Abstract: A method of preparing an active agent or a salt thereof from a pro-drug first compound (1) comprising a propargyl group connected to an oxygen that is directly or indirectly connected to the active agent is provided, wherein the bond between the propargyl group and the oxygen is cleaved by reacting the first compound with palladium or gold, thereby releasing the active agent. Prodrug compositions suitable for use in the method are also provided.

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, (Formula (I)) wherein: R1 is (CH2)mNR11R12; R2 is selected from H, halo, OR13, NHR13, alkyl, alkenyl and alkynyl; R3 is selected from alkyl, alkenyl, alkynyl, aryl, halo, aryloxy, NHCO2R4, NHCONR5R6, NHCOR7, NH-alkyl, NH-alkenyl, NH(CH2);n-aryl, (CH2)p-heteroaryl, (CH2)qCO2R8, (CH2)rCOR9 and NHSO2R10, wherein each alkyl, alkenyl, aryl or heteroaryl moiety in the aforementioned list is optionally further substituted by one or more groups selected from alkyl, halo OH, NH2, alkoxy, aryloxy, alkylamino, arylamino, carboxyl and carboxamide; R4 to R10 and R13 are each independently selected from alkyl, alkenyl and aryl; R11 and R12 are each independently selected from alkyl and alkenyl; or R11 and R:12 are linked together with the nitrogen to which they are attached to form a heterocycloalkyl or heterocycloalkenyl group; n, m, p, q and r are each independently selected from 0, 1, 2, 3, 4, 5

Abstract: The invention provides a new bioorthogonal deprotection method for preparing heterocyclic compounds by bond cleavage using palladium. The methods have general application in the field of biological synthetic chemistry. Compounds, such as prodrugs, which are useful in such methods are also provided.

Abstract: A first aspect of the-invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, (Formula (I)) wherein: R1 is (CH2)mNR11R12; R2 is selected from H, halo, OR13, NHR13, alkyl, alkenyl and alkynyl; R3 is selected from alkyl, alkenyl, alkynyl, aryl, halo, aryloxy, NHCO2R4, NHCONR5R6, NHCOR7, NH-alkyl, NH-alkenyl, NH(CH2);n-aryl, (CH2)p-heteroaryl, (CH2)qCO2R8, (CH2)rCOR9 and NHSO2R10, wherein each alkyl, alkenyl, aryl or heteroaryl moiety in the aforementioned list is optionally further substituted by one or more groups selected from alkyl, halo OH, NH2, alkoxy, aryloxy, alkylamino, arylamino, carboxyl and carboxamide; R4 to R10 and R13 are each independently selected from alkyl, alkenyl and aryl; R11 and R12 are each independently selected from alkyl and alkenyl; or R11 and R:12 are linked together with the nitrogen to which they are attached to form a heterocycloalkyl or heterocycloalkenyl group; n, m, p, q and r are each independently selected from 0, 1, 2, .3.

Abstract: The invention provides a new bioorthogonal deprotection method for preparing heterocyclic compounds by bond cleavage using palladium. The methods have general application in the field of biological synthetic chemistry. Compounds, such as prodrugs, which are useful in such methods are also provided.

Abstract: The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; (ii) a linking moiety of formula (5): —(HNR5)2NC(O)R3C(O)—??(5), wherein: each R5 is independently an optionally substituted C1-4 alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.

Abstract: The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; (ii) a linking moiety of formula (5): —(HNR5)2NC(O)R3C(O)—??(5), wherein: each R5 is independently an optionally substituted C1-4 alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.

Abstract: This invention relates to cationic lipids. More particularly the invention relates to biodegradable cationic lipids having a plurality of cationic headgroups and one or more lipophilic tail groups. The lipids are of utility in various applications, and in particular in permitting transfection of molecules, and in particular DNA and RNA, into cells. As such the lipids have specific utility in the field of gene therapy as well as other applications such as delivery of small molecules into cells, detergents, and metal ion complexation for medical or industrial applications.