain, and one of the radicals can also be a hydrogen atom, as well as processes for their preparation. The compounds according to the invention display an outstanding antitumour action comparable with the action of cyclophosphamide.

Growing community of inventors

Bovenden, Germany

Hansjorg Eibl