Abstract: A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent.

Abstract: This invention relates to compounds to formula (1) wherein B is optionally substituted aryl; R1 and R2 are the same or different and are independently selected from hydrogen or C1-3 alkyl; n is 1 or 2, preferably n is 1; m is 0 or 1; R3 is hydrogen or acyl, R4 and R5 are the same or different and are independently selected from amino, alkylamino, dialkylamino, arylamino and C2-C4 cycloalkylamino; X and Y are independently selected from C, H or N provided at least one of X and Y is N; and salts thereof, solvates thereof, pharmaceutically acceptable derivatives thereof, prodrugs thereof, tautomers thereof and/or isomers thereof, and processes for their reparation and methods of treatment, pharmaceutical formulations and uses involving them.

Abstract: Arylalkylpiperazine compounds (1) wherein B is aryl or optionally substituted aryl; R1 is hydroxy; R2 and R3 are the same or different and are independently selected from hydrogen or C1-3 alkyl; m is 0, 1 or 2; D is a linking chain of atoms which may be optionally substituted and which contains from 1 to 8 atoms in the chain; E is a phenolic antioxidant group or a corresponding amino derivative thereof wherein the phenolic hydroxyl is replaced by amino, are disclosed. The compounds have both free radical scavenging activity and block excitatory amino acid activity. Some compounds of the present invention also display an affinity for voltage-sensitive sodium channels.

Abstract: The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (.+-.)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: The present method provides a short, convergent total synthesis of novel intermediates in the synthesis of (.+-.)-camptothecin and related compounds. The synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the Camptothecin compound. In the synthesis, the following novel precursor is reacted with a phenyl isocyanide: ##STR1## The resulting tetracyclic intermediates comprise a quinoline fused to a pyrrolidine ring, with the pyrrolidine ring being fused to an alpha-pyridone ring. The tetracyclic intermediates thus comprise the A, B, C, and D rings characteristic of camptothecin and camptothecin derivatives, and are easily convertible to camptothecin and camptothecin derivatives via hydroxymethylation and oxidation.