Abstract: A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein: R1, R2 and R3 are independently H or lower alkyl; R4, R5, R6, R7 and R8 are independently H, halo, lower alkyl or —O-lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R4 to R8, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR14R15)n—O—, where n is 1 or 2 and R14 and R15 are independently H or lower alkyl, and the remainder of R4 to R8 are independently H, halo, lower alkyl or —O-lower alkyl; and R9, R10, R11, R12 and R13 are independently H, halo, lower alkyl or —O— lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R9 to R13, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR16R17)m—O—, where m is 1 or 2 and R16 and R17 are independently H or lower alkyl, and the remainder of R9 to R13 are independently H, halo, lower alkyl or —O-

Abstract: A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein: R1, R2 and R3 are independently H or lower alkyl; R4, R5, R6, R7 and R8 are independently H, halo, lower alkyl or —O-lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R4 to R8, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR14R15)n—O—, where n is 1 or 2 and R14 and R15 are independently H or lower alkyl, and the remainder of R4 to R8 are independently H, halo, lower alkyl or —O-lower alkyl; and R9, R10, R11, R12 and R13 are independently H, halo, lower alkyl or —O— lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R9 to R13, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR16R17)m—O—, where m is 1 or 2 and R16 and R17 are independently H or lower alkyl, and the remainder of R9 to R13 are independently H, halo, lower alkyl or —O-l

Abstract: The present invention pertains to the use of a compounds for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula: wherein: each of RB2, RB3, RB4, and RB5 is independently —H, —OH, or —OMe; each of R1 and R2 is independently: —H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is —H, —OH, —OC(?O)RE, —OS(?O)2OH, or —OP(?O)(OH)2; RE is: —H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

Abstract: The present invention pertains to compounds of the following formula: (1) wherein: RALK is primary or secondary aliphatic saturated C2-6alkyl; each of RB2, RB3, RB4, and RB5 is independently —H, —OH, or —OMe; each of R1 and R2 is independently: —H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is —H, —OH, —OC(?O)RE, —OS(?O)2OH, or —OP(?O)(OH)2; RE is: —H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof.

Abstract: The present invention pertains to compounds of the following formula: (1) wherein: RALK is primary or secondary aliphatic saturated C2-6alkyl; each of RB2, RB3, RB4, and RB5 is independently —H, —OH, or —OMe; each of R1 and R2 is independently: —H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is —H, —OH, —OC(═O)RE, —OS(═O)2OH, or —OP(═O)(OH)2; RE is: —H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

Abstract: The present invention pertains to the use of a compounds for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula: 1

Abstract: The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

Abstract: This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof.

Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Abstract: This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)2(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof.

Abstract: A molecule of formula (I); wherein: X is a halogen, or a substituted sulfonate group; m=1-5; n=1-5; R1, R2=H, C1-4 lower alkyl or C1-4 lower alkyl chain having additional functionality; and the amino group −NR1R2 linked to the anthraquinone is primary, secondary or tertiary or is a tertiary group in the N-oxide form having the formula —N(O)R1R2.

Abstract: A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral acid or base, using a chiral resolving agent. The resolved salt can be esterified, to give the therapeutic agent d-threo-methylphenidate.

Abstract: A process for the preparation of substantially single enantiomer (−)-narwedine comprises seeding a solution of racemic narwedine dissolved in a solvent with substantially single enantiomer (−)-narwedine, provided that if an added amine base is present the ratic solvent:added amine base is greater than 15:1.

Abstract: A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral acid or base, using a chiral resolving agent. The resolved salt can be esterified, to give the therapeutic agent d-threo-methylphenidate.

Abstract: A process for the asymmetric transformation of a racemic compound of formula (I) wherein R1 is H or a alkyl group having up to 20 carbon atoms, R2 is H, or an alkyl, aryl, alkaryl or aralkyl group having up to 20 carbon atoms, and X is H, a halogen atom, tert-butyl, or any other removable substituent, comprises reaction of racemic compound (I) with an enantiomerically-enriched acid HY*, wherein Y* is a chiral group, to form a diastereomeric salt of compound (I) having Y* as a counterion. The salt obtained can then be reduced to give enantiomerically-enriched galanthamine, or a derivative thereof.

Abstract: The subject invention pertains to optically-enriched compounds of formula (1), wherein Ar is a C.sub.6-20 aryl group; and R.sup.1 and R.sup.2 are independently H, alkyl or aryl. The subject invention also pertains to method of preparing these compounds. The subject compounds can be prepared by reduction of the corresponding 1,4-dihydropyridine-3-aldehyde, e.g., using hydrogen an a catalyst. The aldehyde can be prepared by hydrolytic cleavage of an aminal obtainable by the reaction of 3-pyridinecarboxaldehyde and a chiral C-2 symmetric diamine, an then stereoselective introduction of the Ar and COOCHR.sup.1 R.sup.2 groups.

Abstract: Process for obtaining an enantiomerically enriched N-acylazetine-2-carboxylic acid by selectine crystallization of a diastereoisomeric salt formed by relcting an enantiomer of the N-acylazetidine-2-carboxylic acid and an enantiomer of 1-phenylethylamine.

Abstract: A process for racemising an optically-enriched chiral amine of the formula: R.sup.1 --CH(NR.sup.3 R.sup.4)--R.sup.2, wherein R.sup.1 is aromatic or unsaturated alkyl; R.sup.2 is aromatic or alkyl; and R.sup.3 and R.sup.4 are independently selected from hydrogen, alkyl and aryl; and wherein any combination(s) of two of the R groups may form a ring; comprises treatment of the optically-enriched amine with a metal hydroxide in an aprotic polar solvent.

Abstract: A process is described for obtaining a single enantiomer from a racemic mixture of the bicyclic lactam 2-azabicyclo?2.2. 1! hept-5-en-one by seeding a supersaturated solution of the lactam and a solvent with a single enantiomer of the lactam.