Abstract: The present invention provides di-substituted acetalanthraquinone-based compounds of the Formulae (l)-(IV) that are useful for cellular staining and for light-based detection of biological material, e.g. fluorescence-based detection of biological material. These compounds may be used in hydrolysed or non-hydrolysed form. Also provided is a fluorescent complex that comprises a nucleic acid and an acetalanthraquinone-based compound of the invention; and a method of staining a biological sample comprising cells or other biological material containing nucleic acid, which method comprises contacting the biological sample with an acetalanthraquinone-based compound of the invention. In the Formulae (l)-(IV), A and B are each independently of formula —RaCH2CH(ORb)2; or one of A and B is of formula —RaCH2CH(ORb)2 and the other one is of formula: —NRb2.

Abstract: A pharmaceutical composition comprising lidocaine N-oxide (LNO), or a pharmaceutically acceptable salt thereof, for use in a method of treatment, said method being a prophylactic treatment to prevent, or decrease the likelihood of, sudden cardiac death associated with ventricular fibrillation (VF) in a subject, whereby the composition is provided to the subject's bloodstream via the oral mucous membrane or via pulmonary absorption in the lungs or by IV administration.

Abstract: According to the invention there is provided a compound of Formula (I) in which: A is a C2-8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1-A-NR2R3R4+(Zm?)1/m, for halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm?)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarized.

Abstract: A pharmaceutical composition comprising lidocaine N-oxide (LNO), or a pharmaceutically acceptable salt thereof, for use in a method of treatment, said method being a prophylactic treatment to prevent, or decrease the likelihood of, sudden cardiac death associated with ventricular fibrillation (VF) in a subject, whereby the composition is provided to the subject's bloodstream via the oral mucous membrane or via pulmonary absorption in the lungs or by IV administration.

Abstract: The present invention provides di-substituted acetalanthraquinone-based compounds of the Formulae (l)-(IV) that are useful for cellular staining and for light-based detection of biological material, e.g. fluorescence-based detection of biological material. These compounds may be used in hydrolysed or non-hydrolysed form. Also provided is a fluorescent complex that comprises a nucleic acid and an acetalanthraquinone-based compound of the invention; and a method of staining a biological sample comprising cells or other biological material containing nucleic acid, which method comprises contacting the biological sample with an acetalanthraquinone-based compound of the invention. In the Formulae (l)-(IV), A and B are each independently of formula —RaCH2CH(ORb)2; or one of A and B is of formula —RaCH2CH(ORb)2 and the other one is of formula: —NRb2.

Abstract: According to the invention there is provided a compound of Formula (X) in which: A is a C2-C8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1—A—NR2R3R4+(Zm-)1/m, for halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm-)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarised.

Abstract: According to the invention there is provided a compound of Formula (I) in which: A is a C2-8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1-A-NR2R3R4+(Zm?)1/m, halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm?)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarised.

Abstract: According to the invention there is provided a compound of Formula (I) in which: A is a C2-8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1-A-NR2R3R4+(Zm?)1/m, halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm?)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarised.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which C is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, which it will act as a DNA alkylating agent preventing cell division.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, where it will act as a DNA alkylating agent preventing cell division.

Abstract: There is disclosed a compound of formula (I) wherein each of X1 and X2 are independently NH-A-NR1R2, and wherein A is A C2-8 alkylene and R1 and R2 are independently selected from hydrogen, C1-4 alkyl, C2-4 hydroxy-alkyl and C2-4 aminoalkyl, or R1 and R2 together form a C2-6 alkylene group which with the nitrogen atom to which R1 and R2 are attached forms a heterocyclic ring, or an N-oxide derivative thereof, and wherein the compound (I) or its N-oxide derivative is optionally in the form of an acid salt derived from an organic or inorganic acid. Also disclosed is a method of its production and its uses, including its use in analyzing a cell or biological material and detecting the emitted fluorescence signal.

Abstract: Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.

Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6, R7 and R8 is selected from X2, and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.

Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.

Abstract: A compound of formula (I): in which A is a C alkylene group with a chain length between NH and N(O)R?R? of at least 2 carbon atoms and R? and R? are each separately selected from C1-4 alkyl groups and C2-4 hydroxyalkyl and C2-4 dihydroxyalkyl groups, or R? and R? together are a C2-6 alkylene group, is formulated so that upon dissolution in aqueous solution the pH of the solution is in the range of 5 to 9. The compound may be in the form of salt with a physiologically acceptable acid having a pKa in the range of ?3.0 (minus 3.0) to 9.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors.

Abstract: Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours.

Abstract: A compound of formula (I): in which A is a C alkylene group with a chain length between NH and N(O)R?R? of at least 2 carbon atoms and R? and R? are each separately selected from C1-4 alkyl groups and C2-4 hydroxyalkyl and C2-4 dihydroxyalkyl groups, or R? and R? together are a C2-6 alkylene group, is formulated so that upon dissolution in aqueous solution the pH of the solution is in the range of 5 to 9. The compound may be in the form of salt with a physiologically acceptable acid having a pKa in the range of ?3.0 (minus 3.0) to 9.

Abstract: There is disclosed a compound of formula (I) wherein each of X1 and X2 are independently NH—A—NR1R2, and wherein A is A C2-8 alkylene and R1 and R2 are independently selected from hydrogen, C1-4 alkyl, C2-4 hydroxy-alkyl and C2-4 aminoalkyl, or R1 and R2 together form a C2-6 alkylene group which with the nitrogen atom to which R1 and R2 are attached forms a heterocyclic ring, or an N-oxide derivative thereof, and wherein the compound (I) or its N-oxide derivative is optionally in the form of an acid salt derived from an organic or inorganic acid. Also disclosed is a method of its production and its uses, including its use in analyzing a cell or biological material and detecting the emitted fluorescence signal.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.