Norskhydro Asa

Norsk Hydro, A.s.

Bernt B&oslash;rretzen

Finn Myhren

Are Dalen

Kjell Torgeir Stokke

Marit Liland Sandvold

The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO&mdash;, RCONH&mdash;, RCOS&mdash;, RCH O&mdash;, RCH NH&mdash;, &mdash;COOCH R, &mdash;CONHCH R and &mdash;SCH R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.

Fatty acid derivatives

New compounds of the general formula (I): Nu-O-Fa, wherein O represents an oxygen, Nu is a nucleoside or nucleoside analogue, and Fa is an acyl group of a mono-unsaturated C18 or 20 fatty acid. The invention also concerns anti viral pharmaceutical and veterinary compositions comprising a compound of formula (I) alone in a combination with a pharmaceutically acceptable carrier.

Fatty acid esters of nucleoside analogs

The invention provides Gemcitabine esters or amides in which the 3&prime;- and/or 5&prime;-OH group and/or the N -amino group is derivatised with a C - and/or C -saturated or mono-unsaturated acyl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-eicosenoyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti-cancer and anti-viral agents.

Gemcitabine derivatives

Therapeutic agents

This invention relates to new nucleoside derivatives of formula (I); wherein R,and R,are independently selected from hydrogen, elaidoyl, oleoyl, stearoyl, eicosenoyl (cis or trans) and eicosanoyl, with the provisos that R,and R,cannot both be hydrogen, oleoyl or stearoyl, R,cannot be hydrogen when R,is oleoyl or stearoyl, and R,cannot be hydrogen when R,is elaidoyl, oleoyl or stearoyl. Further, the invention relates to the use of the nucleoside derivatives of formula (I) wherein R,and R,are independently selected from hydrogen, and C,- and C,-saturated and mono-unsaturated acyl groups, with the provisos that R,and R,cannot both be hydrogen, in the manufacture of a pharmaceutical preparation for the treatment of tumours.

Growing community of inventors

Heistad, Norway

Bernt Børretzen

Growing community of inventors

Heistad, Norway

Bernt B&oslash;rretzen

Bernt Børretzen