Fatty acid derivatives
AssigneeNorsk Hydro ASA
InventorsFinn Myhren, Bernt Borretzen, Are Dalen, Marit Liland Sandvold
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Abstract
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—, RCONH—, RCOS—, RCH 2 O—, RCH 2 NH—, —COOCH 2 R, —CONHCH 2 R and —SCH 2 R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.
Claims55
A lipophilic derivative of a biologically active compound containing in its molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups, other than a nucleoside or nucleoside derivative, said lipophilic derivative being characterised by a molecular structure in which the or at least one said functional group of said biologically active compound is replaced by a lipophilic group selected from those of the formula:
- RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.
The compound:
- 11β, 17α, 21-trihydroxy-pregna-1,4-diene-3,20-dione-21-elaidate.
The compound:
- 9-fluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione-21-elaidate.
The compound:
- (2-[2,6-dichlorophenyl)amino-benzeneacetic acid)-(cis-9′-octadecenyl)ester.
The compound:
- 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid (cis-9-octadecenyl)amide.
The compound:
- S(+)-2-(6-methoxy-2-naphthyl)-propionic acid (cis-9′-octadecenyl)amide.
The compound:
- S(+)-2-(6-methoxy-2-naphthyl)-propionic acid-cis-9′-octadecenyl ester.
The compound:
- 4-O-(trans-9′-octadecenoyl)-2-methyl-N(2-pyridyl)-2H-1,2-benzolthiazone-3-carboxamide-1,1-dioxide.
The compound:
- 4-O-(cis-11′-eicosenoyl)-2-methyl-N(2-pyridyl)-2H-1,2-benzothiazone-3-carboximide-1,1-dioxide.
The compound:
- 2-hydroxy-benzoic acid-(cis-9′-octadecenyl)ester.
The compound:
- 2-(cis-9′-octadecenoxy)-ethyl benzoate.
The compound:
- 2-(cis-9′-octadecenoxy)-benzoic acid.
The compound:
- S(+)-2-(6-[cis-9′-octadecenoxy]-2-naphthyl)-propionic acid ethyl ester.
The compound:
- S(+)-2-(6-[cis-9′-octadecenoxy]-2-naphthyl)-propionic acid.
The compound:
- chlorambucil-oleyl ester.
The compound:
- elaidic acid mephalan amide.
The compound:
- taxol-2′-elaidate.
The compound:
- elaidic acid daunorubicin amide.
The compound:
- elaidic acid doxorubicin amide.
The compound:
- daunorubicine oleyl carbamate.
The compound:
- doxorubicin oleyl carbamate.
The compound:
- p-amino-salicylic acid elaidylester.
The compound:
- 4-(elaidamido)salicylic acid.
The compound:
- elaidic acid chloramphenicol ester.
The compound:
- oxacillin oleyl ester.
The compound:
- elaidic acid ampicillin amide.
The compound:
- ampicillin oleyl ester.
The compound:
- 7-chloro-4-[4-[ethyl(2-elaidoyloxyethyl)-amino]]-methylbutylamino]quinolone.
The compound:
- 3-(α-acetonylbenzyl)-4-elaidoyloxycoumarin.
A method for modifying the activity of a biologically active compound containing in its molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups, other than a nucleoside or nucleoside analogue, comprising replacing the or at least one said functional group of said biologically active compound by a lipophilic group selected from those of the formula:
- RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.
Dependencies are inferred from the claim text.