Chirotech Technology Limited

Spear Therapeutics Limited

Janssen Pharmaceutica Nv

De Montfort University

Astra Ab

Medeva Europe Limited

De Montford University

Gerard Andrew Potter

Brian Michael Adger

Jane Marie Paul

Michael Danny Burke

Lawrence Hylton Patterson

Paul Crispin Butler

Raymond McCague

Hooshang Shahriari Zavareh

Martin Edward Fox

Philip Huxley

Nicholas Bernard Johnson

Peter David Tiffin

Stephen John Taylor

David Andrew Chaplin

Paul Henry Teesdale-Spittle

Laurence Hylton Patterson

Kenneth James Beresford

Taeeba Ijaz

Michael C Harris

Zennia Paniwynk

A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein:

Compounds

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 R, R, R, and Ris independently &#x2014;H, &#x2014;OH, or &#x2014;OMe; each of Rand Ris independently: &#x2014;H, optionally substituted Calkyl, or optionally substituted Caryl; Ris &#x2014;H, &#x2014;OH, &#x2014;OC(&#x2550;O)R, &#x2014;OS(&#x2550;O)OH, or &#x2014;OP(&#x2550;O)(OH); Ris: &#x2014;H, optionally substituted Calkyl, optionally substituted Cheterocyclyl, or optionally substituted Caryl; 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.

3,4-methylenedioxy-substituted chalcones as therapeutic agents

The present invention pertains to compounds of the following formula: (1) wherein: Ris primary or secondary aliphatic saturated Calkyl; each of R, R, R, and Ris independently &#x2014;H, &#x2014;OH, or &#x2014;OMe; each of Rand Ris independently: &#x2014;H, optionally substituted Calkyl, or optionally substituted Caryl; Ris &#x2014;H, &#x2014;OH, &#x2014;OC(&#x2550;O)R, &#x2014;OS(&#x2550;O)OH, or &#x2014;OP(&#x2550;O)(OH); Ris: &#x2014;H, optionally substituted Calkyl, optionally substituted Cheterocyclyl, or optionally substituted Caryl; 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 

4-(c2-6alkoxy)-substituted chalcones as therapeutic agents

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.

Hydroxylation activated drug release

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.

Hydroxylation activated prodrugs

Anthraquinone anticancer drugs

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.

Resolution of ritalinic acid salt

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

Process for preparing single enantiomer narwedine

A process for the asymmetric transformation of a racemic compound of formula (I) wherein R is H or a alkyl group having up to 20 carbon atoms, R 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.

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Leicester, United Kingdom

Gerard Andrew Potter