Cancer Research Technology Limited

Spirogen Sarl

Pharminxo Limited

Geoffrey Wells

Andrew David Westwell

Tracey Dawn Poole

Malcolm Francis Graham Stevens

Philip Wilson Howard

David Edwin Thurston

Malcolm Francis G Stevens

Jane Marie Berry

A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; Ris selected from &#x2014;H, &#x2014;OH, =0, &#x2550;CH, &#x2014;CN, &#x2014;R, OR, halo, &#x2550;CH&#x2014;R, O&#x2014;SO&#x2014;R, COR and COR; Ris selected from H, R, OH, OR, SH, SR, NH, NHR, NRR', nitro, MeSn and halo, where R and R&#x2032; are independently selected from optionally substituted Calkyl, Cheterocyclyl and Caryl groups; Rand Reither together form a double bond, or are selected from H and YR, where Y is selected from O, S and NH and R is H or Calkyl or H and SOM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and Ris Calkyl. The compound is useful for the treatment of proliferative diseases. 

Alkyl 4- [4- (5-oxo-2,3,5, 11a-tetrahydo-5H-pyrrolo [2, 1-c] [1,4] benzodiazepine-8-yloxy)-butyrylamino]-1H-pyrrole-2-carboxylate derivatives and related compounds for the treatment of a proliferative disease

A compound of general structure I, wherein the compound is optionally in the form of an N-oxide or S-oxide or prodrug form and/or pharmaceutically acceptable salt thereof wherein:

2-arylbenzothiazole derivatives

This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/thioredoxin reductase inhibitors: formula (I) wherein: Ar is a 1-(sulfonyl)-1H-indol-2-yl group; the bond marked &#x3b1; is independently: (a) a single bond; or: (b) a double bond; the bond marked &#x3b2; is independently: (a) a single bond; or: (b) a double bond; the group &#x2014;ORis independently: (a) &#x2014;OH; (b) an ether group (e.g., &#x2014;OMe); or: (c) an acyloxy (i.e., reverse ester) group (e.g., &#x2014;OC(&#x2550;O)Me); each of R, R, R, and R, is independently a ring substituent and is: (a) H; (b) a monovalent monodentate substituent; or: (c) a ring substituent which, together with an adjacent ring substituent, and together with the ring atoms to which these ring substituents are attached, form a fused ring; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms 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 example, in the treatment of proliferative conditions, (e.g., cancer), and/or conditions mediated by thioredoxin/thioredoxin reductase.

4-(1-(sulfonyl)-1h-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds and analogs thereof as therapeutic agents

The present invention pertains to compounds of the formula (1) which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is &#x2550;O or &#x2550;N&#x2014;S(&#x2550;O)&#x2014;R;Ris &#x2014;II or optionally substituted Calkyl, Cheterocyclyl, or Caryl; Ar is optionally substituted Caryl; Ris an oxy substituent; the bond marked &#x3b1; is a single bond or a double bond; the bond marked &#x3b2; is a single bond or a double bond; Rand Rare each independently ring substituents; Rand Rare each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms 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 example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g., tuberculosis), and/or conditions mediated by thioredoxin/thioredoxin reductase 

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London, United Kingdom

Geoffrey Wells